oxadiazoles

Summary

Top Publications

  1. ncbi Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists
    Yuan Cheng
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 51:5019-34. 2008
  2. ncbi PTC124 targets genetic disorders caused by nonsense mutations
    Ellen M Welch
    PTC Therapeutics, 100 Corporate Court, South Plainfield, New Jersey 07080, USA
    Nature 447:87-91. 2007
  3. ncbi [1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding
    Michael D Shultz
    Novartis Institutes for BioMedical Research, Inc, Cambridge, Massachusetts 02319, United States
    J Med Chem 55:1127-36. 2012
  4. pmc PTC124 is an orally bioavailable compound that promotes suppression of the human CFTR-G542X nonsense allele in a CF mouse model
    Ming Du
    Department of Microbiology and Gregory Fleming James Cystic Fibrosis Research Center, University of Alabama at Birmingham, Birmingham, AL 35294, USA
    Proc Natl Acad Sci U S A 105:2064-9. 2008
  5. ncbi PTC124 improves readthrough and increases enzymatic activity of the CPT1A R160X nonsense mutation
    Lu Tan
    Department of Pathology and Laboratory Medicine, Children s Hospital of Philadelphia, Philadelphia, PA, USA
    J Inherit Metab Dis 34:443-7. 2011
  6. pmc Identification of oxadiazoles as new drug leads for the control of schistosomiasis
    Ahmed A Sayed
    Department of Biological Sciences, Illinois State University, Normal, Illinois 61790, USA
    Nat Med 14:407-12. 2008
  7. ncbi Safety, tolerability, and pharmacokinetics of PTC124, a nonaminoglycoside nonsense mutation suppressor, following single- and multiple-dose administration to healthy male and female adult volunteers
    Samit Hirawat
    PTC Therapeutics, Inc, 100 Corporate Court, South Plainfield, NJ 07080, USA
    J Clin Pharmacol 47:430-44. 2007
  8. ncbi PTC124-mediated translational readthrough of a nonsense mutation causing Usher syndrome type 1C
    T Goldmann
    Department of Cell and Matrix Biology, Institute of Zoology, Johannes Gutenberg University Mainz, D 55099 Mainz, Germany
    Hum Gene Ther 22:537-47. 2011
  9. ncbi Comparison of the novel angiotensin II receptor blocker azilsartan medoxomil vs valsartan by ambulatory blood pressure monitoring
    Domenic Sica
    Section of Clinical Pharmacology and Hypertension, Virginia Commonwealth University, Richmond, VA 23298 0160, USA
    J Clin Hypertens (Greenwich) 13:467-72. 2011
  10. ncbi Effectiveness of PTC124 treatment of cystic fibrosis caused by nonsense mutations: a prospective phase II trial
    Eitan Kerem
    Hadassah Hebrew University Hospital, Jerusalem, Israel
    Lancet 372:719-27. 2008

Research Grants

Detail Information

Publications255 found, 100 shown here

  1. ncbi Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists
    Yuan Cheng
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 51:5019-34. 2008
    ..This effort resulted in identification of 63 that is a potent and selective agonist at CB2 (EC50 = 2 nM, Emax = 110%) with excellent pharmacokinetic properties...
  2. ncbi PTC124 targets genetic disorders caused by nonsense mutations
    Ellen M Welch
    PTC Therapeutics, 100 Corporate Court, South Plainfield, New Jersey 07080, USA
    Nature 447:87-91. 2007
    ....
  3. ncbi [1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding
    Michael D Shultz
    Novartis Institutes for BioMedical Research, Inc, Cambridge, Massachusetts 02319, United States
    J Med Chem 55:1127-36. 2012
    ..Furthermore, a cocrystal structure of compound 24 complexed to TNKS1 demonstrates an alternate binding mode for PARP family member proteins that does not involve interactions with the nicotinamide binding pocket...
  4. pmc PTC124 is an orally bioavailable compound that promotes suppression of the human CFTR-G542X nonsense allele in a CF mouse model
    Ming Du
    Department of Microbiology and Gregory Fleming James Cystic Fibrosis Research Center, University of Alabama at Birmingham, Birmingham, AL 35294, USA
    Proc Natl Acad Sci U S A 105:2064-9. 2008
    ....
  5. ncbi PTC124 improves readthrough and increases enzymatic activity of the CPT1A R160X nonsense mutation
    Lu Tan
    Department of Pathology and Laboratory Medicine, Children s Hospital of Philadelphia, Philadelphia, PA, USA
    J Inherit Metab Dis 34:443-7. 2011
    ..Our results provide additional evidence for proof of principle that PTC124 is a potential therapeutic agent for treating patients with any genetic condition that results from a nonsense mutation...
  6. pmc Identification of oxadiazoles as new drug leads for the control of schistosomiasis
    Ahmed A Sayed
    Department of Biological Sciences, Illinois State University, Normal, Illinois 61790, USA
    Nat Med 14:407-12. 2008
    ..The compound was active against the three major schistosome species infecting humans. These protective effects exceed benchmark activity criteria set by the World Health Organization for lead compound development for schistosomiasis...
  7. ncbi Safety, tolerability, and pharmacokinetics of PTC124, a nonaminoglycoside nonsense mutation suppressor, following single- and multiple-dose administration to healthy male and female adult volunteers
    Samit Hirawat
    PTC Therapeutics, Inc, 100 Corporate Court, South Plainfield, NJ 07080, USA
    J Clin Pharmacol 47:430-44. 2007
    ..PTC124 pharmacokinetics were described by a 1-compartment model. Collectively, the data support initiation of phase II studies of PTC124 in patients with nonsense mutation-mediated cystic fibrosis and Duchenne muscular dystrophy...
  8. ncbi PTC124-mediated translational readthrough of a nonsense mutation causing Usher syndrome type 1C
    T Goldmann
    Department of Cell and Matrix Biology, Institute of Zoology, Johannes Gutenberg University Mainz, D 55099 Mainz, Germany
    Hum Gene Ther 22:537-47. 2011
    ..Its high readthrough efficiency in combination with excellent biocompatibility makes PTC124 a promising therapeutic agent for PTCs in USH1C, as well as other ocular and nonocular genetic diseases...
  9. ncbi Comparison of the novel angiotensin II receptor blocker azilsartan medoxomil vs valsartan by ambulatory blood pressure monitoring
    Domenic Sica
    Section of Clinical Pharmacology and Hypertension, Virginia Commonwealth University, Richmond, VA 23298 0160, USA
    J Clin Hypertens (Greenwich) 13:467-72. 2011
    ..These findings suggest that AZL-M could provide higher rates of hypertension control compared with other ARBs in the class...
  10. ncbi Effectiveness of PTC124 treatment of cystic fibrosis caused by nonsense mutations: a prospective phase II trial
    Eitan Kerem
    Hadassah Hebrew University Hospital, Jerusalem, Israel
    Lancet 372:719-27. 2008
    ..PTC124 is an orally bioavailable small molecule that is designed to induce ribosomes to selectively read through premature stop codons during mRNA translation, to produce functional CFTR...
  11. ncbi Chronic ataluren (PTC124) treatment of nonsense mutation cystic fibrosis
    M Wilschanski
    Paediatric Gastroenterology, Hadassah University Hospital, Mount Scopus POB 24035, Jerusalem, 91240, Israel
    Eur Respir J 38:59-69. 2011
    ..Adverse clinical and laboratory findings were uncommon and usually mild. Chronic ataluren administration produced time-dependent improvements in CFTR activity and clinical parameters with generally good tolerability...
  12. ncbi A role for intestinal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like Peptide-1 and glucose-dependent insulinotropic Peptide release
    Zhi Liang Chu
    Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA
    Endocrinology 149:2038-47. 2008
    ..These data also suggest that combined stimulation of incretin hormone release and protection against incretin hormone degradation may be an effective antidiabetic strategy...
  13. ncbi Effects of the angiotensin receptor blocker azilsartan medoxomil versus olmesartan and valsartan on ambulatory and clinic blood pressure in patients with stages 1 and 2 hypertension
    William B White
    Division of Hypertension and Clinical Pharmacology, Calhoun Cardiology Center, University of Connecticut Health Center, 263 Farmington Ave, Farmington, CT 06030 3940, USA
    Hypertension 57:413-20. 2011
    ..Azilsartan medoxomil could provide higher rates of hypertension control within the ARB class...
  14. ncbi Synthesis, antimicrobial, and anti-inflammatory activities of novel 2-(1-adamantyl)-5-substituted-1,3,4-oxadiazoles and 2-(1-adamantylamino)-5-substituted-1,3,4-thiadiazoles
    Adnan A Kadi
    Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
    Eur J Med Chem 42:235-42. 2007
    ..derivatives 3a-j, which were cyclized to the corresponding 2-(1-adamantyl)-5-substituted-1,3,4-oxadiazoles 4a-j via heating with phosphorus oxychloride...
  15. ncbi A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release
    Zhi Liang Chu
    Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
    Endocrinology 148:2601-9. 2007
    ..Diabetic KK/A(y) mice were also highly responsive to AR231453. Orally active GPR119 agonists may offer significant promise as novel antihyperglycemic agents acting in a glucose-dependent fashion...
  16. pmc Read-through compound 13 restores dystrophin expression and improves muscle function in the mdx mouse model for Duchenne muscular dystrophy
    Refik Kayali
    Department of Neurology, David Geffen School of Medicine, University of California, Los Angeles, CA 90095, USA
    Hum Mol Genet 21:4007-20. 2012
    ..These studies establish the therapeutic potential of RTC13 in vivo and advance this newly identified compound into preclinical application for DMD...
  17. ncbi Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker
    Takashi Kajiya
    Department of Cardiovascular, Respiratory and Metabolic Medicine, Graduate School of Medicine, Kagoshima University, Kagoshima, Japan
    J Hypertens 29:2476-83. 2011
    ..Although azilsartan is considered to be an unusually potent angiotensin II type 1 (AT1) receptor antagonist, little is known about the potential pleiotropic effects of this molecule...
  18. ncbi In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies
    Mami Ojima
    Pharmacology Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd, Osaka, Japan
    J Pharmacol Exp Ther 336:801-8. 2011
    ..Its tight receptor binding might be expected to produce potent and long-lasting antihypertensive effects in preclinical and clinical settings...
  19. ncbi Multiple independent binding sites for small-molecule inhibitors on the oncoprotein c-Myc
    Dalia I Hammoudeh
    Department of Chemistry, Georgetown University, Washington, District of Columbia 20057, USA
    J Am Chem Soc 131:7390-401. 2009
    ..A rational and generic approach to the inhibition of protein-protein interactions involving ID proteins may therefore be possible through the targeting of ID sequence...
  20. ncbi The comparative effects of azilsartan medoxomil and olmesartan on ambulatory and clinic blood pressure
    George L Bakris
    Hypertensive Diseases Unit, University of Chicago Pritzker School of Medicine, Chicago, IL 60637, USA
    J Clin Hypertens (Greenwich) 13:81-8. 2011
    ..0 to -0.1; P=.038), while AZL-M 40 mg was noninferior to OLM-M 40 mg. The side effect profiles of both ARBs were similar to placebo. AZL-M is well tolerated and more efficacious at its maximal dose than the highest dose of OLM-M...
  21. ncbi Introducing sense into nonsense in treatments of human genetic diseases
    Liat Linde
    Department of Genetics, The Life Sciences Institute, Givat Ram Campus, The Hebrew University, Jerusalem 91904, Israel
    Trends Genet 24:552-63. 2008
    ..A deeper understanding of the molecular basis for variable response to readthrough of PTCs is necessary so that appropriate therapies can be developed to treat many human genetic diseases caused by PTCs...
  22. pmc Differential pharmacology and benefit/risk of azilsartan compared to other sartans
    Theodore W Kurtz
    Department of Laboratory Medicine, University of California, San Francisco, CA 94107, USA
    Vasc Health Risk Manag 8:133-43. 2012
    ....
  23. ncbi Oxadiazoles in medicinal chemistry
    Jonas Boström
    AstraZeneca R and D Molndal, S 431 83 Molndal, Sweden
    J Med Chem 55:1817-30. 2012
    b>Oxadiazoles are five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom, and they exist in different regioisomeric forms...
  24. ncbi Synthesis, crystal structure and anti-HIV activity of 2-adamantyl/adamantylmethyl-5-aryl-1,3,4-oxadiazoles
    Mahmood Ul Hassan Khan
    Department of Chemistry, Quaid i Azam University, Islamabad 45320, Pakistan
    Med Chem 8:1190-7. 2012
    Two series of 2-adamantyl/adamantylmethyl-5-aryl-1,3,4-oxadiazoles (4a-l and 5a-l) were synthesized by cyclodehydration of adamantan-1-carboxylic acid/adamantylacetic acid with various aryl hydrazides (3a-l) in the presence of POCl(3)...
  25. pmc Pharmacophore identification of c-Myc inhibitor 10074-G5
    Jeremy L Yap
    Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 N Pine St, Baltimore, MD 21201, USA
    Bioorg Med Chem Lett 23:370-4. 2013
    ..Importantly, the carboxylic acid of JY-3-094 improves the physicochemical properties of the lead compound, which will facilitate the incorporation of additional hydrophobicity that might enhance Myc inhibitory activity further still...
  26. ncbi Antibacterial activity of chalcones, hydrazones and oxadiazoles against methicillin-resistant Staphylococcus aureus
    Thaís Moreira Osório
    Laboratório de Antibióticos, Universidade Federal de Santa Catarina UFSC, Campus Trindade, CEP 88040 900 Florianópolis, SC, Brazil
    Bioorg Med Chem Lett 22:225-30. 2012
    ..In this context, chalcones, dihydrochalcones, hydrazones and oxadiazoles were tested against Staphylococcus aureus ATCC 25923 and methicillin-resistant S...
  27. pmc Ataluren as an agent for therapeutic nonsense suppression
    Stuart W Peltz
    PTC Therapeutics, Inc, South Plainfield, New Jersey 07080, USA
    Annu Rev Med 64:407-25. 2013
    ....
  28. pmc Membrane blebbing as an assessment of functional rescue of dysferlin-deficient human myotubes via nonsense suppression
    Bingjing Wang
    University of Pennsylvania School of Medicine, Department of Physiology, B400 Richards Bldg, 3700 Hamilton Walk, Philadelphia, PA 19104 6085, USA
    J Appl Physiol (1985) 109:901-5. 2010
    ..Thus ataluren is a potential therapeutic for dysferlin-deficient patients harboring nonsense mutations...
  29. ncbi Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles
    V Padmavathi
    Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India
    Eur J Med Chem 44:2106-12. 2009
    A new class of 1,3,4-oxadiazoles were prepared from acid hydrazides on treatment with different carboxylic acids in the presence of phosphorus oxychloride...
  30. ncbi Azilsartan medoxomil: a new Angiotensin receptor blocker
    Kathy Zaiken
    Massachusetts College of Pharmacy and Health Sciences and Harvard Vanguard Medical Associates, Boston, MA, USA
    Clin Ther 33:1577-89. 2011
    ..Azilsartan medoxomil is an angiotensin receptor blocker, approved on February 25, 2011 by the US Food and Drug Administration (FDA) for hypertension management...
  31. ncbi Synthesis and antifungal activity of novel sulfoxide derivatives containing trimethoxyphenyl substituted 1,3,4-thiadiazole and 1,3,4-oxadiazole moiety
    Fang Liu
    Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China
    Bioorg Med Chem 16:3632-40. 2008
    ..After treating with compound 10a at 100 microg/mL for 12 h, the mycelial reducing sugar, D-GlcNAc, soluble protein and pyruvate content, chitinase activity showed declining tendency...
  32. pmc In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization
    Dana M Clausen
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania 15213, USA
    J Pharmacol Exp Ther 335:715-27. 2010
    ..Our identification of 10074-G5 metabolites in mice will help design new, more metabolically stable small-molecule inhibitors of c-Myc...
  33. pmc Synthesis and evaluation of a series of 2-substituted-5-thiopropylpiperazine (piperidine)-1,3,4-oxadiazoles derivatives as atypical antipsychotics
    Yin Chen
    Department of Systems Biology, Huazhong University of Science and Technology, Wuhan, China
    PLoS ONE 7:e35186. 2012
    ....
  34. ncbi AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines
    Dana S Levy
    Oncology Biology, GlaxoSmithKline, Collegeville, PA 19426, USA
    Blood 113:1723-9. 2009
    ..Overall, our data provide direct evidence for the role of AKT signaling in various hematologic malignancies, especially ALL and some lymphomas...
  35. ncbi Synthesis of novel sulfonamide-1,2,4-triazoles, 1,3,4-thiadiazoles and 1,3,4-oxadiazoles, as potential antibacterial and antifungal agents. Biological evaluation and conformational analysis studies
    P Zoumpoulakis
    Laboratory of Molecular Analysis, Institute of Organic and Pharmaceutical Chemistry, National Hellenic Research Foundation, 48 Vas Constantinou Ave, 11635 Athens, Greece
    Bioorg Med Chem 20:1569-83. 2012
    ..we designed the synthesis of a series of novel sulfonamide-1,2,4-triazoles, -1,3,4-thiadiazoles and -1,3,4-oxadiazoles emphasizing, in particular, on the strategy of combining two chemically different but pharmacologically ..
  36. pmc Read-through strategies for suppression of nonsense mutations in Duchenne/ Becker muscular dystrophy: aminoglycosides and ataluren (PTC124)
    Richard S Finkel
    Division of Neurology, The Children s Hospital of Philadelphia, Philadelphia, PA 19104, USA
    J Child Neurol 25:1158-64. 2010
    ..Use of nonsense mutation suppression in Duchenne/Becker muscular dystrophy may offer the prospect of targeting the specific mutation causing the disease and correcting the fundamental pathophysiology...
  37. ncbi Microwave assisted one pot synthesis of some novel 2,5-disubstituted 1,3,4-oxadiazoles as antifungal agents
    Jaiprakash N Sangshetti
    Department of Chemical Technology, Dr Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, MS, India
    Bioorg Med Chem Lett 21:444-8. 2011
    ..Some of the compounds from the series like 8k was equipotent with miconazole against Candida albicans and Fusarium oxysporum. Also compound 8n was equipotent with miconazole against F. oxysporum...
  38. ncbi Rescue of melanocortin 4 receptor (MC4R) nonsense mutations by aminoglycoside-mediated read-through
    Harald Brumm
    Institute of Experimental Pediatric Endocrinology, Charite Universitatsmedizin Berlin, Berlin, Germany
    Obesity (Silver Spring) 20:1074-81. 2012
    ..Restoration of full-length proteins by PTC124 could not be confirmed. Future pharmaceutical applications must consider the potency of aminoglycosides to restore receptor function as well as the ability to pass the blood-brain barrier...
  39. ncbi The chemical compound PTC124 does not affect cellular electrophysiology of cardiac ventricular myocytes
    Tamara T Koopmann
    Heart Failure Research Center, Department of Clinical and Experimental Cardiology, Academic Medical Center, Amsterdam, The Netherlands
    Cardiovasc Drugs Ther 26:41-5. 2012
    ..In this study, we tested the acute and long-term effects of PTC124 on action potential characteristics of rabbit ventricular cardiomyocytes...
  40. ncbi Discovery and structure-activity relationship of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers and potential anticancer agents
    Han Zhong Zhang
    Maxim Pharmaceuticals Inc, 6650 Nancy Ridge Drive, San Diego, CA 92121, USA
    J Med Chem 48:5215-23. 2005
    ..Therefore, our cell-based chemical genetics approach for the discovery of apoptosis inducers can identify potential anticancer agents as well as their molecular targets...
  41. ncbi Ultrasound-promoted synthesis of 3-trichloromethyl-5-alkyl(aryl)-1,2,4-oxadiazoles
    Lizandra C Bretanha
    NuQuiA Núcleo de Química Aplicada, Departamento de Quimica Organica, Universidade Federal de Pelotas, Brazil
    Ultrason Sonochem 18:704-7. 2011
    The alternative synthesis of 12 1,2,4-oxadiazoles using ultrasound irradiation from trichloroacetoamidoxime and acyl chlorides is reported. Seven of them are novel compounds...
  42. ncbi Development of an HPLC-fluorescence determination method for carboxylic acids related to the tricarboxylic acid cycle as a metabolome tool
    Kazuyuki Kubota
    Laboratory of Bio Analytical Chemistry, Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7 3 1, Hongo, Bunkyo ku, Tokyo 113 0033, Japan
    Biomed Chromatogr 19:788-95. 2005
    ..The method will also be useful for metabolome research, such as for target analyses of metabolites with carboxyl groups, not only in urine but also in cells and organs...
  43. pmc Distinct molecular requirements for activation or stabilization of soluble guanylyl cyclase upon haem oxidation-induced degradation
    L S Hoffmann
    Pharma Research Centre, Bayer HealthCare, Aprather Weg 18a, Wuppertal, Germany
    Br J Pharmacol 157:781-95. 2009
    ....
  44. ncbi A fluorogenic reagent, 4-mercapto-7-methylthio-2,1,3-benzoxadiazole for carboxylic acids, designed by prediction of the fluorescence intensity
    S Uchiyama
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Japan
    Anal Chem 73:2165-70. 2001
    ..The superiority was examined in terms of its reactivity and sensitivity and the avoidance of interfering peaks that were derived from the reagent itself or degradation products in the chromatogram...
  45. ncbi 2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors
    Ester Muraglia
    IRBM Merck Research Laboratories Rome, Via Pontina Km 30, 600 Pomezia, 00040 Rome, Italy
    Bioorg Med Chem Lett 18:6083-7. 2008
    ..Exploration of replacements for the carboxamide with bioisosteric pentatomic heteroaromatic like 1,3,4-oxadiazoles, 1,2,4-oxadiazoles and 1,3-thiazoles, led to the discovery that 2-trifluoroacetylthiophene 1,3,4-oxadiazole ..
  46. ncbi Novel 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives: promising anticancer agents
    Ahmed S Aboraia
    Pharmaceutical Medicinal Chemistry Department, Faculty of Pharmacy, Assiut University, Egypt
    Bioorg Med Chem 14:1236-46. 2006
    ..Compounds 3j and 3k proved to be the active members in this study compared to 5-fluorouracil and cyclophosphamide as reference drugs, respectively. Compounds 3j and 3k were identified as promising lead compounds...
  47. ncbi The molecular mechanism of human hormone-sensitive lipase inhibition by substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones
    Yassine Ben Ali
    Organization and Dynamics of Biological Membranes, UMR 5246 ICBMS, CNRS Universite Claude Bernard Lyon 1, Batiment Raulin, 43, Boulevard du 11 Novembre 1918, 69622 Villeurbanne Cedex, France
    Biochimie 94:137-45. 2012
    ..On the basis of this study, a kinetic model is proposed to describe the inhibition of HSL by compound 7600 in the aqueous phase as well as its partial reactivation at the lipid-water interface...
  48. ncbi In vivo electrophysiological assessment of the putative antidepressant Wf-516 in the rat raphe dorsalis, locus coeruleus and hippocampus
    M el Mansari
    University of Ottawa Institute of Mental Health Research, Room 7407, 1145 Carling Avenue, Ottawa, ON K1Z 7K4, Canada
    Naunyn Schmiedebergs Arch Pharmacol 376:351-61. 2008
    ..These properties of WF-516 define the transporter/receptorial profile of an antidepressant with superior effectiveness...
  49. ncbi Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles
    Zareen Amtul
    International Center for Chemical Sciences, HEJ Research Institute of Chemistry, University of Karachi, Karachi 75270, Pakistan
    Biochem Biophys Res Commun 319:1053-63. 2004
    ..Because of their safe profile in the genotoxic assay, they may be pursued in the near future for human testing..
  50. ncbi 2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors
    Harish Rajak
    Medicinal Chemistry Research Laboratory, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur 495 009, CG, India
    Bioorg Med Chem Lett 21:5735-8. 2011
    ..The results of the present studying indicates 2,5-disubstituted 1,3,4-oxadiazole/thiadiazole as promising surface recognition moiety for development of newer hydroxamic acid based histone deacetylase inhibitor...
  51. pmc Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis
    Ganesha Rai
    NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, Maryland 20892 3370, USA
    J Med Chem 52:6474-83. 2009
    ..The results of these studies verify the utility of oxadiazole-2-oxides as novel inhibitors of TGR and as efficacious antischistosomal agents...
  52. ncbi Azilsartan medoxomil: a new angiotensin II receptor antagonist for treatment of hypertension
    William L Baker
    School of Pharmacy, University of Connecticut, Farmington, CT, USA
    Ann Pharmacother 45:1506-15. 2011
    ....
  53. ncbi Selective, reversible caspase-3 inhibitor is neuroprotective and reveals distinct pathways of cell death after neonatal hypoxic-ischemic brain injury
    Byung Hee Han
    Department of Neurology, Washington University, St Louis, Missouri 63110, USA
    J Biol Chem 277:30128-36. 2002
    ....
  54. pmc Mechanism of PTC124 activity in cell-based luciferase assays of nonsense codon suppression
    Douglas S Auld
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892 3370, USA
    Proc Natl Acad Sci U S A 106:3585-90. 2009
    ..Our results demonstrate the value of understanding potential interactions between reporter enzymes and chemical compounds and emphasize the importance of implementing the appropriate control assays before interpreting HTS results...
  55. ncbi S1P(1)-selective agonist, SEW2871, ameliorates ischemic acute renal failure
    Y Hh Lien
    Section of Nephrology, Department of Medicine, University of Arizona College of Medicine, Tucson, Arizona, USA
    Kidney Int 69:1601-8. 2006
    ..This new class of renoprotective agent shows promise as a novel approach in preventing/treating ischemic acute renal failure...
  56. ncbi Selective sphingosine 1-phosphate 1 receptor activation reduces ischemia-reperfusion injury in mouse kidney
    Alaa S Awad
    Department of Medicine, Univ of Virginia, Charlottesville, VA, USA
    Am J Physiol Renal Physiol 290:F1516-24. 2006
    ..The mechanism of protection is not known but may be related to peripheral lymphocyte depletion or direct effects on kidney cells expressing S1P1 receptor...
  57. ncbi Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity
    Nelson Rhodes
    Oncology Biology, GlaxoSmithKline, Collegeville, PA 19426, USA
    Cancer Res 68:2366-74. 2008
    ..Immunohistochemical analysis of tumor xenografts after repeat dosing with GSK690693 showed reductions in phosphorylated Akt substrates in vivo. These results support further evaluation of GSK690693 as an anticancer agent...
  58. ncbi Utility of small-animal positron emission tomographic imaging of rats for preclinical development of drugs acting on the serotonin transporter
    Takeaki Saijo
    Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan
    Int J Neuropsychopharmacol 12:1021-32. 2009
    ....
  59. ncbi The angiotensin receptor blocker, azilsartan medoxomil (TAK-491), suppresses vascular wall expression of plasminogen activator inhibitor type-I protein potentially facilitating the stabilization of atherosclerotic plaques
    Christopher J French
    Department of Medicine, Cardiovascular Research Institute, University of Vermont, Burlington, VT, USA
    J Cardiovasc Pharmacol 58:143-8. 2011
    ..Accordingly, the suppression of PAI-1 expression by AZL-M may attenuate the evolution of atherosclerotic plaques vulnerable to rupture...
  60. ncbi Synthesis, fungicidal activity, and 3D-QSAR of pyridazinone-substituted 1,3,4-oxadiazoles and 1,3,4-thiadiazoles
    Xia Juan Zou
    State Key Laboratory for Structural Chemistry Studies of Stable and Unstable Species, Institute of Physical Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing, P R China, 100871
    J Agric Food Chem 50:3757-60. 2002
    A series of novel 5-[1-aryl-1,4-dihydro-6-methylpyridazin-4-one-3-yl] -2-arylamino-1,3,4-oxadiazoles, fungicidally active, were synthesized based on bioisosterism and tested in vivo against wheat leaf rust, Puccinia recondita...
  61. ncbi TAK-536, a new AT1 receptor blocker, improves glucose intolerance and adipocyte differentiation
    Masaru Iwai
    Department of Molecular Cardiovascular Biology and Pharmacology, Ehime University Graduate School of Medicine, Shitsukawa, Tohon, Ehime, Japan
    Am J Hypertens 20:579-86. 2007
    ..The effects of a new AT(1) receptor blocker (ARB), TAK-536, on insulin resistance were explored using type 2 diabetic KK-A(y) mice and compared with those of candesartan cilexetil (candesartan)...
  62. ncbi Pleconaril, a novel antipicornaviral agent
    Naomi R Florea
    Department of Pharmacy Research, Hartford Hospital, Hartford, Connecticut 06102, USA
    Pharmacotherapy 23:339-48. 2003
    ..It shows promising results in treatment of picornaviral respiratory tract infections, meningitis, and other life-threatening infections...
  63. pmc Emerging genetic therapies to treat Duchenne muscular dystrophy
    Stanley F Nelson
    Department of Physiological Science, UCLA, Los Angeles, CA 90095 7334, USA
    Curr Opin Neurol 22:532-8. 2009
    ..The purpose of this review is to highlight two emerging therapies designed to repair the primary genetic defect, called 'exon skipping' and 'nonsense codon suppression'...
  64. ncbi Azilsartan treatment improves insulin sensitivity in obese spontaneously hypertensive Koletsky rats
    M Zhao
    Department of Medicine and Clinical Science, Kyoto University Graduate School of Medicine, Kyoto, Japan
    Diabetes Obes Metab 13:1123-9. 2011
    ..We investigated the metabolic effects of the new angiotensin II type 1 receptor blocker azilsartan using the obese Koletsky rats superimposed on the background of the spontaneously hypertensive rats...
  65. ncbi Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models
    Keiji Kusumoto
    Metabolic Disease Drug Discovery Unit, Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, Osaka, Japan
    Eur J Pharmacol 669:84-93. 2011
    ..These results suggest that azilsartan medoxomil is a potent angiotensin II receptor blocker that has an attractive pharmacological profile as an antihypertensive agent...
  66. ncbi Defects in cGMP-PKG pathway contribute to impaired NO-dependent responses in hepatic stellate cells upon activation
    Roman E Perri
    Gastroenterology Research Unit, Department of Physiology, and Tumor Biology Program, Mayo Clinic, 200 First St SW, Rochester, MN 55905, USA
    Am J Physiol Gastrointest Liver Physiol 290:G535-42. 2006
    ..Activating targets downstream from NO-cGMP in activated HSC may represent a novel therapeutic target for portal hypertension...
  67. ncbi Synthesis and biological evaluation of radioiodinated 2,5-diphenyl-1,3,4-oxadiazoles for detecting beta-amyloid plaques in the brain
    Hiroyuki Watanabe
    Graduate School of Biomedical Sciences, Nagasaki University, 1 14 Bunkyo machi, Nagasaki 852 8521, Japan
    Bioorg Med Chem 17:6402-6. 2009
    ..The novel radioiodinated 1,3,4-DPOD derivatives may be useful probes for detecting beta-amyloid plaques in the Alzheimer's brain...
  68. pmc Peripheral analgesic blockade of hypernociception: activation of arginine/NO/cGMP/protein kinase G/ATP-sensitive K+ channel pathway
    Daniela Sachs
    Department of Pharmacology, Faculty of Medicine of Ribeirao Preto, University of Sao Paulo, Ribeirao Preto, 14049 900, Sao Paulo, Brazil
    Proc Natl Acad Sci U S A 101:3680-5. 2004
    ....
  69. ncbi Pharmaceuticals targeting nonsense mutations in genetic diseases: progress in development
    Steven M Rowe
    Department of Medicine, University of Alabama at Birmingham, Birmingham, AL 35233, USA
    BioDrugs 23:165-74. 2009
    ..These results, coupled with our improved understanding of how translation termination is regulated at PTCs, will help guide future directions of research involving this innovative treatment strategy for genetic diseases...
  70. pmc Role of Rho-kinase in mediating contraction of chicken embryo femoral arteries
    Bea Zoer
    Department of Pediatrics, Maastricht University Medical Centre, School for Oncology and Developmental Biology GROW, P Debyelaan 25, P O Box 5800, 6202 AZ Maastricht, The Netherlands
    J Comp Physiol B 180:427-35. 2010
    ..In summary, our findings are indicative of a role for Rho-kinase activity in depolarization- and agonist-induced force generation in chicken embryo femoral arteries...
  71. ncbi Synthesis, characterization and antimicrobial activity of some disubstituted 1,3,4-oxadiazoles carrying 2-(aryloxymethyl)phenyl moiety
    Channamata Shankara Naveena
    Department of Chemistry, Mangalore University, Mangalagangothri 575199, Karnataka, India
    Eur J Med Chem 45:4708-19. 2010
    ..All the synthesized compounds were screened for their in vitro antibacterial and antifungal activity and some of them exhibited good activity...
  72. pmc Nitric oxide-soluble guanylyl cyclase signaling regulates corticostriatal transmission and short-term synaptic plasticity of striatal projection neurons recorded in vivo
    Stephen Sammut
    Department of Neuroscience, Rosalind Franklin University of Medicine and Science, North Chicago, IL 60064, USA
    Neuropharmacology 58:624-31. 2010
    ..Moreover, phasic activation of NO signaling is likely to regulate short-term changes in corticostriatal synaptic plasticity via complex mechanisms involving both sGC-cGMP-dependent and independent pathways...
  73. ncbi Synthesis, characterization, and in vitro antimicrobial activities of 5-alkenyl/hydroxyalkenyl-2-phenylamine-1,3,4-oxadiazoles and thiadiazoles
    Nida N Farshori
    Department of Chemistry, Aligarh Muslim University, Aligarh, India
    Bioorg Med Chem Lett 20:1933-8. 2010
    ..and thiosemicarbazides (4a-d), which on further refluxing with POCl(3) and Ac(2)O yielded corresponding 1,3,4-oxadiazoles (3a-d) and thiadiazoles (5a-d), respectively...
  74. ncbi Nitric oxide-mediated nonadrenergic noncholinergic relaxation of piglet pulmonary arteries decreases with postnatal age
    G Gonzáles-Luis
    Department of Pediatrics, University Hospital Maastricht, Research Institute Growth and Development GROW, Maastricht, The Netherlands
    J Physiol Pharmacol 58:45-56. 2007
    ..In conclusion, NANC relaxation is present in neonatal pulmonary and mesenteric arteries and it is, at least partially, mediated through NO. NANC relaxation of porcine pulmonary and mesenteric arteries decreases with postnatal maturation...
  75. ncbi Keto-1,3,4-oxadiazoles as cathepsin K inhibitors
    James T Palmer
    Celera Genomics, Inc, 180 Kimball Way, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 16:2909-14. 2006
    ..This series thus represents a promising chemotype that could be used in diseases implicated by imbalances in cathepsin K activity such as osteoporosis...
  76. ncbi Design and synthesis of new 2-substituted-5-(2-benzylthiophenyl)-1,3,4-oxadiazoles as benzodiazepine receptor agonists
    Afshin Zarghi
    Department of Medicinal Chemistry, Faculty of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran 14155 6153, Iran
    Bioorg Med Chem Lett 15:3126-9. 2005
    A series of new 2-substituted-5-(2-benzylthiophenyl)-1,3,4-oxadiazoles was designed and synthesized as anticonvulsant agents...
  77. ncbi Aroylpropionic acid based 2,5-disubstituted-1,3,4-oxadiazoles: synthesis and their anti-inflammatory and analgesic activities
    Mymoona Akhter
    Faculty of Pharmacy, Jamia Hamdard University, Department of Pharmaceutical Chemistry, Hamdard Nagar, New Delhi 110062, India
    Eur J Med Chem 44:2372-8. 2009
    ..The study showed that the cyclization of carboxylic group of aroylpropionic acids into an oxadiazole nucleus resulted in compounds having good anti-inflammatory and analgesic effects with reduced gastric irritation...
  78. ncbi Synthesis and anticonvulsant activity of new 2-substituted-5- [2-(2-fluorophenoxy)phenyl]-1,3,4-oxadiazoles and 1,2,4-triazoles
    Ali Almasirad
    Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
    Bioorg Med Chem Lett 14:6057-9. 2004
    A series of new 2-substituted-5-[2-(2-fluorophenoxy)phenyl]-1,3,4-oxadiazoles has been synthesized and screened for their anticonvulsant activities. Compound 3 shows considerable anticonvulsant activity both in PTZ and MES models...
  79. ncbi Design and synthesis of new 2-substituted-5-[2-(2-halobenzyloxy)phenyl]-1,3,4-oxadiazoles as anticonvulsant agents
    Afshin Zarghi
    Department of Medicinal Chemistry, Shaheed Beheshti University of Medical Sciences, Tehran, Iran
    Chem Pharm Bull (Tokyo) 56:509-12. 2008
    A new series of 2-substituted-5-[2-(2-halobenzyloxy)phenyl]-1,3,4-oxadiazoles was designed and synthesized as anticonvulsant agents...
  80. ncbi 2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase)
    Joseph S Warmus
    Department of Chemistry, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 18:6171-4. 2008
    ..This compound suffered from less than ideal solubility and metabolic stability. An oxadiazole moiety behaves as a bioisostere for the hydroxamate group, leading to a more metabolically stable and efficacious MEK inhibitor...
  81. ncbi Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity
    Harish Rajak
    Medicinal Chemistry Research Laboratory, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur 495 009, CG, India
    Bioorg Med Chem Lett 20:4168-72. 2010
    ..The results of the present studying validated that the pharmacophoric model with four binding sites is essential for anticonvulsant activity...
  82. ncbi Hypervalent iodine(III) mediated synthesis of novel unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles as antibacterial and antifungal agents
    Om Prakash
    Department of Chemistry, Kurukshetra University, Kurukshetra 136 119, Haryana, India
    Eur J Med Chem 45:4252-7. 2010
    A series of novel 2,5-disubstituted 1,3,4-oxadiazoles 4 have been conveniently synthesized by oxidative cyclization of pyrazolylaldehyde N-acylhydrazones 3 promoted by iodobenzene diacetate under mild conditions (11 examples, up to 92% ..
  83. ncbi Synthesis of 3-aryl-5-decapentyl-1,2,4-oxadiazoles possessing antiinflammatory and antitumor properties
    Natércia M Miranda Bezerra
    Departamento de Quimica Fundamental, Centro de Ciencias Exatas e de Natureza, Universidade Federal de Pernambuco, CEP 50740 540 Recife, PE, Brazil
    Farmaco 60:955-60. 2005
    A simple, convenient and straightforward synthesis of 3-aryl-1,2,4-oxadiazoles 4a-f from arylamidoximes 1a-f and palmitic acid 2 is described. Compounds 4a-f are non-lethal in mice at four times the therapeutic dose (i.p...
  84. ncbi Vascular reactivity in intrapulmonary arteries of chicken embryos during transition to ex ovo life
    Eduardo Villamor
    Department of Pediatrics, University Hospital Maastricht, Research Institute Growth and Development, University of Maastricht, 6202 AZ Maastricht, The Netherlands
    Am J Physiol Regul Integr Comp Physiol 282:R917-27. 2002
    ..Chicken embryo pulmonary arteries show a marked endothelium-dependent relaxation that is unaffected by transition to ex ovo life. Endothelium-derived NO seems to be the main mediator responsible for this relaxation...
  85. ncbi Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors
    Robert M Rydzewski
    Department of Medicinal Chemistry, 180 Kimball Way, South San Francisco, California 94080, USA
    J Med Chem 49:2953-68. 2006
    ..The resulting optimized P4-P3-P2 sequence was grafted onto a novel proteasome inhibitor warhead, 2-keto-1,3,4-oxadiazoles (KOD), to produce reversible, subnanomolar proteasome inhibitors that were 1000-fold selective versus cathepsin ..
  86. pmc GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt
    Deborah A Altomare
    Women s Cancer, Fox Chase Cancer Center, Philadelphia, Pennsylvania 19111, USA
    Clin Cancer Res 16:486-96. 2010
    ..The broad long-term objective of this project was to use preclinical cancer models with precisely defined genetic lesions to elucidate the efficacy of targeting Akt with GSK690693...
  87. ncbi The toxic and anti-feedant activity of 2H-pyridazin-3-one-substituted 1,3,4-oxadiazoles against the armyworm Pseudaletia separata (Walker) and other insects and mites
    Qingchun Huang
    Institute of Pesticides and Pharmaceuticals, East China University of Science and Technology, Shanghai, 200237, China
    Pest Manag Sci 59:933-9. 2003
    The toxicities and anti-feedant activities of thirteen asymmetrical 1,3,4-oxadiazoles containing a 2H-pyridazin-3-one group were investigated...
  88. pmc Differential efficacy of caspase inhibitors on apoptosis markers during sepsis in rats and implication for fractional inhibition requirements for therapeutics
    Nathalie Methot
    Merck Frosst Centre for Therapeutic Research, Merck Research Laboratories, Montreal, Quebec, Canada H9H 3L1
    J Exp Med 199:199-207. 2004
    ..Furthermore, this requirement presents substantial therapeutic challenges owing to the need for persistent and complete caspase blockade...
  89. ncbi NO scavenging by 3-hydroxyanthranilic acid and 3-hydroxykynurenine: N-nitrosation leads via oxadiazoles to o-quinone diazides
    Claudia Backhaus
    Johann Friedrich Blumenbach Institute of Zoology and Anthropology, University of Goettingen, Berliner Strasse 28, D 37073 Goettingen, Lower Saxony, Germany
    Nitric Oxide 19:237-44. 2008
    ..ion formation from diazonium ions of non-hydroxylated anilines, nitrogen is practically not released from oxadiazoles/quinone diazides at moderate temperatures...
  90. ncbi Synthesis of some new 2-(6-methoxy-2-naphthyl)- 5-aryl-1,3,4-oxadiazoles as possible non-steroidal anti-inflammatory and analgesic agents
    Badiadka Narayana
    Department of Post Graduate Studies and Research in Chemistry, Mangalore University, Mangalagangotri, India
    Arch Pharm (Weinheim) 338:373-7. 2005
    The synthesis of some new 2-(6-methoxy-2-naphthyl)-5-aryl-1,3,4-oxadiazoles (4a-k) has been described. Ethyl-6-methoxy-2-naphthoate (1) yielded on treatment with hydrazine hydrate to 6-methoxy-2-naphthoic acid hydrazide (2)...
  91. ncbi Synthesis and antimicrobial studies of a new series of 2-[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]-5-substituted-1,3,4-oxadiazoles
    S L Gaonkar
    Department of Studies in Chemistry, University of Mysore, Manasagangotri, India
    Eur J Med Chem 41:841-6. 2006
    A series of novel 2-[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]-5-substituted-1,3,4-oxadiazoles were synthesized by the oxidative cyclisation of hydrazones derived from 4-[2-(5-ethylpyridin-2-yl)ethoxy]benzaldehyde and aroylhydrazines ..
  92. ncbi Synthesis and anticonvulsant activity of new 2-substituted-5-(2-benzyloxyphenyl)-1,3,4-oxadiazoles
    Afshin Zarghi
    Department of Medicinal Chemistry, Faculty of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran 141556153, Iran
    Bioorg Med Chem Lett 15:1863-5. 2005
    A series of new 2-substituted-5-(2-benzyloxyphenyl)-1,3,4-oxadiazoles have been synthesized and evaluated as anticonvulsant agents. Compound 4b shows considerable anticonvulsant activity both in PTZ and MES models...
  93. ncbi Syntheses, antifeedant activity, and QSAR analysis of new oxa(thia)diazolyl 3(2H)-pyridazinones
    Song Cao
    Institute of Pesticides and Pharmaceuticals, East China University of Science and Technology, P O Box 544, 130 Meilong Road, Shanghai 200237, China
    J Agric Food Chem 53:3120-5. 2005
    ..The results showed that dipole moment, molar refractivity, and log P are identified as critical parameters for chronic growth effects...
  94. ncbi Synthesis, antimicrobial, and anti-HIV-1 activity of certain 5-(1-adamantyl)-2-substituted thio-1,3,4-oxadiazoles and 5-(1-adamantyl)-3-substituted aminomethyl-1,3,4-oxadiazoline-2-thiones
    Ali A El-Emam
    Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
    Bioorg Med Chem 12:5107-13. 2004
    ..ethanolic potassium hydroxide yielded the corresponding 5-(1-adamantyl)-2-ethyl or substituted ethylthio-1,3,4-oxadiazoles 3a-c...
  95. ncbi Synthesis and antifeedant activity of new oxadiazolyl 3(2H)-pyridazinones
    Song Cao
    Institute of Pesticides and Pharmaceuticals, East China University of Science and Technology, P O Box 544, 130 Meilong Road, Shanghai 200237, P R China
    J Agric Food Chem 51:152-5. 2003
    ..The compounds exhibited significant levels of activity. The feeding deterrency values of IIIa,j were 57% and 51% at 500 mg/kg concentration, respectively...
  96. ncbi Synthesis of Schiff bases of 2-amino-5-aryl-1,3,4-oxadiazoles and their evaluation for antimicrobial activities
    Pradeep Mishra
    Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar, India
    J Gen Appl Microbiol 51:133-41. 2005
    Twenty Schiff bases of 2-amino-5-aryl-1,3,4-oxadiazoles have been synthesized with different aromatic aldehydes. The structures of the compounds were confirmed by nitrogen analysis, IR and 13C-NMR spectral data...
  97. ncbi Synthesis and biological evaluation of 3,4-diphenyl-1,2,5-oxadiazole-2-oxides and 3,4-diphenyl-1,2,5-oxadiazoles as potential hybrid COX-2 inhibitor/nitric oxide donor agents
    Carlos Velazquez
    Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada T6G 2N8
    Bioorg Med Chem 13:2749-57. 2005
    ..3,4-diphenyl-1,2,5-oxadiazole-2-oxides (3,4-diphenylfuroxans) and the corresponding N-desoxy 3,4-diphenyl-1,2,5-oxadiazoles (3,4-diphenylfurazans) analogs, were synthesized for in vitro evaluation as hybrid cyclooxygenase (COX) ..
  98. ncbi Synthesis of novel 5-aryl-2-thio-1,3,4-oxadiazoles and the study of their structure-anti-mycobacterial activities
    Fliur Macaev
    Institute of Chemistry, Academy of Sciences of Moldova, Chisinau, MD 2028, Republic of Moldova
    Bioorg Med Chem 13:4842-50. 2005
    The preparation of novel 5-aryl-2-thio-1,3,4-oxadiazoles 4a-41 and the computer-aided study of their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) are reported...
  99. pmc Nitric oxide preferentially induces type 1 T cell differentiation by selectively up-regulating IL-12 receptor beta 2 expression via cGMP
    Wanda Niedbala
    Department of Immunology and Bacteriology, University of Glasgow, Glasgow G11 6NT, United Kingdom
    Proc Natl Acad Sci U S A 99:16186-91. 2002
    ..Our results also provide an example of the regulation of cytokine receptor expression by NO. The selectivity of such action via cGMP suggests that it is amenable to therapeutic intervention...
  100. pmc Inhibition of rat platelet aggregation by the diazeniumdiolate nitric oxide donor MAHMA NONOate
    Kerry L Homer
    Department of Physiology and Pharmacology, The University of Queensland, Brisbane, Queensland 4072, Australia k homer
    Br J Pharmacol 137:1071-81. 2002
    ..7. Thus inhibition of rat platelet aggregation by MAHMA NONOate (like GSNO) is largely ODQ-resistant and, by implication, independent of soluble guanylate cyclase. A likely mechanism of inhibition is activation of SERCA...
  101. pmc Role of the NO/cGMP/K(ATP) pathway in the protective effects of sildenafil against ethanol-induced gastric damage in rats
    J V R Medeiros
    Department of Physiology and Pharmacology, Federal University of Ceara, Fortaleza, Ceara, Brazil
    Br J Pharmacol 153:721-7. 2008
    ..Activation of ATP-sensitive potassium channels (K(ATP)) is involved in gastric defence. Our objective was to evaluate the role of the NO/cGMP/K(ATP) pathway in the protective effects of sildenafil against ethanol-induced gastric damage...

Research Grants55

  1. Defining target specificity of oxadiazole 2-oxides in Ancylostoma ceylanicum
    Jon J Vermeire; Fiscal Year: 2012
    ..ceylanicum. Recent work has identified oxadiazoles as lead compounds targeting the trematode multifunctional redox protein, thioredoxin glutathione reductase (TGR)..
  2. Vindoline and Vinblastine
    Dale L Boger; Fiscal Year: 2013
    ..vinblastine are detailed based on the implementation of a tandem [4+2]/[3+2] cycloaddition cascade of 1,3,4-oxadiazoles, and a recently developed single step Fe(III)-promoted biomimetic coupling and subsequent oxidation reaction of ..
  3. ANTITUMOR ANTIBIOTICS
    Dale L Boger; Fiscal Year: 2013
    ..generated p-delocalized singlet vinylcarbenes, and (4) tandem Diels- Alder/1,3-dipolar cycloadditions of 1,3,4-oxadiazoles will be pursued and provide the opportunity to comprehensively extend past studies...
  4. RNAi-medicated inhibition of BDNF expression and alcohol-drinking behavior
    QINGSHAN YAN; Fiscal Year: 2008
    ..abstract_text> ..
  5. ALCOHOL AND MESOLIMBIC DOPAMINE PATHWAY
    QINGSHAN YAN; Fiscal Year: 2002
    ..This will elucidate the relative contribution of 5-HT2 receptors to the regulation of ethanol-induced DA release and help to explain the effects of 5-HT2 antagonists on alcohol consumption reported in the literature. ..
  6. Sphingosine-1-phosphate-activated telomerase in stroke
    Christian Waeber; Fiscal Year: 2006
    ..This project will study a novel system that can provide long-lasting improvement in EC function following stroke and serve as a new target for stroke therapy. ..
  7. Endocannabinoids and cue-induced drug-seeking behavior
    Loren Parsons; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  8. COMPLEX INVOLVED IN MRNA DECAY IN YEAST
    STUART PELTZ; Fiscal Year: 2006
    ..The goal is to amass a set of AU-rich elements large enough to facilitate computer analysis of the sequences to identify commonalities between them that might specify the proteins they interact with and their regulation. ..
  9. Afferent modulation in bladde dysfunction
    Naoki Yoshimura; Fiscal Year: 2007
    ..abstract not provided ..
  10. Regulation of heme uptake in intestinal epithelial cells
    Aliye Uc; Fiscal Year: 2007
    ..heme uptake pathways will have a great impact in understanding disorders associated with iron overload (hereditary hemochromatosis, iron overload secondary to blood transfusions) and nutritional iron deficiency [unreadable] [unreadable]..
  11. Mast Cells: Role in the Pathophysiology of Headache
    Dan Levy; Fiscal Year: 2007
    ..Results may help identify pharmacological targets that could lead to the development of novel analgesic drugs for the treatment of headaches and possibly other intractable pain syndromes. [unreadable] [unreadable] [unreadable]..
  12. MOLECULAR MECHANISMS OF LUNG SURFACTANT SECRETION
    Lin Liu; Fiscal Year: 2007
    ..Accomplishing the goals of this proposal will give a valuable direction to the therapy of pulmonary diseases such as neonatal respiratory distress syndrome. ..
  13. MECHANISMS OF NO-MEDIATED PROTEIN S-NITROSYLATION IN EAE
    OSCAR BIZZOZERO; Fiscal Year: 2007
    ..abstract_text> ..
  14. Regulation of Heme Uptake and Transport in Caco-2 Cells
    Aliye Uc; Fiscal Year: 2007
    ..g. hereditary hemochromatosis, iron overload secondary to blood transfusions) and explore the role of intestinal epithelial cell bi-directional heme movement on the regulation of iron stores. ..
  15. Neurophysiology and Biomechanics of Urethra in Stress Urinary Incontinence
    Naoki Yoshimura; Fiscal Year: 2008
    ..This is recognized as a high priority in the urologic/gynecologic care of SUI patients. [unreadable] [unreadable]..
  16. CB1 Modulation of Opioid Peptides and Ethanol Intake
    Loren Parsons; Fiscal Year: 2008
    ..abstract_text> ..
  17. AFFERENT PLASTICITY UNDERLYING URETHRAL AND PELVIC PAIN
    Naoki Yoshimura; Fiscal Year: 2010
    ..This is recognized as a high priority in the urologic care of patients with IC/CPPS. ..
  18. REACTIVE OXYGEN SPECIES AND VASCULAR O2 SENSING
    Michael S Wolin; Fiscal Year: 2010
    ..These studies should help define the origins of differences in physiological responses of pulmonary and coronary arteries to changes in O2 tension. ..
  19. NEW APPROACH TO ENDOTHELIAL CLEFT STRUCTURE
    Fitz Roy E Curry; Fiscal Year: 2010
    ..Our experiments evaluate the common mechanical properties of the endothelial glycocalyx that modulate water, solute, leukocyte, and red cell fluxes at the endothelial cell surface. ..
  20. Computational Approach to Ligand Discovery for LPA GPCR and PPAR
    Abby L Parrill; Fiscal Year: 2010
    ..This research can therefore lead to new treatments for cardiovascular disease and cancer. ..
  21. Neuron-Dervied S1P and Endothelial Function in Stroke
    Christian Waeber; Fiscal Year: 2010
    ..This project will study a novel system that can provide long-lasting improvement in EC function following stroke and serve as a target for stroke therapy. ..
  22. Characterization of Pancreatic Disease in a Novel Porcine Cystic Fibrosis Model
    Aliye Uc; Fiscal Year: 2010
    ..The goal of this application is to fully characterize pancreatic involvement in our novel CF pig model and to better understand the pathophysiological mechanisms leading to PI in CF. ..
  23. Mechanisms of Alveolar Epithelial Cell Differentiation
    Lin Liu; Fiscal Year: 2006
    ..abstract_text> ..
  24. HIV FRAMESHIFTING--FROM BIOLOGY TO THERAPEUTICS
    STUART PELTZ; Fiscal Year: 2003
    ..Their long-term goal will be to develop compounds that affect frame-shifting to the point that proof of principle has been established and antiviral agents targeting this process will be subsequently developed for clinical use. ..
  25. Lower urinary tract dysfunction in Parkinson's disease
    Naoki Yoshimura; Fiscal Year: 2003
    ..This is a high priority in the urologic care of patients with Parkinson's disease. ..
  26. Sphingosine 1 Phosphate and Embolic Stroke
    Christian Waeber; Fiscal Year: 2003
    ..Together, these studies will explore the significance of a novel system, which appear to be cerebro-selective, and potentially a useful therapeutic target for stroke therapy. ..
  27. KIDNEY SPECIFIC GENE TRANSFER IN HYPERTENSION
    Theodore Kurtz; Fiscal Year: 2003
    ..Under this alternative hypothesis, the results of the cDNA microarray analysis will be used to identify potential downstream target genes whose expression is altered by the primary genetic defect on chromosome 1. ..
  28. Regulation of Vascular Tone During Cirrhosis
    ETHAN CARTER; Fiscal Year: 2003
    ..This project will not only define the cellular basis for hepatopulmonary syndrome, but will also contribute to our understanding of how pulmonary vascular tone is controlled at the most basic level. ..
  29. WHY DO METABOLIC RISK FACTORS CLUSTER WITH HYPERTENSION?
    Theodore Kurtz; Fiscal Year: 2003
    ....
  30. G PROTEINS AND PAROTID SECRETORY GRANULE
    EILEEN WATSON; Fiscal Year: 2002
    ..These studies will also provide a framework for examining cellular biochemical defects in diseases relating to salivary dysfunction. ..
  31. Regulation of Pulmonary Vascular Tone During Cirrhosis
    CHRYSTELLE GARAT CARTER; Fiscal Year: 2004
    ..This project will not only define the cellular basis for hepatopulmonary syndrome, but will also contribute to our understanding of how pulmonary vascular tone is controlled at the most basic level. ..
  32. IMPROVEMENT OF MEMBRANE BIOLOGY FACILITY
    FITZ ROY CURRY; Fiscal Year: 2002
    ..That project addressed other laboratory and basic infrastructure deficiencies in the same building that contains the subject laboratories in the current application. ..
  33. Bladder Pain Gene Therapy with Pro-opiomelanocortin cDNA
    Naoki Yoshimura; Fiscal Year: 2004
    ..This research project is important to provide a solid basis for potential future clinical application. ..
  34. COCAINE REWARD AND 5 HT 1B RECEPTORS--NEURAL MECHANISMS
    Loren Parsons; Fiscal Year: 2002
    ....
  35. OPIOID INDUCED REM SLEEP INHIBITION
    Ralph Lydic; Fiscal Year: 2005
    ..The potential health relatedness of these basic studies derives from the unwanted side effects of opioids on sleep and breathing. ..
  36. Genetic Modifiers of Cystic Fibrosis
    Michael Boyle; Fiscal Year: 2007
    ..Last, we will evaluate three of the strongest current CF candidate modifier genes to determine if the distribution of their functional alleles segregates with severity of lung disease in our CF clinic population. ..
  37. SALIVARY SECRETION-ROLE OF CALCIUM
    EILEEN WATSON; Fiscal Year: 2005
    ..Mechanisms/pathways involved in AA/metabolite-mediated cAMP signaling will be assessed by correlating MAPK activation with cAMP synthesis and degradation. ..
  38. MMI SL microCut Laser Microdissection System
    Christian Waeber; Fiscal Year: 2005
    ..We believe that the integration of an LCM core within the workflow of the Neuroscience Center's researchers will markedly improve our understanding of processes and diseases affecting discrete cell populations of the nervous system. ..
  39. CHIMERIC RNA/DNA OLIGONUCLEOTIDE BASED GENE THERAPY
    YEONG HAU LIEN; Fiscal Year: 2003
    ..This preclinical study will provide critical information for future development of optimal gene targeting therapy for treating hereditary renal diseases, such as autosomal dominant polycystic kidney disease. ..
  40. NONSENSE MEDIATED MRNA DECAY PATHWAY
    STUART PELTZ; Fiscal Year: 2005
    ..The goals of the experiments in this grant proposal are to investigate the sequences and factors involved in the NMD pathway in order to dissect its mechanism and how it is regulated. ..
  41. Therapeutic effect of boswellin in prostate cancer
    Yongkui Jing; Fiscal Year: 2005
    ..We hope our proposal will lead to the discovery of a novel complementary agent for prostate cancer treatment. ..
  42. NITRIC OXIDE, PLP ACYLATION & THE PATHOPHYSIOLOGY OF MS
    OSCAR BIZZOZERO; Fiscal Year: 2003
    ..abstract_text> ..
  43. PULMONARY VASODILATION AND GUANYLATE CYCLASE REGULATION
    Michael S Wolin; Fiscal Year: 2010
    ....
  44. CHOLINERGIC MECHANISMS OF BREATHING DURING SLEEP
    Ralph Lydic; Fiscal Year: 2010
    ..Aim 4 will use pontine and systemic drug administration to test the hypothesis that pontine cholinergic mechanisms modulate the ability of adenosine AI receptors to alter arousal and breathing. ..
  45. MATURATION OF CEREBROVASCULAR RELAXANT MECHANISMS
    William Pearce; Fiscal Year: 2009
    ..This approach should also identify which cGMP-dependent mechanisms may be most amenable to therapeutic pharmacological manipulation in the critically ill neonate. ..
  46. MATURATION OF CEREBROVASCULAR CONTRACTILE MECHANISMS
    William Pearce; Fiscal Year: 2005
    ..abstract_text> ..
  47. Brain serotonin and angiotensin II systems in migraine
    JOSE TERRON; Fiscal Year: 2007
    ..5-HT content will be measured by HPLC in brain homogenates. ..
  48. 5-HTIB RECEPTORS AND MECHANISMS OF ETHANOL REINFORCEMENT
    Loren Parsons; Fiscal Year: 2005
    ..abstract_text> ..
  49. Basic mechanisms of antidepressant augmentation
    Michael Newman; Fiscal Year: 2003
    ..These experiments will permit a comprehensive assessment of the role of serotonergic mechanisms in AD augmentation by T3 and an empirical basis for its use in the treatment of depression. ..
  50. Mechanisms of Alveolar Fluid Transport
    Lin Liu; Fiscal Year: 2009
    ..An understanding of the mechanisms of fluid transport in the lung will provide valuable insights and directions toward therapeutic intervention in fetal lung diseases and the resolution of pulmonary edema. ..
  51. PURINERGIC AXIS OF CARDIAC BLOOD VESSELS
    IAIN BUXTON; Fiscal Year: 2001
    ..We will approach these aims with biochemical, pharmacological, molecular, cell biological and microscopic methods employing intact blood vessels, cells in primary culture and subcellular fractions. ..
  52. Brain Cannabinoid Signaling: Selectivity and Adaptation
    Laura J Sim Selley; Fiscal Year: 2010
    ..This project will determine roles of specific signaling proteins in the effects of acute and long-term CB1R activation by THC and are relevant to cannabinoid therapeutics and drug abuse. ..
  53. Brainstem Mechanisms of Craniofacial Muscle Pain
    JIN RO; Fiscal Year: 2006
    ..abstract_text> ..
  54. CONFOCAL MICROSCOPE
    Mark Ackermann; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  55. Preterm birth, lung innate immunity, and RSV
    Mark Ackermann; Fiscal Year: 2009
    ..The work is significant because it discovers the underlying basis for RSV susceptibility preterm and mechanistic approaches to enhance innate immunity. ..