benzamidines

Summary

Summary: Amidines substituted with a benzene group. Benzamidine and its derivatives are known as peptidase inhibitors.

Top Publications

  1. ncbi Laser in situ keratomileusis treatment for myopia after Acanthamoeba keratitis
    Li Lim
    Corneal Service, Singapore National Eye Centre, Singapore
    Eye Contact Lens 30:103-4. 2004
  2. ncbi Mutation of surface residues to promote crystallization of activated factor XI as a complex with benzamidine: an essential step for the iterative structure-based design of factor XI inhibitors
    Lei Jin
    Daiichi Asubio Medical Research Laboratories LLC, USA
    Acta Crystallogr D Biol Crystallogr 61:1418-25. 2005
  3. pmc New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289
    Tanja Wenzler
    Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Basel, Switzerland
    Antimicrob Agents Chemother 53:4185-92. 2009
  4. ncbi Synthesis and antiprotozoal activity of aza-analogues of furamidine
    Mohamed A Ismail
    Department of Chemistry, Georgia State University, Atlanta, Georgia 30303 3083, USA
    J Med Chem 46:4761-9. 2003
  5. pmc Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration
    R E Mdachi
    Kenya Agricultural Research Institute Trypanosomiasis Research Centre, Kikuyu, Kenya
    Antimicrob Agents Chemother 53:953-7. 2009
  6. ncbi Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase
    I J Enyedy
    Structural Biology and Cancer Drug Discovery Program, Lombardi Cancer Center, and Department of Oncology, Georgetown University Medical Center, 3900 Reservoir Road, Washington DC 20007, USA
    J Med Chem 44:1349-55. 2001
  7. ncbi Pharmacokinetics and metabolism of the prodrug DB289 (2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) in rat and monkey and its conversion to the antiprotozoal/antifungal drug DB75 (2,5-bis(4-guanylphenyl)furan dihydrochloride)
    Ian Midgley
    Department of Drug Metabolism, Huntingdon Life Sciences Ltd, Alconbury, Huntingdon, Cambridgeshire, PE28 4HS, UK
    Drug Metab Dispos 35:955-67. 2007
  8. pmc CYP4F enzymes are the major enzymes in human liver microsomes that catalyze the O-demethylation of the antiparasitic prodrug DB289 [2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime]
    Michael Zhuo Wang
    Division of Molecular Pharmaceutics, School of Pharmacy, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
    Drug Metab Dispos 34:1985-94. 2006
  9. ncbi In vitro metabolism of an orally active O-methyl amidoxime prodrug for the treatment of CNS trypanosomiasis
    J H Ansede
    Division of Drug Delivery and Disposition, School of Pharmacy, The University of North Carolina, Chapel Hill, NC 27599, USA
    Xenobiotica 35:211-26. 2005
  10. ncbi Direct synthesis of quinazolines through copper-catalyzed reaction of aniline-derived benzamidines
    Yusuke Ohta
    Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo ku, Kyoto 606 8501, Japan
    Org Lett 12:3963-5. 2010

Research Grants

  1. FOCUSED PARALLEL SYNTHESIS OF DICATION ANTIFUNGAL AGENTS
    Richard Tidwell; Fiscal Year: 2003
  2. Ophthalmic Antibiotic Resistance Study
    Kirk Wilhelmus; Fiscal Year: 2003
  3. TRANSMISSION OF PNEUMOCYSTIS INFECTION
    Melanie Cushion; Fiscal Year: 2001
  4. LACTATIONAL EFFECTORS OF TRIACYLGLYCEROL MOBILIZATION
    JAMES MCMANAMAN; Fiscal Year: 2008
  5. Simple, Selective Antimitotic Antiparasitic Agents
    Karl Werbovetz; Fiscal Year: 2007
  6. New Approaches for Development of PcP Therapy
    Melanie Cushion; Fiscal Year: 2006
  7. PNEUMOCYSTIS GENOME PROJECT
    Melanie Cushion; Fiscal Year: 2004
  8. ENDOGENOUS NITROSATION CHEMISTRY IN CARCINOGENESIS
    RICHARD LOEPPKY; Fiscal Year: 2004
  9. Eighth International Workshops on Opportunistic Protists
    Melanie Cushion; Fiscal Year: 2003
  10. MECHANISMS OF HORMONE THERAPY IN POSTMENOPAUSAL WOMEN
    L Newby; Fiscal Year: 2003

Detail Information

Publications162 found, 100 shown here

  1. ncbi Laser in situ keratomileusis treatment for myopia after Acanthamoeba keratitis
    Li Lim
    Corneal Service, Singapore National Eye Centre, Singapore
    Eye Contact Lens 30:103-4. 2004
    ..We report a case of a patient with a history of Acanthamoeba keratitis in the right eye who was successfully treated with Laser in situ keratomileusis (LASIK) for myopia correction...
  2. ncbi Mutation of surface residues to promote crystallization of activated factor XI as a complex with benzamidine: an essential step for the iterative structure-based design of factor XI inhibitors
    Lei Jin
    Daiichi Asubio Medical Research Laboratories LLC, USA
    Acta Crystallogr D Biol Crystallogr 61:1418-25. 2005
    ..The benzamidine in the preformed crystals was easily exchanged with other FXIa small-molecule inhibitors. These crystals have facilitated the structure-based design of small-molecule FXIa inhibitors...
  3. pmc New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289
    Tanja Wenzler
    Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Basel, Switzerland
    Antimicrob Agents Chemother 53:4185-92. 2009
    ..In conclusion, DB868 with oral and DB829 with parenteral application are potential candidates for further development of a second-stage African sleeping sickness drug...
  4. ncbi Synthesis and antiprotozoal activity of aza-analogues of furamidine
    Mohamed A Ismail
    Department of Chemistry, Georgia State University, Atlanta, Georgia 30303 3083, USA
    J Med Chem 46:4761-9. 2003
    ..of less than 10 nM. Against P. f. 8a, 8b, and 14b exhibited IC(50) values less than 10 nM. In an in vivo mouse model for T. b. r. four compounds 6a, 6c, 6d, and 8a were curative. Compound 6a produced cures at an oral dosage of 5 mg/kg...
  5. pmc Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration
    R E Mdachi
    Kenya Agricultural Research Institute Trypanosomiasis Research Centre, Kikuyu, Kenya
    Antimicrob Agents Chemother 53:953-7. 2009
    ..This study has shown that oral diamidines have potential for the treatment of early-stage sleeping sickness...
  6. ncbi Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase
    I J Enyedy
    Structural Biology and Cancer Drug Discovery Program, Lombardi Cancer Center, and Department of Oncology, Georgetown University Medical Center, 3900 Reservoir Road, Washington DC 20007, USA
    J Med Chem 44:1349-55. 2001
    ..We report herein the structure-based approach for the discovery of bis-benzamidines as a novel class of potent matriptase inhibitors...
  7. ncbi Pharmacokinetics and metabolism of the prodrug DB289 (2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) in rat and monkey and its conversion to the antiprotozoal/antifungal drug DB75 (2,5-bis(4-guanylphenyl)furan dihydrochloride)
    Ian Midgley
    Department of Drug Metabolism, Huntingdon Life Sciences Ltd, Alconbury, Huntingdon, Cambridgeshire, PE28 4HS, UK
    Drug Metab Dispos 35:955-67. 2007
    ..It was estimated that almost half of an oral dose of DB289 to rats and about one-third of that to monkeys was metabolized to DB75...
  8. pmc CYP4F enzymes are the major enzymes in human liver microsomes that catalyze the O-demethylation of the antiparasitic prodrug DB289 [2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime]
    Michael Zhuo Wang
    Division of Molecular Pharmaceutics, School of Pharmacy, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
    Drug Metab Dispos 34:1985-94. 2006
    ..g., CYP4F2, CYP4F3B) are the major enzymes responsible for M1 formation by HLMs. These findings indicate that, in human liver, members of the CYP4F subfamily biotransform not only endogenous compounds but also xenobiotics...
  9. ncbi In vitro metabolism of an orally active O-methyl amidoxime prodrug for the treatment of CNS trypanosomiasis
    J H Ansede
    Division of Drug Delivery and Disposition, School of Pharmacy, The University of North Carolina, Chapel Hill, NC 27599, USA
    Xenobiotica 35:211-26. 2005
    ..The active antitrypanosomal metabolite, DB820, was the last metabolite to be formed and thus provides evidence that DB844 may effectively be metabolized to its active metabolite in vivo...
  10. ncbi Direct synthesis of quinazolines through copper-catalyzed reaction of aniline-derived benzamidines
    Yusuke Ohta
    Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo ku, Kyoto 606 8501, Japan
    Org Lett 12:3963-5. 2010
    ....
  11. pmc DB75, a novel trypanocidal agent, disrupts mitochondrial function in Saccharomyces cerevisiae
    Charlotte A Lanteri
    Department of Pathology and Laboratory Medicine, Room 805, Brinkhous Bullitt Building, University of North Carolina, Chapel Hill, NC 27599 7525, USA
    Antimicrob Agents Chemother 48:3968-74. 2004
    ..We conclude that the mitochondrion is a cellular target of DB75 in yeast cells and anticipate that the results of this study will aid in the target-based design of new antimicrobial aromatic diamidines...
  12. ncbi Unusual dehydroxylation of antimicrobial amidoxime prodrugs by cytochrome b5 and NADH cytochrome b5 reductase
    Janelle Y Saulter
    School of Pharmacy, University of North Carolina at Chapel Hill, USA
    Drug Metab Dispos 33:1886-93. 2005
    ..These results indicate that cytochrome b5 and b5 reductase play a direct role in metabolic activation of DB289 to furamidine...
  13. ncbi Pafuramidine for Pneumocystis jiroveci pneumonia in HIV-infected individuals
    Donald Chen
    New York University, Department of Medicine, Division of Infectious Disease, AIDS Clinical Trials Unit, Bellevue C and D Building, Room 558, 550 First Avenue, New York, NY 10016 6481, USA
    Expert Rev Anti Infect Ther 5:921-8. 2007
    ..To date, human trials suggest that pafuramidine is well tolerated overall and has clinical activity against Pneumocystis pneumonia. In this article, we review the available data for the use of pafuramidine in Pneumocystis pneumonia...
  14. ncbi Diamidines as antitrypanosomal, antileishmanial and antimalarial agents
    Karl Werbovetz
    The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus 43210 1291, USA
    Curr Opin Investig Drugs 7:147-57. 2006
    ....
  15. pmc Phase I/II evaluation of the prophylactic antimalarial activity of pafuramidine in healthy volunteers challenged with Plasmodium falciparum sporozoites
    Myaing M Nyunt
    Department of Medicine, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
    Am J Trop Med Hyg 80:528-35. 2009
    ..We conclude that a single dose of 100 mg pafuramidine does not adequately protect non-immune individuals against P. falciparum and shows no clinically or statistically significant evidence of causal prophylactic activity...
  16. ncbi Roles for the Trypanosoma brucei P2 transporter in DB75 uptake and resistance
    Charlotte A Lanteri
    Division of Infection and Immunity, Institute of Biomedical and Life Sciences, The Glasgow Biomedical Research Centre, University of Glasgow, Glasgow G12 8QQ, United Kingdom
    Mol Pharmacol 70:1585-92. 2006
    ....
  17. ncbi Phenyl substitution of furamidine markedly potentiates its anti-parasitic activity against Trypanosoma cruzi and Leishmania amazonensis
    E M De Souza
    Lab Biologia Celular, Instituto Oswaldo Cruz, Avenida Brasil 4365, Manguinhos, 21045 900 Rio de Janeiro, RJ, Brazil
    Biochem Pharmacol 68:593-600. 2004
    ..Altogether, the data suggest that the phenyl-substituted furamidine analogue DB569 is a potential new candidate for the treatment of the Chagas' disease and Leishmaniasis...
  18. ncbi Efficacy of the diamidine DB75 and its prodrug DB289, against murine models of human African trypanosomiasis
    J K Thuita
    Trypanosomiasis Research Centre, Kenya Agricultural Research Institute TRC KARI, P O Box 362, Kikuyu, Kenya
    Acta Trop 108:6-10. 2008
    ..This shows that the prodrug strategy was successful in terms of reducing toxicity and increasing efficacy and oral bioavailability...
  19. ncbi In vitro assessment of the pharmacodynamic properties of DB75, piperaquine, OZ277 and OZ401 in cultures of Plasmodium falciparum
    Sandra Hofer
    Swiss Tropical Institute, Socinstrasse 57, CH 4002 Basel, Switzerland
    J Antimicrob Chemother 62:1061-4. 2008
    ....
  20. ncbi Thiophene-based diamidine forms a "super" at binding minor groove agent
    Sirish Mallena
    Department of Chemistry, Georgia State University, P O Box 4098, Atlanta, Georgia 30302 4098, USA
    J Am Chem Soc 126:13659-69. 2004
    ....
  21. pmc Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes
    Amanda M Mathis
    Molecular Pharmaceutics, UNC School of Pharmacy, 3312 Kerr Hall, CB 7360, Chapel Hill, NC 27599, USA
    Antimicrob Agents Chemother 51:2801-10. 2007
    ..This investigation suggests that the extent of accumulation alone is not responsible for killing trypanosomes and that organelle-specific accumulation may not predict in vitro activity...
  22. ncbi Trypanocidal activity of the phenyl-substituted analogue of furamidine DB569 against Trypanosoma cruzi infection in vivo
    Elen M de Souza
    Lab Biologia Celular, DUBC, Instituto Oswaldo Cruz FIOCRUZ, Rio de Janeiro, RJ, Brasil
    J Antimicrob Chemother 58:610-4. 2006
    ..Our present aim was to investigate the efficacy of DB569 in a T. cruzi mouse model...
  23. pmc The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei
    Charlotte A Lanteri
    Department of Pathology and Laboratory Medicine, University of North Carolina, 2102C McGavran Greenberg Hall, Chapel Hill, NC 27599, USA
    Antimicrob Agents Chemother 52:875-82. 2008
    ..Taken together, these findings suggest that the mitochondrion is a target of the trypanocidal action of DB75...
  24. ncbi Thermodynamic analysis of binding of p-substituted benzamidines to trypsin
    R Talhout
    Physical Organic Chemistry Unit, Stratingh Institute, University of Groningen, The Netherlands
    Eur J Biochem 268:1554-60. 2001
    ..This behaviour might result from a bulk solvation effect, meaning that the more polar, lower potency inhibitors will be more stabilized in water than the less polar, higher potency inhibitors...
  25. ncbi Efficacy of DB289 in Thai patients with Plasmodium vivax or acute, uncomplicated Plasmodium falciparum infections
    Patrick Yeramian
    Immtech International, Vernon Hills, Illinois, USA
    J Infect Dis 192:319-22. 2005
    ..DB289 is the orally active prodrug of the diamidine DB75, which was developed for the treatment of human African trypanosomiasis...
  26. pmc Accumulation and intracellular distribution of antitrypanosomal diamidine compounds DB75 and DB820 in African trypanosomes
    Amanda M Mathis
    Division of Molecular Pharmaceutics, School of Pharmacy, University of North Carolina, Chapel Hill, Chapel 27599, USA
    Antimicrob Agents Chemother 50:2185-91. 2006
    ..Analyses of the kinetics of uptake and intracellular distribution are necessary to begin to define antitrypanosomal mechanisms of action of DB75, DB820, and other aromatic diamidines...
  27. ncbi Comparative thermodynamics for monomer and dimer sequence-dependent binding of a heterocyclic dication in the DNA minor groove
    Lei Wang
    Department of Chemistry, Georgia State University, Atlanta, GA 30303, USA
    J Mol Biol 317:361-74. 2002
    ..9 kcal/mol (per mol of bound compound), respectively. These results show that the thermodynamic components for binding of compounds of this type to DNA are very dependent on the structure, solvation and sequence of the DNA binding site...
  28. ncbi Distribution of furamidine analogues in tumor cells: targeting of the nucleus or mitochondria depending on the amidine substitution
    Amelie Lansiaux
    Institut National de la Santé et de la Recherche Médicale U 524 et Laboratoire de Pharmacologie Antitumorale du Centre Oscar Lambret, 59045 Lille, France
    Cancer Res 62:7219-29. 2002
    ..This drug design strategy may prove useful to trigger drug-induced apoptosis...
  29. ncbi Infectious keratitis in orthokeratology
    Kenneth Hutchinson
    Department of Ophthalmology, Royal Brisbane Hospital, Queensland, Australia
    Clin Experiment Ophthalmol 30:49-51. 2002
    ..Patients should be adequately warned of the associated risks and advised that any envisaged benefits of the procedure are temporary...
  30. ncbi A keratitis rat model for evaluation of anti-Acanthamoeba polyphaga agents
    Caroline Vasseneix
    Laboratoire de Parasitologie, ADEN EA 3234, CHU Charles Nicolle, Rouen, France
    Cornea 25:597-602. 2006
    ..To develop a rat model of chronic Acanthamoeba polyphaga keratitis suitable for pharmacologic assessment of therapeutic agents...
  31. ncbi Clonidine displacement from type 1 imidazoline receptor by p-aminobenzamidine, the prototype of trypsin-like serine protease inhibitors
    Valentina Pallottini
    Department of Biology, University Roma Tre, Viale G Marconi 446, 1 00146 Roma, Italy
    IUBMB Life 54:301-4. 2002
    ..Therefore, trypsin-like serine protease inhibitors structurally related to p-aminobenzamidine should be administrated under careful control...
  32. ncbi Treatment of Acanthamoeba keratitis
    David Seal
    Applied Vision Research Centre, City University, Northampton Square, London, EC1V 0HB, UK
    Expert Rev Anti Infect Ther 1:205-8. 2003
    ..This role may be taken up by certain antineoplastic drugs, such as alkylphosphocholine-1 (Miltefosine), that also have antiprotozoal activity...
  33. ncbi Visual outcome and rehabilitation in a case of bilateral acanthamoeba sclerokeratitis
    Roberto Pineda
    Department of Ophthalmology, Massachusetts Eye and Ear Infirmary, Harvard Medical School, Boston, MA 02114, USA
    Cornea 26:1150-2. 2007
    ..To report a rare and complicated case of bilateral Acanthamoeba sclerokeratitis (ASK)...
  34. ncbi Acanthamoeba keratitis associated with misuse of daily disposable contact lenses
    Nuwan Niyadurupola
    Department of Ophthalmology, The Norfolk and Norwich University Hospital, Colney Lane, Norwich, NR4 7UY, UK
    Cont Lens Anterior Eye 29:269-71. 2006
    ..To report a case of Acanthamoeba keratitis that occurred in a daily disposable contact lens wearer...
  35. ncbi An atypical presentation of Acanthamoeba keratitis in a noncontact lens wearer
    Christine E Speer
    Cornea Service, Wills Eye Hospital, Philadelphia, PA 19107, USA
    Eye Contact Lens 29:21-2. 2003
    ..His case was atypical given his lack of contact lens wear or antecedent trauma and rapid progression to a ring infiltrate, usually seen as late findings...
  36. ncbi Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles
    Donald A Patrick
    Department of Pathology and Laboratory Medicine, School of Medicine, University of North Carolina, Chapel Hill, North Carolina 27599 7525, USA
    J Med Chem 50:2468-85. 2007
    ..Fourteen of these compounds had cytotoxic indices ranging between 10 and 120 times higher than that of furamidine, and five analogues exhibited high selectivity for P. falciparum over T. brucei rhodesiense...
  37. ncbi Persistently culture positive acanthamoeba keratitis: in vivo resistance and in vitro sensitivity
    Juan J Perez-Santonja
    Cornea and External Disease Service, Moorfields Eye Hospital, London, UK
    Ophthalmology 110:1593-600. 2003
    ..To characterize the risk factors, clinical course, treatment outcome and the association between in vivo resistance and in vitro sensitivity for subjects with persistently culture-positive Acanthamoeba keratitis...
  38. ncbi [Painless acanthamoeba keratitis]
    K Stemberger
    Universitätsklinik für Augenheilkunde und Optometrie, Medizinische Universitat Innsbruck, 6020, Innsbruck
    Ophthalmologe 104:415-7. 2007
    ..Acanthamoeba keratitis should be considered even in the absence of pain, especially when the patients are contact lens wearers...
  39. ncbi Are cataract and iris atrophy toxic complications of medical treatment of acanthamoeba keratitis?
    Niels Ehlers
    Department of Ophthalmology, Arhus University Hospital, Arhus, Denmark
    Acta Ophthalmol Scand 82:228-31. 2004
    ..02% and propamidine isethionate 0.1%. It is suggested that these complications were caused by the chemicals, rather than resulting from the amoebae-induced inflammation...
  40. ncbi Understanding protein-ligand interactions: the price of protein flexibility
    Daniel Rauh
    Institut für Pharmazeutische Chemie der Philipps, Universitat Marburg, Marbacher Weg 6, D35032 Marburg, Germany
    J Mol Biol 335:1325-41. 2004
    ..The insights provided by these studies will be helpful in improving our understanding of ligand binding for the drug design process...
  41. ncbi Azaterphenyl diamidines as antileishmanial agents
    Laixing Hu
    Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, Atlanta, GA 30303, USA
    Bioorg Med Chem Lett 18:247-51. 2008
    ..Transmission electron microscopy studies showed a dramatic dilation of the mitochondrion and evidence of disintegration of the kinetoplast of the amastigotes...
  42. ncbi DB-289 Immtech International
    Clive Yeates
    6 Dudley Hill Close, Welwyn, Herts, AL6 0QQ, UK
    IDrugs 6:1086-93. 2003
    ....
  43. ncbi Acanthamoeba keratitis during orthokeratology
    Kirk R Wilhelmus
    Cullen Eye Institute, Department of Ophthalmology, Baylor College of Medicine, Houston, TX 77030, USA
    Cornea 24:864-6. 2005
    ..To report an infectious complication of overnight rigid gas-permeable contact lenses...
  44. ncbi [Acanthamoeba keratitis, a possible dibromo propamidine isethionate resistance]
    M Vaquero Ruano
    Hospital Universitario Clinica Puerta de Hierro, Madrid, Espana
    Arch Soc Esp Oftalmol 77:279-81. 2002
    ..To point out that acanthamoeba keratitis can show therapeutical resistance to dibrome propamidine isethionate (Brolene). We have a late diagnosis case of corneal melting on a bilateral acanthamoeba keratitis...
  45. ncbi Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors
    Penglie Zhang
    Department of Medicinal Chemistry, Millennium Pharmaceuticals, Inc, 256 E Grand Avenue, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 12:1657-61. 2002
    ..The monoamidines show high efficacy in a DVT model, but lack desirable oral bioavailability. The benzopyrrolidinone-based aminoisoquinolines 8 do not show significant improvement in oral bioavailability...
  46. ncbi [Acanthamoeba keratitis treated with propamidine and polyhexamethyl biguanide (PHMB)]
    Rodrigo Donoso
    Servicio de Oftalmologia, Hospital del Salvador, Santiago Chile
    Rev Med Chil 130:396-401. 2002
    ..The use of biassociated therapy has resulted in a better prognosis and lower complication rate...
  47. ncbi Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification
    Yonghong Song
    Millennium Pharmaceuticals, Inc, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 12:2043-6. 2002
    ..Modification of P4 moiety of these compounds further improved their pharmacokinetic properties...
  48. pmc Interaction of monobenzamidine-linked trypanocides with the Trypanosoma brucei P2 aminopurine transporter
    Mhairi L Stewart
    University of Glasgow, Institute of Biomedical and Life Sciences, Division of Infection and Immunity, Glasgow G12 8QQ, United Kingdom
    Antimicrob Agents Chemother 49:5169-71. 2005
    ..Trypanocidal activity was evident, but compounds were equally toxic against trypanosomes lacking the P2 transporter, which indicates additional uptake routes for monobenzamidine-derived compounds...
  49. pmc Corin, a transmembrane cardiac serine protease, acts as a pro-atrial natriuretic peptide-converting enzyme
    W Yan
    Department of Cardiovascular Research, Berlex Biosciences, 15049 San Pablo Avenue, Richmond, CA 94804, USA
    Proc Natl Acad Sci U S A 97:8525-9. 2000
    ..Our findings suggest that corin is the long-sought pro-ANP-converting enzyme and that the corin-mediated pro-ANP activation may play a role in regulating blood pressure...
  50. ncbi Rapidly progressive cataract and iris atrophy during treatment of Acanthamoeba keratitis
    Natasha L Herz
    Sid W Richardson Ocular Microbiology Laboratory, Cullen Eye Institute, Department of Ophthalmology, Baylor College of Medicine, Houston, Texas, USA
    Ophthalmology 115:866-9. 2008
    ..To identify characteristics associated with cataract occurring during the course of Acanthamoeba keratitis...
  51. ncbi Antiparasitic activity of aromatic diamidines is related to apoptosis-like death in Trypanosoma cruzi
    E M De Souza
    Lab Biologia Celular, DUBC, Instituto Oswaldo Cruz, FIOCRUZ, Avenida Brasil 4365, Manguinhos, 21045 900, Rio de Janeiro, RJ, Brasil
    Parasitology 133:75-9. 2006
    ..cruzi after treatment with both DB75 and DB569 make important contributions to the understanding of the mechanisms of the aromatic diamidines, which represent promising trypanocidal compounds...
  52. ncbi Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa
    Barbara A Schweitzer
    Department of Medicinal and Combinatorial Chemistry, Pfizer Corp, 800 N Lindbergh Blvd, St Louis, MO 63167, USA
    Bioorg Med Chem Lett 15:3006-11. 2005
    ....
  53. ncbi [Acanthamoeba keratitis: about the first two Tunisian cases]
    S Ben Salah
    Service d Ophtalmologie, CHU Habib Bourguiba, Sfax, Tunisie
    Bull Soc Pathol Exot 100:41-2. 2007
    ..Trophozoit and cysts of Acanthamoeba were found in the contact lens solution. She was treated quickly with Désomédine. Visual acuity improved to 7/10 but the corneal ulceration left a residual opacity..
  54. ncbi Design, synthesis, and biological activity of potent and selective inhibitors of blood coagulation factor Xa
    J Adam Willardsen
    Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA
    J Med Chem 47:4089-99. 2004
    ....
  55. ncbi Crystal structure reveals basis for the inhibitor resistance of human brain trypsin
    Gergely Katona
    Department of Biochemistry, Eotvos Lorand University, Puskin u 3, Budapest, 1088, Hungary
    J Mol Biol 315:1209-18. 2002
    ..These unique features of the crystal structure provide a structural basis for the enhanced inhibitor resistance, and enhanced substrate restriction, of human trypsin IV...
  56. ncbi N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors
    Zhaozhong J Jia
    Millennium Pharmaceuticals, Inc, 256 East Grand Ave, South San Francisco, CA 94080, USA
    Bioorg Med Chem Lett 14:2073-8. 2004
    A class of N,N-dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines has been discovered as potent factor Xa inhibitors with desirable in vitro and in vivo ..
  57. ncbi Relocating a negative charge in the binding pocket of trypsin
    J J Perona
    Department of Pharmaceutical Chemistry, University of California, San Francisco 94143 0446
    J Mol Biol 230:934-49. 1993
    ..This structural flexibility may be of critical importance to the retention of catalytic activity by the variant enzyme...
  58. ncbi Determination of ligand-protein dissociation constants by electrospray mass spectrometry-based diffusion measurements
    Sonya M Clark
    Department of Chemistry, The University of Western Ontario, London, Ontario N6A 5B7, Canada
    Anal Chem 76:7077-83. 2004
    ....
  59. ncbi Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants
    Patrick Y S Lam
    Bristol Myers Squibb Company, P O Box 5400, Princeton, New Jersey 08542 5400, USA
    J Med Chem 46:4405-18. 2003
    ..SQ311, which utilizes a 1-aminoisoquinoline as the P1 ligand, inhibits factor Xa with a K(i) of 0.33 nM and demonstrates both good in vivo antithrombotic efficacy and oral bioavailability...
  60. ncbi Trypanocidal activity of piperazine-linked bisbenzamidines and bisbenzamidoxime, an orally active prodrug
    Tien L Huang
    College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA
    Int J Antimicrob Agents 30:555-61. 2007
    ..Three compounds (7, 11 and 15) provided 100% cure when administered parenterally. The results indicate that the nature of the substituents at the amidinium nitrogens of bisbenzamidines strongly influence their trypanocidal activity...
  61. ncbi Design, synthesis, and evaluation of oxyanion-hole selective inhibitor substituents for the S1 subsite of factor Xa
    Sochanchingwung Rumthao
    Center for Pharmaceutical Biotechnology, University of Illinois at Chicago, 900 S Ashland Avenue, M C 870, Chicago, IL 60607 7173, USA
    Bioorg Med Chem Lett 14:5165-70. 2004
    ..One nonamidine based substituent also shows promising activity...
  62. ncbi PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors
    John W Liebeschuetz
    Protherics Molecular Design, Beechfield House, Lyme Green Business Park, Macclesfield SK11 0JL, UK
    J Med Chem 45:1221-32. 2002
    ..Highly potent molecules with selectivity for factor Xa over other serine proteases were rapidly obtained...
  63. ncbi Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library
    Patrick Y S Lam
    Bristol Myers Squibb Co, Experimental Station, PO Box 80500, Wilmington, DE 19880 0500, USA
    Bioorg Med Chem Lett 13:1795-9. 2003
    ..In an effort to identify orally bioavailable factor Xa inhibitors, two isoxazolines libraries were prepared to scan for novel P1 ligands. From this work, 4-chloro-3-aniline was identified as a novel and potent benzamidine mimic...
  64. ncbi Characterizing the fragmentation of 2,5-bis (4-amidinophenyl)furan-bis-O-methylamidoxime and selected metabolites using ion trap mass spectrometry
    Lian Zhou
    Division of Medicinal Chemistry and Natural Products, School of Pharmacy, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
    Rapid Commun Mass Spectrom 16:1078-85. 2002
    ..The fragmentation pathways uncovered in this work will facilitate structural characterization of all the metabolites produced in the metabolic activation of DB289...
  65. ncbi Melarsoprol- and pentamidine-resistant Trypanosoma brucei rhodesiense populations and their cross-resistance
    Sonja C Bernhard
    Swiss Tropical Institute, Socinstr 57, Basel, Switzerland
    Int J Parasitol 37:1443-8. 2007
    ..The melarsoprol-selected population apparently had lost TbAT1, whereas in the pentamidine-selected trypanosome population it was still present...
  66. ncbi Chronic microsporidial stromal keratitis in an immunocompetent, non-contact lens wearer
    Rajesh Fogla
    Cornea Services, Sankara Nethralaya, Chennai, India
    Indian J Ophthalmol 53:123-5. 2005
    ..Electron microscopy of the keratoplasty specimen demonstrated sporoblasts with diplokaryotic nuclei and multiple coils of the filament. The light and electron microscopic features were consistent with microsporidial keratitis...
  67. ncbi Amidine nitrosation
    Richard N Loeppky
    Department of Chemistry, University of Missouri Columbia, Columbia, Missouri 65211, USA
    J Org Chem 69:3015-24. 2004
    ..Tertiary amidines also produce nitrosamines in minor, but significant, yields. The benzamidines did not react, and the N-acylamidines hydrolyzed much more rapidly than they nitrosated...
  68. ncbi 1,2-ethane bis-1-amino-4-benzamidine is active against several brain insult and seizure challenges through anti-NMDA mechanisms targeting the 3H-TCP binding site and antioxidant action
    Joseph Vamecq
    INSERM UNIV 045131, Faculty of Medicine, Research Branch, University of Lille 2, France
    Eur J Med Chem 45:3101-10. 2010
    Five bis-benzamidines were screened towards murine magnesium deficiency-dependent audiogenic seizures, unravelling two compounds with efficacious doses 50 (ED(50)) less than 10mg/kg...
  69. ncbi Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase
    Julian Levell
    Drug Innovation and Approval, Aventis Pharmaceuticals, 1041 Route 202 206, Mail Stop N 103A, Bridgewater, NJ 08807 6800, USA
    Bioorg Med Chem 13:2859-72. 2005
    ..Screening of in-house inhibitors of factor Xa (a closely related serine protease) identified beta-amidoester benzamidines as potent inhibitors of recombinant human betaII tryptase...
  70. ncbi Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand
    Yong Mi Choi-Sledeski
    Department of Medicinal Chemistry and Department of Biology, Aventis Pharmaceuticals, Route 202 206, Bridgewater, New Jersey 08807 0800, USA
    J Med Chem 46:681-4. 2003
    ..33 (RPR209685), is selective against related serine proteases and attains higher levels of exposure upon oral dosing than comparable benzamidines and benzamidine isosteres. Compound 33 was efficacious in the canine AV model of thrombosis.
  71. ncbi Ligand-free copper-catalyzed arylation of amidines
    Michelle Cortes-Salva
    Department of Chemistry, University of South Florida, 4202 East Fowler Avenue CHE 205A, Tampa, Florida 33620, USA
    J Org Chem 76:1456-9. 2011
    ..DMF was the superior solvent for the N-arylation of benzamidines, while MeCN was used in the formation of N-aryl amidines in moderate to high yield.
  72. ncbi Screening of benzamidine-based thrombin inhibitors via a linear interaction energy in continuum electrostatics model
    Orazio Nicolotti
    Dipartimento Farmaco Chimico, University of Bari, Via Orabona 4, 70125, Bari, Italy
    J Comput Aided Mol Des 24:117-29. 2010
    ..The herein proposed LIECE model has the potential for successfully driving the design of novel thrombin inhibitors with benzamidine and/or benzamidine-like chemical structure...
  73. ncbi Synthesis, antileishmanial activity and structure-activity relationship of 1-N-X-phenyl-3-N'-Y-phenyl-benzamidines
    Cláudio Eduardo Rodrigues-Santos
    Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal Rural do Rio de Janeiro, 23890 900 Seropédica, RJ, Brazil
    Eur J Med Chem 67:166-74. 2013
    Two series of N,N'-diphenyl-benzamidines were synthesized as part of a study to search potential new drugs with antileishmanial activity...
  74. ncbi Copper catalyzed N-arylation of amidines with aryl boronic acids and one-pot synthesis of benzimidazoles by a Chan-Lam-Evans N-arylation and C-H activation/C-N bond forming process
    Jihui Li
    Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, Laboratoire International Associé, CNRS, 91198 Gif sur Yvette Cedex, France
    Org Lett 14:5980-3. 2012
    Mono-N-arylation of benzamidines 1 with aryl boronic acids 2 was effectively achieved in the presence of a catalytic amount of Cu(OAc)(2) and NaOPiv under mild aerobic conditions...
  75. ncbi Acanthamoeba keratitis due to Acanthamoeba genotype T4 in a non-contact-lens wearer in Turkey
    Hatice Ertabaklar
    Department of Parasitology, Adnan Menderes University Medical Faculty, Aydin, Turkey
    Parasitol Res 100:241-6. 2007
    ..To the best of our knowledge, this is the first study identifying an AK-causing Acanthamoeba strain in Turkey and the first isolation of genotype T9 in this country...
  76. ncbi Riboflavin and ultraviolet light a therapy as an adjuvant treatment for medically refractive Acanthamoeba keratitis: report of 3 cases
    Yasin A Khan
    The Wilmer Ophthalmological Institute, The Johns Hopkins University, School of Medicine, Baltimore, Maryland 21205, USA
    Ophthalmology 118:324-31. 2011
    ..To present the first 3 cases of Acanthamoeba keratitis (AK), unresponsive to medical treatment, that were successfully treated with a novel adjunctive therapy using ultraviolet light A (UVA) and riboflavin (B2)...
  77. pmc Large, sequence-dependent effects on DNA conformation by minor groove binding compounds
    Denise S Tevis
    Department of Chemistry, Georgia State University, Atlanta, GA 30302, USA
    Nucleic Acids Res 37:5550-8. 2009
    ..With ATATA the groove is intrinsically wider and must close to bind the compounds tightly. The conformational change at the binding site then leads to significant bending of the alternating DNA sequence...
  78. ncbi Reverse-benzamidine antimalarial agents: design, synthesis, and biological evaluation
    Olivier Berger
    Institut des Biomolécules Max Mousseron UMR 5247 CNRS Universités Montpellier I et II, Faculte de Pharmacie, 15 av Ch Flahault, 34093 Montpellier Cedex 5, France
    Bioorg Med Chem Lett 20:5815-7. 2010
    ..Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies...
  79. ncbi Co-isolation of Vahlkampfia and acanthamoeba in acanthamoeba-like keratitis in a Spanish population
    Francisco Arnalich-Montiel
    Cornea Unit, Ophthalmology Department, Ramon y Cajal Hospital, Madrid, Spain
    Cornea 32:608-14. 2013
    ..To report the co-isolation incidence of Acanthamoeba and Vahlkampfia in amoebic keratitis from a tertiary care institution in Madrid, Spain...
  80. ncbi Bilateral acanthamoeba keratitis
    Kirk R Wilhelmus
    Cullen Eye Institute, Department of Ophthalmology, Baylor College of Medicine, 6565 Fannin Street, Houston, TX 77030, USA
    Am J Ophthalmol 145:193-197. 2008
    ..To determine the prevalence and characteristics of binocular involvement among patients with Acanthamoeba keratitis...
  81. ncbi Copper-catalyzed synthesis of quinazolines in water starting from o-bromobenzylbromides and benzamidines
    Chandi C Malakar
    Institut fur Chemie, Universitat Hohenheim, Garbenstr 30, 70599 Stuttgart, Deutschland
    Chemistry 18:8882-5. 2012
    Water makes it possible: The Cu(2)O-catalyzed reaction between easily available o-bromobenzylbromides and benzamidines by using Cs(2)CO(3) as the base and N,N'-dimethylethylenediamine (DMEDA) as the additive in water as the solvent gives ..
  82. ncbi Spectroscopic characterization of bioactive carboxyamide with trinuclear lanthanide (III) ions
    Bibhesh K Singh
    Inorganic and Bioinorganic Research Lab, Department of Chemistry, Govt Postgraduate College, Ranikhet 263645 Uttarakhand, India
    Spectrochim Acta A Mol Biomol Spectrosc 74:657-64. 2009
    ..Kinetic and thermodynamic parameters were computed from the thermal data using Coats and Redferm method, which confirm first order kinetics...
  83. ncbi Insights into structure-activity relationships and CNS therapeutic applications of NR2B selective antagonists
    C Beinat
    School of Chemistry, University of Sydney, NSW 2006, Australia
    Curr Med Chem 17:4166-90. 2010
    ..This review describes recent advances in the development of NR2B antagonists as well as their therapeutic applications...
  84. ncbi Interaction of proteinase inhibitors with Cry1Ac toxicity and the presence of 15 chymotrypsin cDNAs in the midgut of the tobacco budworm, Heliothis virescens (F.) (Lepidoptera: Noctuidae)
    Yu Cheng Zhu
    USDA ARS, Stoneville, MS, USA
    Pest Manag Sci 68:692-701. 2012
    ..Proactive action to examine proteinase inhibitors for synergistic interaction with Bt toxin and cloning of proteinase cDNAs for RNAi is necessary to make transgenic cotton more versatile and durable...
  85. ncbi Acanthamoeba keratitis: 2007: a train wreck in slow motion
    H Dwight Cavanagh
    Eye Contact Lens 33:209. 2007
  86. ncbi Limitations of conventional inhibitor classifications
    Ryan Walsh
    Department of Chemistry, Carleton University, Ottawa, Ontario, Canada
    Integr Biol (Camb) 3:1197-201. 2011
    ..The arguments presented are illustrated using the known competitive inhibition of Kallikrein with benzamidine...
  87. ncbi Reduction of N(ω)-hydroxy-L-arginine by the mitochondrial amidoxime reducing component (mARC)
    Jürke Kotthaus
    Department of Pharmaceutical and Medicinal Chemistry, Pharmaceutical Institute, Christian Albrechts University of Kiel, Germany
    Biochem J 433:383-91. 2011
    ..Moreover, this reduction is not restricted to NOHA since the analogous arginase inhibitor NHAM (N(ω)-hydroxy-N(δ)-methyl-L-arginine) is also reduced by this system...
  88. ncbi ONO 3403, a synthetic serine protease inhibitor, inhibits lipopolysaccharide-induced tumor necrosis factor-{alpha} and nitric oxide production and protects mice from lethal endotoxic shock
    Gantsetseg Tumurkhuu
    Department of Microbiology and Immunology, Aichi Medical University School of Medicine, Nagakute, Aichi, Japan
    Innate Immun 17:97-105. 2011
    ..ONO 3403 was suggested to inhibit LPS-induced inflammatory responses via inactivation of MyD88-dependent and independent pathways...
  89. ncbi A recombinant, chimeric enzyme with a novel mechanism of action leading to greater potency and selectivity than tissue-type plasminogen activator
    J H Robinson
    Department of Biotechnology, SmithKline Beecham Pharmaceuticals, Surrey, England, UK
    Circulation 86:548-52. 1992
    ..CONCLUSIONS. An acylated, recombinant plasminogen/t-PA hybrid has sufficiently slow clearance to be administered by bolus and is more potent and fibrin selective than t-PA in vivo...
  90. ncbi Thrombin inhibition by novel benzamidine derivatives: a free-energy perturbation study
    Cristiano Ruch Werneck Guimarães
    Physical Organic Chemistry Group, Departamento de Quimica Organica, Instituto de Quimica, Universidade Federal do Rio de Janeiro, Cidade Universitaria, CT, Bloco A, lab 609, Brazil
    J Med Chem 45:4995-5004. 2002
    ..We also obtained the following order for thrombin binding: p-(2-oxo-1-propyl)benzamidine > p-ethylbenzamidine > p-(1-propyl)benzamidine > p-methylbenzamidine > benzamidine > p-amidinophenylpyruvate...
  91. ncbi The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa
    S D Jones
    Prosthetics Molecular Design, Beechfield House, Macclesfield, UK
    Bioorg Med Chem Lett 11:733-6. 2001
    ..Here we describe the development of phenylglycine containing benzamidine carboxamides as novel, potent and selective inhibitors of factor Xa...
  92. ncbi Purification and partial characterization of feline classical pancreatic lipase
    Jorg M Steiner
    Gastrointestinal Laboratory, Department of Small Animal Medicine and Surgery, College of Veterinary Medicine, Texas A and M University, College Station, TX, USA
    Comp Biochem Physiol B Biochem Mol Biol 134:151-9. 2003
    ..This sequence showed close homology with the amino acid sequence of classical pancreatic lipase in other species...
  93. ncbi Different effects of trypsin inhibitors on intestinal gene expression of secretin and on pancreatic bicarbonate secretion in CCK-A-receptor-deficient rats
    T Kawanami
    Department of Clinical Physiology, Tokyo Metropolitan Institute of Gerontology, Japan
    Jpn J Pharmacol 81:339-45. 1999
    ..These observations suggest that increased bicarbonate secretion produced by synthetic trypsin inhibitors in CCK-A-receptor-deficient rats may not be due to secretin but due to ONO-3403 in the circulation...
  94. ncbi Receptor rigidity and ligand mobility in trypsin-ligand complexes
    Olgun Guvench
    Department of Molecular Biology TPC 6, The Scripps Research Institute, La Jolla, California 92037, USA
    Proteins 58:407-17. 2005
    ....
  95. ncbi Effects of a new cholecystokinin antagonist, TS-941, on experimental acute pancreatitis in rats
    Y Wang
    Department of Internal Medicine II, Nagoya University School of Medicine, Japan
    Pancreas 17:289-94. 1998
    ..ONO-3403 has beneficial effects on trypsin-taurocholate-induced hemorrhagic pancreatitis, but the combination of TS-941 and ONO-3403 has no additive effect...
  96. ncbi Aromatic amidines: inhibitory effect on purified plasma serine proteinases, blood coagulation and platelet aggregation
    R Ferroni
    Dipartimento di Scienze Farmaceutiche, , Italy
    Farmaco Sci 43:5-13. 1988
    ....
  97. ncbi AT selectivity and DNA minor groove binding: modelling, NMR and structural studies of the interactions of propamidine and pentamidine with d(CGCGAATTCGCG)2
    T C Jenkins
    CRC Biomolecular Structure Unit, Institute of Cancer Research, Sutton, UK
    Biochim Biophys Acta 1350:189-204. 1997
    ....
  98. ncbi Neutrophil elastase cleavage of human factor IX generates an activated factor IX-like product devoid of coagulant function
    J A Samis
    Department of Pathology, Queen s University, Kingston, Ontario, Canada
    Blood 92:1287-96. 1998
    ..These in vitro observations support the possibility that increased HNE cleavage of F.IX in vivo may contribute to the disregulation of hemostasis that occurs in conditions such as disseminated intravascular coagulation (DIC)...
  99. ncbi I2-catalyzed oxidative cross-coupling of methyl ketones and benzamidines hydrochloride: a facile access to α-ketoimides
    Xia Wu
    Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, P R China
    Org Lett 16:2888-91. 2014
    ..simple and efficient approach constructed α-ketoimides in good to excellent yields from methyl ketones and benzamidines hydrochloride under metal-free and peroxide-free conditions...
  100. ncbi [Microbiological analysis in contact lens-associated keratits]
    M R R Böhm
    Klinik und Poliklinik für Augenheilkunde, Universitatsklinikum Munster
    Klin Monbl Augenheilkd 228:808-14. 2011
    ..0.011 - 0.2 % of the wearers develop keratitis per year. The aim of this study was to explore and analyse the spectrum of germs in different microbiological analysis techniques to optimize the strategy of antiobiotic therapy...
  101. ncbi Efficacy of miltefosine for topical treatment of Acanthamoeba keratitis in Syrian hamsters
    Zubeyde Akin Polat
    Department of Medical Parasitology, Cumhuriyet University School of Medicine, 58140 Sivas, Turkey
    Parasitol Res 110:515-20. 2012
    ..Furthermore, no Acanthamoeba cells could be recovered from the miltefosine-treated eye samples. Miltefosine appeared to hold necessary therapeutic properties for the treatment of Acanthamoeba keratitis...

Research Grants14

  1. FOCUSED PARALLEL SYNTHESIS OF DICATION ANTIFUNGAL AGENTS
    Richard Tidwell; Fiscal Year: 2003
    ..abstract_text> ..
  2. Ophthalmic Antibiotic Resistance Study
    Kirk Wilhelmus; Fiscal Year: 2003
    ..abstract_text> ..
  3. TRANSMISSION OF PNEUMOCYSTIS INFECTION
    Melanie Cushion; Fiscal Year: 2001
    ..These studies will result in a clearer understanding of the biology leading to infection with Pc and will provide a rational basis for clinical management and therapeutic intervention. ..
  4. LACTATIONAL EFFECTORS OF TRIACYLGLYCEROL MOBILIZATION
    JAMES MCMANAMAN; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  5. Simple, Selective Antimitotic Antiparasitic Agents
    Karl Werbovetz; Fiscal Year: 2007
    ..abstract_text> ..
  6. New Approaches for Development of PcP Therapy
    Melanie Cushion; Fiscal Year: 2006
    ..Finally, they will select the most efficacious combinations of agents and evaluate their effects on gene expression again using the macroarray approach. ..
  7. PNEUMOCYSTIS GENOME PROJECT
    Melanie Cushion; Fiscal Year: 2004
    ..Thus, there is but a single aim to this proposal: 1. To finish sequencing the genome of pneumocystis carinii and provide a completed assembly. ..
  8. ENDOGENOUS NITROSATION CHEMISTRY IN CARCINOGENESIS
    RICHARD LOEPPKY; Fiscal Year: 2004
    ..Computational methods will be employed to reveal reaction paths of intermediates and lead to better predictions of the types of compounds which pose a carcinogenic threat through their endogenous nitrosation. ..
  9. Eighth International Workshops on Opportunistic Protists
    Melanie Cushion; Fiscal Year: 2003
    ..Mead's and Cushion's ancestors include native Americans; Marciano-Cabral is Hispanic; Kaneshiro has Pacific-Asian ancestry; Lindsay, Weiss are white. Lindsay is a physically handicapped individual. ..
  10. MECHANISMS OF HORMONE THERAPY IN POSTMENOPAUSAL WOMEN
    L Newby; Fiscal Year: 2003
    ....
  11. ANTI-VIRAL TREATMENT OF DEVELOPING BOVINE EMBRYOS
    Maurice Givens; Fiscal Year: 2002
    ....
  12. AP13000 LCMS/MS System
    Richard Tidwell; Fiscal Year: 2002
    ..Drs. Hall and Kashuba will prioritize CPA CC use and Dr. Gary Pollack will prioritize use by School of Pharmacy scientists. The instrument will be housed in newly renovated space in the School of Pharmacy. ..
  13. CARCINOGENESIS--HIGHLY REACTIVE NITROSAMINES
    RICHARD LOEPPKY; Fiscal Year: 2001
    ....
  14. Actin assembly in platelets & megakaryoctyes
    Charles Abrams; Fiscal Year: 2008
    ..In the second Aim, we will formally address how PIP2 drives reorganization of platelet actin using a combination of biochemistry, murine genetics, and ex vivo platelet adhesion models. ..