pyridones

Summary

Summary: Pyridine derivatives with one or more keto groups on the ring.

Top Publications

  1. ncbi Diverse functionalization of thiazolo ring-fused 2-pyridones
    Erik Chorell
    Department of Chemistry, Umea University, SE 90187 Umea, Sweden
    J Org Chem 72:4917-24. 2007
  2. ncbi Pirfenidone in patients with idiopathic pulmonary fibrosis (CAPACITY): two randomised trials
    Paul W Noble
    Duke University School of Medicine, Durham, NC 27710, USA
    Lancet 377:1760-9. 2011
  3. ncbi Apixaban in patients with atrial fibrillation
    Stuart J Connolly
    Population Health Research Institute, McMaster University and Hamilton Health Sciences, Hamilton, ON, Canada
    N Engl J Med 364:806-17. 2011
  4. ncbi GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition
    Aidan G Gilmartin
    GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Clin Cancer Res 17:989-1000. 2011
  5. ncbi Pirfenidone in idiopathic pulmonary fibrosis
    H Taniguchi
    Dept of Respiratory Medicine, Tosei General Hospital, Aichi, Japan
    Eur Respir J 35:821-9. 2010
  6. ncbi Double-blind, placebo-controlled trial of pirfenidone in patients with idiopathic pulmonary fibrosis
    Arata Azuma
    Fourth Department of Internal Medicine, Nippon Medical School, Tokyo, Japan
    Am J Respir Crit Care Med 171:1040-7. 2005
  7. ncbi Apixaban versus enoxaparin for thromboprophylaxis after hip replacement
    Michael Rud Lassen
    Department of Orthopedics, Spine Clinic, and Clinical Trial Unit, Hørsholm Hospital, University of Copenhagen, Hørsholm, Denmark
    N Engl J Med 363:2487-98. 2010
  8. ncbi Apixaban or enoxaparin for thromboprophylaxis after knee replacement
    Michael Rud Lassen
    Department of Orthopedics, Spine Clinic, Clinical Trial Unit, Hørsholm Hospital, University of Copenhagen, Hørsholm, Denmark
    N Engl J Med 361:594-604. 2009
  9. pmc Pirfenidone inhibits transforming growth factor-β1-induced fibrogenesis by blocking nuclear translocation of Smads in human retinal pigment epithelial cell line ARPE-19
    Kyungsun Choi
    Department of Bio and Brain Engineering, KAIST, Daejeon, Republic of Korea
    Mol Vis 18:1010-20. 2012
  10. ncbi Apixaban with antiplatelet therapy after acute coronary syndrome
    John H Alexander
    Duke Clinical Research Institute, Duke University Medical Center, Durham, NC 27715, USA
    N Engl J Med 365:699-708. 2011

Detail Information

Publications290 found, 100 shown here

  1. ncbi Diverse functionalization of thiazolo ring-fused 2-pyridones
    Erik Chorell
    Department of Chemistry, Umea University, SE 90187 Umea, Sweden
    J Org Chem 72:4917-24. 2007
    Thiazolo ring-fused 2-pyridones have proven to be highly interesting scaffolds for the development of biologically active compounds...
  2. ncbi Pirfenidone in patients with idiopathic pulmonary fibrosis (CAPACITY): two randomised trials
    Paul W Noble
    Duke University School of Medicine, Durham, NC 27710, USA
    Lancet 377:1760-9. 2011
    ....
  3. ncbi Apixaban in patients with atrial fibrillation
    Stuart J Connolly
    Population Health Research Institute, McMaster University and Hamilton Health Sciences, Hamilton, ON, Canada
    N Engl J Med 364:806-17. 2011
    ..Apixaban, a novel factor Xa inhibitor, may be an alternative treatment for such patients...
  4. ncbi GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition
    Aidan G Gilmartin
    GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Clin Cancer Res 17:989-1000. 2011
    ..Our studies characterize GSK1120212' enzymatic, cellular, and in vivo activities, describing its unusually long circulating half-life...
  5. ncbi Pirfenidone in idiopathic pulmonary fibrosis
    H Taniguchi
    Dept of Respiratory Medicine, Tosei General Hospital, Aichi, Japan
    Eur Respir J 35:821-9. 2010
    ..Pirfenidone was relatively well tolerated in patients with IPF. Treatment with pirfenidone may decrease the rate of decline in VC and may increase the PFS time over 52 weeks. Additional studies are needed to confirm these findings...
  6. ncbi Double-blind, placebo-controlled trial of pirfenidone in patients with idiopathic pulmonary fibrosis
    Arata Azuma
    Fourth Department of Internal Medicine, Nippon Medical School, Tokyo, Japan
    Am J Respir Crit Care Med 171:1040-7. 2005
    ..In conclusion, treatment with pirfenidone improved VC and prevented acute exacerbation of IPF during the 9 months of follow-up. Future long-term studies are needed to clarify the overall safety and efficacy of pirfenidone in IPF...
  7. ncbi Apixaban versus enoxaparin for thromboprophylaxis after hip replacement
    Michael Rud Lassen
    Department of Orthopedics, Spine Clinic, and Clinical Trial Unit, Hørsholm Hospital, University of Copenhagen, Hørsholm, Denmark
    N Engl J Med 363:2487-98. 2010
    ..Orally active, specific factor Xa inhibitors such as apixaban may provide effective thromboprophylaxis with a lower risk of bleeding and improved ease of use...
  8. ncbi Apixaban or enoxaparin for thromboprophylaxis after knee replacement
    Michael Rud Lassen
    Department of Orthopedics, Spine Clinic, Clinical Trial Unit, Hørsholm Hospital, University of Copenhagen, Hørsholm, Denmark
    N Engl J Med 361:594-604. 2009
    ..Apixaban, a specific factor Xa inhibitor, may provide effective thromboprophylaxis with a low risk of bleeding and improved ease of use...
  9. pmc Pirfenidone inhibits transforming growth factor-β1-induced fibrogenesis by blocking nuclear translocation of Smads in human retinal pigment epithelial cell line ARPE-19
    Kyungsun Choi
    Department of Bio and Brain Engineering, KAIST, Daejeon, Republic of Korea
    Mol Vis 18:1010-20. 2012
    ..Herein, we tested the effect of pirfenidone, a novel antifibrotic agent, on TGF-β1-mediated fibrogenesis in the human RPE cell line ARPE-19...
  10. ncbi Apixaban with antiplatelet therapy after acute coronary syndrome
    John H Alexander
    Duke Clinical Research Institute, Duke University Medical Center, Durham, NC 27715, USA
    N Engl J Med 365:699-708. 2011
    ..Apixaban, an oral, direct factor Xa inhibitor, may reduce the risk of recurrent ischemic events when added to antiplatelet therapy after an acute coronary syndrome...
  11. ncbi Apixaban versus enoxaparin for thromboprophylaxis after knee replacement (ADVANCE-2): a randomised double-blind trial
    Michael Rud Lassen
    Department of Orthopaedics, Spine Clinic, Clinical Trial Unit, Hørsholm Hospital, University of Copenhagen, Hørsholm, Denmark
    Lancet 375:807-15. 2010
    ..Apixaban, an orally active factor Xa inhibitor, might be as effective, have lower bleeding risk, and be easier to use than is enoxaparin. We assessed efficacy and safety of these drugs after elective total knee replacement...
  12. ncbi Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in development
    Bengt I Eriksson
    Orthopaedics Department, University Hospital Sahlgrenska Ostra, Gothenburg, Sweden
    Clin Pharmacokinet 48:1-22. 2009
    ..Here, we compare the pharmacokinetic and pharmacodynamic features of these new oral agents...
  13. ncbi Apixaban metabolism and pharmacokinetics after oral administration to humans
    Nirmala Raghavan
    Pharmaceutical Candidate Optimization, Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543 4000, USA
    Drug Metab Dispos 37:74-81. 2009
    ..Thus, apixaban is an orally bioavailable inhibitor of factor Xa with elimination pathways that include metabolism and renal excretion...
  14. ncbi Chelation of intracellular iron with the antifungal agent ciclopirox olamine induces cell death in leukemia and myeloma cells
    Yanina Eberhard
    Princess Margaret Hospital, Ontario Cancer Institute, Toronto, ON, Canada
    Blood 114:3064-73. 2009
    ..Thus, in summary, CPX has previously unrecognized anticancer activity at concentrations that are pharmacologically achievable. Therefore, CPX could be rapidly repurposed for the treatment of malignancies, including leukemia and myeloma...
  15. ncbi Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies
    P C Wong
    Thrombosis Research, Bristol Myers Squibb Company, Pennington, NJ 08534, USA
    J Thromb Haemost 6:820-9. 2008
    ..Apixaban is an oral, direct and highly selective factor Xa (FXa) inhibitor in late-stage clinical development for the prevention and treatment of thromboembolic diseases...
  16. ncbi Efficacy and safety of the oral direct factor Xa inhibitor apixaban for symptomatic deep vein thrombosis. The Botticelli DVT dose-ranging study
    H Buller
    Department of Vascular Medicine, Academic Medical Centre, University of Amsterdam, Amsterdam, The Netherlands
    J Thromb Haemost 6:1313-8. 2008
    ..We conducted a dose-ranging study in patients with deep vein thrombosis...
  17. ncbi Clinical laboratory measurement of direct factor Xa inhibitors: anti-Xa assay is preferable to prothrombin time assay
    Yu Chen Barrett
    Bristol Myers Squibb, Princeton, New Jersey, USA
    Thromb Haemost 104:1263-71. 2010
    ..88-0.89) compared with PT/INR (r2 = 0.36) in patients undergoing VTE treatment suggested that anti-Xa activity was the better indicator of apixaban plasma concentrations...
  18. ncbi Antifibrotic action of pirfenidone and prednisolone: different effects on pulmonary cytokines and growth factors in bleomycin-induced murine pulmonary fibrosis
    Hisashi Oku
    Division of Frontier Drug Discovery, Discovery Research Laboratories, Shionogi and Co, Ltd, 2 5 1, Mishima, Settsu, Osaka 566 0022, Japan
    Eur J Pharmacol 590:400-8. 2008
    ..The effect on SDF-1alpha and IL-18 levels may also be related to the antifibrotic effects of pirfenidone...
  19. ncbi Effect of pirfenidone on rat hepatic stellate cell proliferation and collagen production
    Antonio Di Sario
    Department of Gastroenterology, University of Ancona, Ancona, Italy
    J Hepatol 37:584-91. 2002
    ..Pirfenidone has been recently shown to reduce dimethynitrosamine-induced liver fibrosis in the rat, but no information are available on the effect of this drug on cultured hepatic stellate cells (HSC)...
  20. ncbi A novel anti-epileptic agent, perampanel, selectively inhibits AMPA receptor-mediated synaptic transmission in the hippocampus
    Laura Ceolin
    MRC Centre for Synaptic Plasticity, School of Physiology and Pharmacology, University of Bristol, Bristol BS8 1TD, United Kingdom
    Neurochem Int 61:517-22. 2012
    ..The concentrations of perampanel required to reduce AMPA receptor-mediated responses are not dissimilar to those in plasma following anti-convulsant doses and are consistent with AMPA receptor antagonism being its primary mode of action...
  21. ncbi A randomized controlled 1-year study of daily deferiprone plus twice weekly desferrioxamine compared with daily deferiprone monotherapy in patients with thalassemia major
    Yesim Aydinok
    Ege University, Faculty of Medicine, Department of Pediatric Hematology 35100 Bornova, Izmir, Turkey
    Haematologica 92:1599-606. 2007
    ..The aim of this prospective, randomized, 1-year study was to compare the efficacy and safety of oral deferiprone (DFP) with those of combinations of parenteral desferrioxamine (DFO) with oral DFP...
  22. pmc Pharmacokinetics of pirfenidone after topical administration in rabbit eye
    Guoying Sun
    State Key Laboratory of Ophthalmology, Zhongshan Ophthalmic Center, Sun Yat Sen University, Guangzhou, China
    Mol Vis 17:2191-6. 2011
    ..This study investigated the pharmacokinetics of topically administered pirfenidone (0.5%) in rabbit eyes...
  23. ncbi Evaluation of pirfenidone as a new postoperative antiscarring agent in experimental glaucoma surgery
    Hua Zhong
    State Key Laboratory of Ophthalmology, Zhongshan Ophthalmic Center, Sun Yat Sen University, Guangzhou, China
    Invest Ophthalmol Vis Sci 52:3136-42. 2011
    ..To investigate whether topical administration of pirfenidone eye drops could be used to prevent postoperative scarring in a rabbit model of experimental glaucoma filtration surgery...
  24. ncbi Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor
    Kan He
    Pharmaceutical Candidate Optimization, Bristol Myers Squibb Company, Princeton, NJ, USA
    Eur J Drug Metab Pharmacokinet 36:129-39. 2011
    ..3 μM for dog. Apixaban exhibits desirable PK and PD properties for clinical development with good oral bioavailability, small Vd, low CL, and direct, predictable, concentration-dependent PD responses...
  25. pmc Adjunctive perampanel for refractory partial-onset seizures: randomized phase III study 304
    Jacqueline A French
    NYU Comprehensive Epilepsy Center, New York, NY, USA
    Neurology 79:589-96. 2012
    ....
  26. ncbi Local delivery of biodegradable pirfenidone nanoparticles ameliorates bleomycin-induced pulmonary fibrosis in mice
    Ruchit Trivedi
    Department of Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus, Aurora, CO 80045, USA
    Nanotechnology 23:505101. 2012
    ..1% in the NP group and by 37.7% and 44.5%, respectively, in the solution group, compared to bleomycin alone.In conclusion, nanoparticles sustain lung pirfenidone delivery and enhance its anti-fibrotic efficacy...
  27. ncbi In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies
    Lifei Wang
    Pharmaceutical Candidate Optimization, Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543, USA
    Drug Metab Dispos 38:448-58. 2010
    ..Together with a low clinical efficacious concentration and multiple clearance pathways, these results demonstrate that the metabolic drug-drug interaction potential between apixaban and coadministered drugs is low...
  28. pmc Design and synthesis of C-2 substituted thiazolo and dihydrothiazolo ring-fused 2-pyridones: pilicides with increased antivirulence activity
    Erik Chorell
    Department of Chemistry, Umea University, SE 90187 Umea, Sweden
    J Med Chem 53:5690-5. 2010
    ..The structural basis of the PapD chaperone-pilicide interactions was determined by X-ray crystallography...
  29. ncbi Perampanel, a selective, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist, as adjunctive therapy for refractory partial-onset seizures: interim results from phase III, extension study 307
    Gregory L Krauss
    Johns Hopkins University, Baltimore, Maryland, USA
    Epilepsia 54:126-34. 2013
    ..To evaluate safety, tolerability, and seizure outcome data during long-term treatment with once-daily adjunctive perampanel (up to 12 mg/day) in patients with refractory partial-onset seizures...
  30. ncbi Evaluation of adjunctive perampanel in patients with refractory partial-onset seizures: results of randomized global phase III study 305
    Jacqueline A French
    NYU Comprehensive Epilepsy Center, New York, New York 10016, USA
    Epilepsia 54:117-25. 2013
    ..To assess the efficacy and safety of once-daily doses of perampanel 8 and 12 mg when added to 1-3 concomitantly administered, approved antiepileptic drugs (AEDs) in patients with uncontrolled partial-onset seizures...
  31. ncbi Roles of activated Src and Stat3 signaling in melanoma tumor cell growth
    Guilian Niu
    Immunology Program, H Lee Moffitt Cancer Center and Research Institute, Department of Oncology, University of South Florida College of Medicine, Tampa, Florida, FL 33612, USA
    Oncogene 21:7001-10. 2002
    ..These findings demonstrate that Src-activated Stat3 signaling is important for the growth and survival of melanoma tumor cells...
  32. ncbi Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial
    Jeffrey R Infante
    Sarah Cannon Research Institute Tennessee Oncology, PLLC, Nashville, TN, USA
    Lancet Oncol 13:773-81. 2012
    ..We aimed to define the maximum tolerated dose and recommended phase 2 dose of trametinib and to assess its safety, pharmacokinetics, pharmacodynamics, and response rate in individuals with advanced solid tumours...
  33. ncbi Biodegradation of chlorpyrifos and its hydrolysis product 3,5,6-trichloro-2-pyridinol by Bacillus pumilus strain C2A1
    Samina Anwar
    National Institute for Biotechnology and Genetic Engineering, Faisalabad, Pakistan
    J Hazard Mater 168:400-5. 2009
    ..The strain C2A1 showed 90% degradation of TCP (300 mg L(-1)) within 8 days of incubation...
  34. ncbi Site-specific incorporation of a photo-crosslinking component into RNA by T7 transcription mediated by unnatural base pairs
    Michiko Kimoto
    Protein Research Group, RIKEN Genomic Sciences Center, 1 7 22 Suehiro cho, Tsurumi ku, Yokohama, Kanagawa 230 0045, Japan
    Chem Biol 11:47-55. 2004
    ....
  35. ncbi A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
    Sarah K Knutson
    Epizyme, Inc, Cambridge, MA, USA
    Nat Chem Biol 8:890-6. 2012
    ....
  36. ncbi Pirfenidone suppresses tumor necrosis factor-alpha, enhances interleukin-10 and protects mice from endotoxic shock
    Hisashi Oku
    Department of Immunology, Shionogi Discovery Research Laboratories, Shionogi and Co, Ltd, 2 5 1, Mishima, Osaka 566 0022, Settsu, Japan
    Eur J Pharmacol 446:167-76. 2002
    ..These findings may offer an alternative for both protective and therapeutical treatment of several human acute or chronic inflammatory diseases by pirfenidone...
  37. pmc A biomarker validation study of prenatal chlorpyrifos exposure within an inner-city cohort during pregnancy
    Robin M Whyatt
    Columbia Center for Children s Environmental Health, Department of Environmental Health Sciences, Joseph L Mailman School of Public Health, Columbia University, New York, New York 10032, USA
    Environ Health Perspect 117:559-67. 2009
    ....
  38. ncbi Apixaban compared with warfarin in patients with atrial fibrillation and previous stroke or transient ischaemic attack: a subgroup analysis of the ARISTOTLE trial
    J Donald Easton
    Department of Neurology, University of California San Francisco, San Francisco, CA 94143 0114, USA
    Lancet Neurol 11:503-11. 2012
    ..We therefore aimed to assess the efficacy and safety of apixaban compared with warfarin in prespecified subgroups of patients with and without previous stroke or TIA...
  39. ncbi Apixaban for reduction in stroke and other ThromboemboLic events in atrial fibrillation (ARISTOTLE) trial: design and rationale
    Renato D Lopes
    Duke Clinical Research Institute, Duke University Medical Center, Durham, NC, USA
    Am Heart J 159:331-9. 2010
    ....
  40. ncbi Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer
    Qing Dong
    Takeda San Diego, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:1315-9. 2011
    ..Lead optimization of this series led to the discovery of TAK-733. This was advanced to Phase I clinical studies for cancer treatment...
  41. ncbi Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation fa
    Donald J P Pinto
    Discovery Chemistry, Research and Development, Bristol Myers Squibb Company, 31 Pennington Rocky Hill Road, Pennington, New Jersey 08534, USA
    J Med Chem 50:5339-56. 2007
    ..Compound 40 exhibits a high degree of fXa potency, selectivity, and efficacy and has an improved pharmacokinetic profile relative to 4...
  42. ncbi Apixaban, an oral, direct, selective factor Xa inhibitor, in combination with antiplatelet therapy after acute coronary syndrome: results of the Apixaban for Prevention of Acute Ischemic and Safety Events (APPRAISE) trial
    John H Alexander
    Duke Clinical Research Institute, Duke University Medical Center, DUMC Box 3850, Durham, NC 27715, USA
    Circulation 119:2877-85. 2009
    ..After an acute coronary syndrome, patients remain at risk of recurrent events. Apixaban, an oral direct factor Xa inhibitor, is a novel anticoagulant that may reduce these events but also poses a risk of bleeding...
  43. pmc The antitumor activity of the fungicide ciclopirox
    Hongyu Zhou
    Department of Biochemistry and Molecular Biology, Louisiana State University Health Sciences Center, Shreveport, LA 71130 3932, USA
    Int J Cancer 127:2467-77. 2010
    ..The results indicate that CPX is a potential antitumor agent...
  44. pmc Deferasirox, deferiprone and desferrioxamine treatment in thalassemia major patients: cardiac iron and function comparison determined by quantitative magnetic resonance imaging
    Alessia Pepe
    Magnetic Resonance Imaging Unit, Fondazione G Monasterio, C N R Regione Toscana, Pisa, Italy
    Haematologica 96:41-7. 2011
    ....
  45. ncbi In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists
    Gentaroh Suzuki
    Tsukuba Research Institute, Banyu Pharmaceutical Co, Ltd, 3 Okubo, Tsukuba, Ibaraki 300 2611, Japan
    J Pharmacol Exp Ther 323:147-56. 2007
    ..MMPIP is the first allosteric mGluR7-selective antagonist that could potentially be useful as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions...
  46. ncbi Pirfenidone protects endotoxin-induced liver injury after hepatic ischemia in rats
    M Kaibori
    Department of Surgery, Kansai Medical University, Osaka, Japan
    Transplant Proc 36:1973-4. 2004
    ..Pirfenidone (PFD), an experimental antifibrotic agent, was investigated for its effects on endotoxin-induced liver injury after hepatic ischemia-reperfusion...
  47. ncbi A metathesis-based approach to the synthesis of 2-pyridones and pyridines
    Timothy J Donohoe
    Department of Chemistry, Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford, OX1 3TA, United Kingdom
    Org Lett 10:285-8. 2008
    ..This mild and novel approach to six-membered heteroaromatic compounds then provides access to a wide variety of substituted pyridines in excellent overall yield...
  48. ncbi The antimycotic ciclopirox olamine induces HIF-1alpha stability, VEGF expression, and angiogenesis
    Tobias Linden
    Institute of Physiology, Medical University of Lubeck, Lubeck, Germany
    FASEB J 17:761-3. 2003
    ..In summary, these results suggest that CPX induces angiogenesis in vivo via HIF-1 and VEGF induction. Therefore, CPX might serve as an alternative to recombinant VEGF treatment or to VEGF gene therapy for therapeutic angiogenesis...
  49. pmc Antimycotic ciclopirox olamine in the diabetic environment promotes angiogenesis and enhances wound healing
    Sae Hee Ko
    Hagey Laboratory for Regenerative Medicine, Division of Plastic and Reconstructive Surgery, Department of Surgery, Stanford University School of Medicine, Stanford, California, United States of America
    PLoS ONE 6:e27844. 2011
    ..These findings offer a promising new topical pharmacologic therapy for the treatment of diabetic wounds...
  50. ncbi Acute management of bleeding in patients on novel oral anticoagulants
    Deborah M Siegal
    Division of Hematology and Thromboembolism, Department of Medicine, McMaster University, Hamilton, Ontario, Canada
    Eur Heart J 34:489-498b. 2013
    ..We provide an approach to the management of patients with bleeding complications with evidence for various interventions for reversal, where available...
  51. pmc Inhibition of HIV-1 gene expression by Ciclopirox and Deferiprone, drugs that prevent hypusination of eukaryotic initiation factor 5A
    Mainul Hoque
    Department of Biochemistry and Molecular Biology, UMDNJ New Jersey Medical School, NJ 07103, USA
    Retrovirology 6:90. 2009
    ..DOHH activity is inhibited by two clinically used drugs, the topical fungicide ciclopirox and the systemic medicinal iron chelator deferiprone. Deferiprone has been reported to inhibit HIV-1 replication in tissue culture...
  52. pmc Pirfenidone inhibits TGF-β1-induced over-expression of collagen type I and heat shock protein 47 in A549 cells
    Keiko Hisatomi
    Second Department of Internal Medicine, Nagasaki University School of Medicine, 1 7 1 Sakamoto, Nagasaki 852 8501, Japan
    BMC Pulm Med 12:24. 2012
    ..The present study evaluates the effects of pirfenidone on collagen type I and HSP47 expression in the human alveolar epithelial cell line, A549 cells in vitro...
  53. ncbi Pirfenidone: significant treatment effects in idiopathic pulmonary fibrosis
    Ole Hilberg
    Aarhus University Hospital, Respiratory Diseases and Allergology, Aarhus, Denmark
    Clin Respir J 6:131-43. 2012
    ..This review summarizes the background to the recommended use of pirfenidone for the treatment of IPF...
  54. ncbi Tolerability and safety of perampanel: two randomized dose-escalation studies
    G L Krauss
    Johns Hopkins Hospital, Baltimore, MD 21287, USA
    Acta Neurol Scand 125:8-15. 2012
    ..To evaluate, for the first time in patients with epilepsy, the tolerability and safety of escalating doses of oral perampanel, a novel, selective, non-competitive AMPA antagonist, as adjunctive therapy for refractory partial-onset seizures...
  55. ncbi Potent antimalarial 4-pyridones with improved physico-chemical properties
    José M Bueno
    Tres Cantos Medicines Development Campus, Diseases of the Developing World, GlaxoSmihKline, C Severo Ochoa, 2, 28760 Tres Cantos, Madrid, Spain
    Bioorg Med Chem Lett 21:5214-8. 2011
    Antimalarial 4-pyridones are a novel class of inhibitors of the plasmodial mitochondrial electron transport chain targeting Cytochrome bc1 (complex III)...
  56. ncbi Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development
    Mike Ufer
    Institute for Experimental and Clinical Pharmacology, University Hospital Schleswig Holstein, Kiel, Germany
    Thromb Haemost 103:572-85. 2010
    ..Hence, this review reports PK/PD, efficacy and safety data of dabigatran, rivaroxaban and apixaban throughout preclinical and clinical development...
  57. ncbi Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily
    Gretchen M Schroeder
    Bristol Myers Squibb Research and Development, Princeton, New Jersey, 08543 4000, USA
    J Med Chem 52:1251-4. 2009
    ..Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclinical safety profiles, 10 has been advanced into phase I clinical trials...
  58. ncbi C-Terminal properties are important for ring-fused 2-pyridones that interfere with the chaperone function in uropathogenic E. coli
    Veronica Aberg
    Organic Chemistry, Department of Chemistry, Umea University, SE 90187 Umea, Sweden
    Org Biomol Chem 3:3886-92. 2005
    ..Substituted bicyclic 2-pyridones, pilicides, inhibit pilus formation, possibly by interfering with the active site residues Arg8 and Lys112 of ..
  59. ncbi Effects of pirfenidone on proliferation, migration, and collagen contraction of human Tenon's fibroblasts in vitro
    Xianchai Lin
    State Key Laboratory of Ophthalmology, Zhongshan Ophthalmic Center, Sun Yat Sen University, Guangzhou, China
    Invest Ophthalmol Vis Sci 50:3763-70. 2009
    ..To investigate the effect of pirfenidone, a novel antifibrotic agent, on proliferation, migration, and collagen contraction of human Tenon's fibroblasts (HTFs)...
  60. ncbi Antifibrotic effect of Pirfenidone on orbital fibroblasts of patients with thyroid-associated ophthalmopathy by decreasing TIMP-1 and collagen levels
    Hyunmi Kim
    Department of Pharmacology, Ajou University School of Medicine, Suwon, Korea
    Invest Ophthalmol Vis Sci 51:3061-6. 2010
    ..The aim of this study was to determine the antifibrotic effects of pirfenidone in orbital fibroblasts of patients with thyroid-associated ophthalmopathy (TAO)...
  61. ncbi The antifungal drug ciclopirox inhibits deoxyhypusine and proline hydroxylation, endothelial cell growth and angiogenesis in vitro
    Paul M J Clement
    Oral and Pharyngeal Cancer Branch, National Institute of Dental and Craniofacial Research, National Institutes of Health, Bethesda, MD 20892, USA
    Int J Cancer 100:491-8. 2002
    ..The strong antiangiogenic activity of this readily available antifungal drug along with its antiproliferative effects suggests a new potential application for ciclopirox in the treatment of solid tumors...
  62. ncbi Intracellular labile iron pools as direct targets of iron chelators: a fluorescence study of chelator action in living cells
    Hava Glickstein
    Department of Biological Chemistry, Alexander Silberman Institute of Life Sciences, Hebrew University of Jerusalem, Safra Givat Ram Campus, Jerusalem 91904, Israel
    Blood 106:3242-50. 2005
    ....
  63. pmc Improved survival of thalassaemia major in the UK and relation to T2* cardiovascular magnetic resonance
    Bernadette Modell
    UCL Centre for Health Informatics and Multiprofessional Education, Holborn Union Building, Whittington Campus, Highgate Hill, London, N19 5LW, UK
    J Cardiovasc Magn Reson 10:42. 2008
    ..A study of survival and causes of death was undertaken which aimed to include the possible impact of T2* cardiovascular magnetic resonance (CMR)...
  64. ncbi Beyond unfractionated heparin and warfarin: current and future advances
    Jack Hirsh
    Henderson Research Centre, Hamilton Health Sciences Corporatin, Ontario, Canada
    Circulation 116:552-60. 2007
  65. ncbi Pirfenidone reduces in vitro rat renal fibroblast activation and mitogenesis
    T D Hewitson
    Department of Nephrology, The Royal Melbourne Hospital, Australia
    J Nephrol 14:453-60. 2001
    ..The objective of this study was therefore to determine if these effects include down-regulation of fibroblast function...
  66. pmc Ciclopirox olamine treatment affects the expression pattern of Candida albicans genes encoding virulence factors, iron metabolism proteins, and drug resistance factors
    Markus Niewerth
    Robert Koch Institut, 13353 Berlin, Germany
    Antimicrob Agents Chemother 47:1805-17. 2003
    ..Furthermore, neither the expression of certain multiple-drug resistance genes nor other resistance mechanisms caused C. albicans resistance to this drug even after long-term exposure...
  67. ncbi Favorable therapeutic index of the direct factor Xa inhibitors, apixaban and rivaroxaban, compared with the thrombin inhibitor dabigatran in rabbits
    P C Wong
    Thrombosis Research, Bristol Myers Squibb Company, Pennington, NJ 08534, USA
    J Thromb Haemost 7:1313-20. 2009
    ..This study assessed effects of the direct FXa inhibitors, apixaban and rivaroxaban, vs. the direct thrombin inhibitor, dabigatran, on venous thrombosis (VT), bleeding time (BT) and clotting times in rabbits...
  68. pmc Rationally designed small compounds inhibit pilus biogenesis in uropathogenic bacteria
    Jerome S Pinkner
    Department of Molecular Microbiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Proc Natl Acad Sci U S A 103:17897-902. 2006
    ..The activity of a family of bicyclic 2-pyridones, termed pilicides, was evaluated in two different pilus biogenesis systems in uropathogenic Escherichia coli...
  69. pmc Pirfenidone prevents the development of a vulnerable substrate for atrial fibrillation in a canine model of heart failure
    Ken W Lee
    Cardiac Electrophysiology and Cardiovascular Research Institute, University of California, San Francisco, San Francisco, CA, USA
    Circulation 114:1703-12. 2006
    ..This atrial remodeling is a potential therapeutic target. The objective of the present study is to evaluate the effects of the antifibrotic drug pirfenidone (PFD) on arrhythmogenic atrial remodeling in a canine CHF model...
  70. ncbi BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro
    Yao Dai
    Department of Radiation Oncology, University of Florida, Cancer Genetic Research Complex, Room 485E, Gainesville, Florida 32610, USA
    Mol Cancer Ther 9:1554-61. 2010
    ....
  71. ncbi Sulfation of o-demethyl apixaban: enzyme identification and species comparison
    Lifei Wang
    Pharmaceutical Candidate Optimization, Bristol Myers Squibb, P O Box 4000, Princeton, NJ 08543, USA
    Drug Metab Dispos 37:802-8. 2009
    ..The results indicated that liver S9 samples from dogs, monkeys, and humans had higher activities for formation of O-demethyl apixaban sulfate than those of mice, rats, and rabbits...
  72. ncbi Long-term sequential deferiprone-deferoxamine versus deferiprone alone for thalassaemia major patients: a randomized clinical trial
    Aurelio Maggio
    U O C Ematologia II con Talassemia, A O V Cervello, Palermo, Italy
    Br J Haematol 145:245-54. 2009
    ....
  73. ncbi Normalisation of total body iron load with very intensive combined chelation reverses cardiac and endocrine complications of thalassaemia major
    Kallistheni Farmaki
    Transfusion Department and Thalassaemia Unit, General Hospital of Corinth, Leoforos Athinon 53, Corinth 20100, Greece
    Br J Haematol 148:466-75. 2010
    ..These results suggest that intensive combined chelation normalized patients' iron load and thereby prevented and reversed cardiac and multiple endocrine complications associated with transfusion iron overload...
  74. ncbi Pirfenidone slows renal function decline in patients with focal segmental glomerulosclerosis
    Monique E Cho
    Kidney Disease Section, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892 1268, USA
    Clin J Am Soc Nephrol 2:906-13. 2007
    ..Our objective was to determine whether pirfenidone slows the loss of renal function in focal segmental glomerulosclerosis...
  75. ncbi Microwave-assisted decarboxylation of bicyclic 2-pyridone scaffolds and identification of Abeta-peptide aggregation inhibitors
    Veronica Aberg
    Organic Chemistry, Department of Chemistry, Umea University, SE 90187, Umea, Sweden
    Org Biomol Chem 3:2817-23. 2005
    A reagent-free microwave-assisted decarboxylation procedure for carboxylic acid functionalized bicyclic 2-pyridones has been developed...
  76. pmc Repeated pesticide exposure among North Carolina migrant and seasonal farmworkers
    Thomas A Arcury
    Department of Family and Community Medicine, Wake Forest University School of Medicine, Winston Salem, NC27157 1084, USA
    Am J Ind Med 53:802-13. 2010
    ..Limited data document the multiple and repeated pesticide absorption experienced by farmworkers in an agricultural season or their risk factors...
  77. ncbi Pirfenidone in idiopathic pulmonary fibrosis
    T M Maher
    Interstitial Lung Disease Unit, Royal Brompton Hospital, London, UK
    Drugs Today (Barc) 46:473-82. 2010
    ..These questions notwithstanding, pirfenidone represents an important development in the treatment of IPF and is a much needed addition to the previously inadequate therapeutic armamentarium for this devastating disease...
  78. ncbi Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase
    I Wayne Cheney
    Valeant Pharmaceuticals Research and Development, 3300 Hyland Avenue, Costa Mesa, CA 92626, USA
    Bioorg Med Chem Lett 17:1679-83. 2007
    ....
  79. ncbi Design, synthesis and evaluation of peptidomimetics based on substituted bicyclic 2-pyridones-targeting virulence of uropathogenic E. coli
    Veronica Berg
    Organic Chemistry, Department of Chemistry, Umea University, SE 90187 Umea, Sweden
    Bioorg Med Chem 14:7563-81. 2006
    Substituted bicyclic 2-pyridones, termed pilicides, are dipeptide mimetics that prevent pilus assembly in uropathogenic Escherichia coli...
  80. ncbi Pirfenidone diminishes cyclophosphamide-induced lung fibrosis in mice
    J P Kehrer
    Division of Pharmacology Toxicology, College of Pharmacy, University of Texas at Austin, 78712 1074, USA
    Toxicol Lett 90:125-32. 1997
    ..Overall, these data support an antifibrotic effect of pirfenidone against CP-induced lung fibrosis in mice. The mechanism of its effect is not known, but appears to be unrelated to an inhibition of collagen synthesis...
  81. ncbi The anti-fibrotic effect of pirfenidone in rat liver fibrosis is mediated by downregulation of procollagen alpha1(I), TIMP-1 and MMP-2
    A Di Sario
    Gastrointestinal Unit, University of Ancona, Polo Didattico, III piano, Via Tronto 10, 60020 Torrette, Ancona, Italy
    Dig Liver Dis 36:744-51. 2004
    ....
  82. ncbi Improving survival with deferiprone treatment in patients with thalassemia major: a prospective multicenter randomised clinical trial under the auspices of the Italian Society for Thalassemia and Hemoglobinopathies
    Aurelio Maggio
    U O C Ematologia II con Talassemia, A O V Cervello, Palermo, Italy
    Blood Cells Mol Dis 42:247-51. 2009
    ..013). In conclusion, the results of this study show that the risk factors for predicting mortality in patients with thalassemia major are deferoxamine-treatment, complications, and the interaction effect of sex and age...
  83. ncbi Single- and multiple-dose pharmacokinetics of pirfenidone, an antifibrotic agent, in healthy Chinese volunteers
    Shaojun Shi
    Department of Pharmacy of Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Shanghai, China
    J Clin Pharmacol 47:1268-76. 2007
    ..Concomitant intake of food will reduce the rate and extent (about 20%) of absorption, which is associated with better tolerability of pirfenidone...
  84. ncbi The possible mechanism of action of ciclopirox olamine in the yeast Saccharomyces cerevisiae
    Sun Hee Leem
    Department of Biology, Dong A University, Busan 604 714, Korea
    Mol Cells 15:55-61. 2003
    ..These results suggest that CPO inhibits multiple aspects of cell growth and metabolism, possibly via multiple targets...
  85. ncbi Pirfenidone effectively reverses experimental liver fibrosis
    Leonel Garcia
    Institute for Molecular Biology in Medicine and Gene Therapy, CUCS, University of Guadalajara, Apdo Postal 2 123, Guadalajara, Jal 44281, Mexico
    J Hepatol 37:797-805. 2002
    ..The aim of this study was to evaluate the effect of Pirfenidone in the reversion or prevention of cirrhosis experimentally induced in rats by chronic administration of CCl(4) and bile-duct ligation (BDL)...
  86. ncbi 6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors
    Karen Coffman
    Pfizer Global Research and Development, Groton Laboratories, Groton, CT 06340, USA
    Bioorg Med Chem Lett 21:1429-33. 2011
    The synthesis and structure-activity relationships for a novel series of 6-amino-4-(pyrimidin-4-yl)pyridones derived from a high throughput screening hit are discussed...
  87. ncbi Synthesis of substituted N-benzyl pyridones via an O- to N-alkyl migration
    Erica L Lanni
    Department of Chemistry, Pomona College, 645 North College Avenue, Claremont, California 91711, USA
    J Org Chem 73:6425-8. 2008
    ..This method serves as an efficient means for the preparation of N-benzyl pyridones, quinolones, and pyrimidones.
  88. ncbi Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation
    Yao Dai
    Department of Radiation Oncology, University of Florida, Gainesville, FL 32610, USA
    Clin Exp Metastasis 29:253-61. 2012
    ..Together, the present findings demonstrate that the disruption of c-Met signaling by BMS-777607 significantly impairs the metastatic phenotype, suggesting that this agent may have therapeutic utility in targeting cancer metastasis...
  89. pmc Antiproliferative and apoptosis inducing properties of pyrano[3,2-c]pyridones accessible by a one-step multicomponent synthesis
    Igor V Magedov
    Department of Organic Chemistry, Timiryazev Agriculture Academy, Moscow 127550, Russia
    Bioorg Med Chem Lett 17:3872-6. 2007
    4-Arylpyrano-[3,2-c]-pyridones have been prepared by a one-step cyclocondensation of 4-hydroxy-1,6-dimethylpyridin-2(1H)-one with various substituted benzaldehydes and malononitrile...
  90. ncbi Combined chelation therapy in thalassemia major with deferiprone and desferrioxamine: a retrospective study
    Paolo Ricchi
    Dipartimento di Oncoematologia, UOC Centro delle Microcitemie A Mastrobuoni, AORN A Cardarelli, Naples, Italy
    Eur J Haematol 85:36-42. 2010
    ..We retrospectively evaluated the efficacy of different schedules of combined chelation therapy and the incidence of adverse events...
  91. ncbi Pirfenidone inhibits the expression of HSP47 in TGF-beta1-stimulated human lung fibroblasts
    Seiko Nakayama
    Second Department of Internal Medicine, Nagasaki University School of Medicine, Nagasaki, Japan
    Life Sci 82:210-7. 2008
    ....
  92. ncbi Effective combination therapy of deferiprone and deferoxamine for the rapid clearance of excess cardiac IRON and the prevention of heart disease in thalassemia. The Protocol of the International Committee on Oral Chelators
    Annita Kolnagou
    Postgraduate Research Institute of Science, Technology, Environment and Medicine, Limassol, Cyprus
    Hemoglobin 30:239-49. 2006
    ..The ICOC combination therapy protocol appears to be the most effective and least cumbersome form of chelation treatment for the rapid clearance of excess iron from the heart...
  93. ncbi Regioselective halogenations and subsequent Suzuki-Miyaura coupling onto bicyclic 2-pyridones
    Christoffer Bengtsson
    Department of Chemistry, Umea University, SE 901 80 Umea, Sweden
    J Org Chem 75:972-5. 2010
    A selective synthesis of 6-bromo-8-iodo dihydro thiazolo ring-fused 2-pyridones is described. These halogenated 2-pyridones are selectively arylated by sequential Suzuki-Miyaura couplings...
  94. pmc Carboxylic acid isosteres improve the activity of ring-fused 2-pyridones that inhibit pilus biogenesis in E. coli
    Veronica Berg
    Department of Chemistry, Umea University, SE 90187 Umea, Sweden
    Bioorg Med Chem Lett 18:3536-40. 2008
    Ring-fused 2-pyridones, termed pilicides, are small synthetic compounds that inhibit pilus assembly in uropathogenic Escherichia coli. Their biological activity is clearly dependent upon a carboxylic acid functionality...
  95. pmc Pirfenidone for the treatment of Hermansky-Pudlak syndrome pulmonary fibrosis
    Kevin O'Brien
    Office of the Clinical Director, National Human Genome Research Institute, NIH, Bethesda, MD 20892, USA
    Mol Genet Metab 103:128-34. 2011
    ..There were no significant safety concerns. Other clinical trials are indicated to identify single or multiple drug regimens that may be effective in treatment for progressive HPS-1 pulmonary fibrosis...
  96. ncbi Reduction of body iron stores to normal range levels in thalassaemia by using a deferiprone/deferoxamine combination and their maintenance thereafter by deferiprone monotherapy
    Annita Kolnagou
    Postgraduate Research Institute of Science, Technology, Environment and Medicine, Limassol, Cyprus
    Eur J Haematol 85:430-8. 2010
    ..New chelating drug protocols are necessary to treat completely transfusional iron overload and eliminate associated toxicity. Appropriate deferiprone/deferoxamine combinations could achieve this goal...
  97. pmc Combined chelation therapy in thalassemia major for the treatment of severe myocardial siderosis with left ventricular dysfunction
    Mark A Tanner
    Cardiovascular Magnetic Resonance Unit, Royal Brompton Hospital, London, UK
    J Cardiovasc Magn Reson 10:12. 2008
    ..Combined chelation therapy with deferiprone and deferoxamine is effective for moderate myocardial siderosis, but has not been prospectively examined in severe myocardial siderosis...
  98. ncbi Effects on fibrin network porosity of anticoagulants with different modes of action and reversal by activated coagulation factor concentrate
    Margareta Blomback
    Department of Molecular Medicine and Surgery Coagulation Research, Karolinska Institutet, Stockholm AstraZeneca R and D, Molndal, Sweden
    Br J Haematol 152:758-65. 2011
    ..In conclusion, all examined anticoagulants rendered the fibrin network more porous. FEIBA(®) reversed the increased permeability in warfarin plasma but had only partial effects on the other anticoagulants...
  99. ncbi Exposures of preschool children to chlorpyrifos and its degradation product 3,5,6-trichloro-2-pyridinol in their everyday environments
    Marsha K Morgan
    National Exposure Research Laboratory, USEPA, Research Triangle Park, NC 27711, USA
    J Expo Anal Environ Epidemiol 15:297-309. 2005
    ..In conclusion, the results showed that the preschool children were exposed to chlorpyrifos and TCP from several sources, through several pathways and routes. ...
  100. ncbi Synthesis studies toward chloroazaphilone and vinylogous gamma-pyridones: two common natural product core structures
    Wan Guo Wei
    State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, China
    J Org Chem 70:4585-90. 2005
    ..Reaction of this chloroazaphilone with various primary amines to afford the corresponding vinylogous gamma-pyridones was also fully investigated...
  101. ncbi Chlorpyrifos exposure in farm families: results from the farm family exposure study
    Bruce H Alexander
    Division of Environmental Health Sciences, School of Public Health, University of Minnesota, Minneapolis, Minnesota 55455, USA
    J Expo Sci Environ Epidemiol 16:447-56. 2006
    ..Chlorpyrifos exposure to farm family members from the observed application was largely determined by the extent of contact with the mixing, loading, and application process...

Research Grants64

  1. Indoleamine 2,3-dioxygenase protective role in lung transplantation
    Gary A Visner; Fiscal Year: 2010
    ....
  2. Mechanism of Slow Onset Enzyme Inhibition and Drug Target Residence Time
    Peter J Tonge; Fiscal Year: 2013
    ..while both enzymes are inhibited by the diphenyl ether compound class, and a second related series based on pyridones, through the same two-step slow-onset induced-fit kinetic mechanism, the structural changes that accompany ..
  3. ASYMMETRIC SYNTHESIS OF PHYSIOLOGICALLY ACTIVE COMPOUNDS
    Gary Posner; Fiscal Year: 1992
    ..of asymmetric inverse-electron-demand Diels-Alder cycloadditions between electron-deficient pyrones and pyridones and electron-rich dienophiles...
  4. Transition Metal Mediated Routes to Heterocycles and Carbocycles
    Janis Louie; Fiscal Year: 2009
    ..catalysts for mediating carbon dioxide/diyne and isocyanate/diyne annulations to produce 2-pyrones and 2-pyridones, respectively...
  5. SYNTHESIS AND SYNTHETIC UTILITY OF 1-ACYLDIHYDROPYRIDINE
    DANIEL COMINS; Fiscal Year: 2004
    ..studying the asymmetric synthesis and reactions of 1-acyl-2-alkyl 1,2-dihydropyridines and 2,3-dihydro-4-pyridones. 2 .To complete the enantioselective total syntheses of streptazolin, cannabisativine and allopumiliotoxin. 3 ...
  6. CARDIOPROTECTIVE EFFECT--NEW CHELATORS FOR THALASSEMIA
    Chaim Hershko; Fiscal Year: 2001
    ..abstract_text> ..
  7. Free Iron, Estrogen and Postmenopausal Osteoporosis
    Gang Liu; Fiscal Year: 2002
    ..Moreover, this new approach will permit the reevaluation of the role of estrogen and will expedite the development of novel pharmaceutical agents for the prevention or treatment of osteoporosis. ..
  8. Nanoparticle Brain Delivery of Iron Chelators for AD
    Gang Liu; Fiscal Year: 2004
    ..Overall, this: exploratory: study may open the door for the use of iron chelator nanoparticle systems to target diseased organs for iron chelation therapy. ..
  9. INNOVATIVE BIOMONITORING FOR LEAD IN SALIVA
    Charles Timchalk; Fiscal Year: 2006
    ..It is reasonable to speculate that once this model system has been adequately validated it can readily be employed to screen sensitive populations (e.g. children) that are at greatest risk from chronic Pb exposure. ..
  10. Mixture Modeling: Pesticide Drug Interactions
    Charles Timchalk; Fiscal Year: 2009
    ..It is fully anticipated that this approach will facilitate the understanding of a variety of complex chemical interactions as it relates to the occupational health implications of working with insecticides. ..
  11. Development of Selective Nanoporous Sorbents for Radionuclide Decorporation
    Charles Timchalk; Fiscal Year: 2008
    ..abstract_text> ..
  12. ERYTHROCYTAPHERESIS TO LOWER IRON LOADING IN THALASSEMIA
    Alan Cohen; Fiscal Year: 2002
    ....
  13. MODELING OF MIXED LIGAND THERAPY FOR IRON OVERLOAD
    Robert Hider; Fiscal Year: 2002
    ..We aim to define the principles and potential candidates for optimal mixed ligand therapy for iron overload. ..
  14. Chemistry to Improve Human Genomic Array Analysis Architectures
    Steven A Benner; Fiscal Year: 2010
    ..This proposal seeks funds to benchmark the improvements in array performance generated by these new technologies, improve them by a cycle of test and redesign, and provide them to the genomics community. ..
  15. Artificial Genetic Systems
    Steven A Benner; Fiscal Year: 2010
    ..Multiplexed PCR is the rate limiting step in many genomics analyses. Our long term, highly ambitious goal is to develop a "synthetic biology", a chemical system capable of Darwinian evolution, based on AEGIS components. ..
  16. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2006
    ..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
  17. DNA Sequencing using Nanopores
    Steven Benner; Fiscal Year: 2007
    ..These will then be targeted against specific sequences extracted from mammalian genomes. [unreadable] [unreadable]..
  18. DISRUPTION OF PDGF SIGNAL TRANSDUCTION IN LUNG FIBROSIS
    Joseph Lasky; Fiscal Year: 2006
    ..abstract_text> ..
  19. Dynamic combinatorial chemistry for nucleic acids
    Steven Benner; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  20. Polymerases for Sequencing by Synthesis
    Steven Benner; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  21. Novel Antifungal Strategies for Lethal Mucormycosis
    Ashraf Ibrahim; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  22. Role of EBV gene products in lung fibrogenesis
    Joseph Lasky; Fiscal Year: 2009
    ..There are currently no proven medicinal therapies for the treatment of IPF. Defining the mechanisms through which EBV gene products promote IPF will provide new options for the treatment of this fatal disease. ..
  23. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 2009
    ..Daphnicyclidin A. This recent discovery has revealed a new molecular architecture which exhibits significant antitumor activity. Our research will investigate strategies for chemical synthesis of these complex polycyclic systems. ..
  24. Near Term Development of Reagents and Enzymes for Genome Sequencing
    Steven A Benner; Fiscal Year: 2010
    ..This proposal, from a laboratory with a track record of innovation in structures, reagents, and enzymes to manipulate nucleic acids, is focused on near term development of these to enable NHGRI cost-reduction sequencing goals. ..
  25. Targeted Assisted Combinational Synthesis
    Steven Benner; Fiscal Year: 2004
    ..abstract_text> ..
  26. Viral Protein Mediators of HIV-Related Pulmonary Hypertension
    Joseph Lasky; Fiscal Year: 2009
    ....
  27. Treatment of Fungal Infections with ATAK Cells
    Ashraf Ibrahim; Fiscal Year: 2004
    ..Furthermore, the genetic construct targeting ATAK cells to Candida can easily be adapted to any other pathogen against which a MAb has been raised. ..
  28. CTGF IN LUNG FIBROGENESIS
    Joseph Lasky; Fiscal Year: 2004
    ..These studies will establish the role that CTGF plays in lung fibrogenesis. ..
  29. NON-STANDARD BASE PAIRS AS BIOMEDICAL RESEARCH TOOLS
    Steven Benner; Fiscal Year: 2004
    ....
  30. Role of reactive oxygen species in synaptic transmission
    Michael Levy; Fiscal Year: 2002
    ..In addition to characterizing the VDAC knockout mouse, I will determine the downstream effectors involved in ROS signaling during synaptic transmission. ..
  31. EVOLUTION OF THE RIBONUCLEASE SUPERFAMILY
    Steven Benner; Fiscal Year: 2001
    ....
  32. Mechanism of Action of Novel Dual Actiing Pyrimidinediones
    Robert Buckheit; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  33. Biomimetic Lanthanide & Actinide Decorporation Agents: Preclinical Development
    Kenneth Raymond; Fiscal Year: 2008
    ..abstract_text> ..
  34. OU Human Research Protection Program, Year 2
    Gary Raskob; Fiscal Year: 2003
    ..The University of Oklahoma is committed to maintaining these initiatives after the term of this award. ..
  35. SYNTHESIS OF CANNABINOIDS, ANALOGUES AND METABOLITES
    John Huffman; Fiscal Year: 2009
    ..There a possibility that these metabolites may be contributing to the enhanced potency of cannabinoids with a dimethylheptyl side chain. ..
  36. Farmwoker Environmental Health Research Comparable Data
    Thomas Arcury; Fiscal Year: 2004
    ..The purpose of limiting the size of the conference is to facilitate active interaction, discussion and debate among leaders in the field. ..
  37. Pathophysiology of thiamine-responsive anemia syndrome
    Ellis Neufeld; Fiscal Year: 2006
    ....
  38. PATHOGENESIS OF HEPATIC FIBROSIS AND PORTAL HYPERTENSION
    Don C Rockey; Fiscal Year: 2010
    ..These studies have direct relevance to human liver disease and will lead to new approaches for the treatment of hepatic fibrosis and portal hypertension as well as other forms of fibrosing injury. ..
  39. Passive PAH and Micro-Camera Personal Monitoring System
    Paul Lioy; Fiscal Year: 2003
    ....
  40. Nanoparticle Brain Delivery of Iron Chelators for AD
    Gang Liu; Fiscal Year: 2010
    ..Moreover, this approach may be applied to other neurodegenerative diseases mediated by excess metals, and to neuro-imaging. ..
  41. Ethnic Variation in CAM Use and Health Self Management among Rural Older Adults
    Thomas Arcury; Fiscal Year: 2009
    ....
  42. Estrogen and the Aging Blood Brain Barrier
    OAK CHI; Fiscal Year: 2002
    ..The information obtained from our study will be crucially important for the clinical application of estrogen therapy for stroke as well as understanding the pathophysiology of age related cerebrovascular changes. ..
  43. Community-Based Participatory Approach to Farmworker Housing, Exposures & Health
    Thomas A Arcury; Fiscal Year: 2010
    ....
  44. SYNTHESIS OF BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    BARRY SNIDER; Fiscal Year: 2009
    ..In the course of these studies new methods will be developed that are of general utility for preparing drugs more economically. ..
  45. Mechanism of pirfenidone-induced lung transplant survival
    Gary Visner; Fiscal Year: 2008
    ..This proposal will further evaluate its potential in promoting long term survival of lung transplants and the mechanisms of its protective effects. [unreadable] [unreadable] [unreadable]..
  46. MECHANISMS OF RENAL TUBULAR EPITHELIAL CELL INJURY
    Sudhir Shah; Fiscal Year: 2005
    ..abstract_text> ..
  47. Syntheses of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2005
    ..Targets include cyclic, unsaturated, and, beta substituted derivatives (beta amino, beta hydroxy, and beta fluoro). ..
  48. Differences in CAM Use Among Minority Older Adults
    Thomas Arcury; Fiscal Year: 2005
    ..abstract_text> ..
  49. African American Men Prostate & Colorectal Cancer Belief
    Thomas Arcury; Fiscal Year: 2007
    ..A preliminary framework of the intervention strategy for this R01 application will be developed and evaluated as part of this project. [unreadable] [unreadable]..
  50. Maternal Phthalate Exposure and Infertility, Fetal Loss
    Russ Hauser; Fiscal Year: 2007
    ..Since occupational and environmental exposure to phthalates is widespread, detecting even small adverse effects will have large public health significance. ..
  51. Prenatal Insecticide Exposures Among Urban Minorities
    Robin Whyatt; Fiscal Year: 2005
    ..The research will provide important information about pesticide exposure during pregnancy among this minority cohort. ..
  52. Chronic Thromboembolic Pulmonary Hypertension
    TIMOTHY MORRIS; Fiscal Year: 2006
    ..The fragments will be subjected to liquid chromatography-mass spectroscopy with data-dependent MS-2 data acquisition, followed by computer-assisted sequence analysis. ..
  53. Cardiac Function and Cardiac iron (T2*) in Thalassemia
    John Wood; Fiscal Year: 2007
    ..These studies will provide the necessary groundwork for longitudinal studies of cardiac iron load on cardiac performance in thalassemia patients. ..
  54. Survivin Regulation of Pulmonary Fibrosis
    Paul Noble; Fiscal Year: 2006
    ..2. Determine the role of survivin in vivo in the initiation and progression of experimental pulmonary fibrosis. 3. Determine the role of survivin in regulating the IPF fibroblast phenotype in vitro. ..
  55. KIDNEY RESPONSE TO RADIATION AND CHEMOTHERAPY
    JOHN MOULDER; Fiscal Year: 2006
    ..unreadable] 4) Complete the randomized, prospective, trial of the use of ACE inhibitors to prevent the development of radiation nephropathy in BMT patients. [unreadable] [unreadable]..
  56. Synthesis of Cannabinoid Receptor Ligands
    John Huffman; Fiscal Year: 2005
    ..A number of new classical cannabinoids will be synthesized, including additional 1',2'-dimethylheptyl-delta8-tetrahydrocannabinol analogues and the six geminally disubstituted dimethylheptyl-delta8-tetrahydrocannabinols. ..
  57. Validation of biomarkers of prenatal pesticides exposure
    Robin Whyatt; Fiscal Year: 2003
    ....
  58. Development of Pyrimidinedione HIV Inhibitors as Topical Microbicides
    Robert Buckheit; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  59. NEW DEVELOPMENTS IN ORGANOCOPPER CHEMISTRY
    R Dieter; Fiscal Year: 2004
    ..The proposed synthetic routes to pyrrolidine aza sugars will develop the potential synthetic power of alpha-aminoalkylcuprate chemistry. ..
  60. Nitric Oxide and the Liver
    Don Rockey; Fiscal Year: 2003
    ..The dates of the entire AASLD scientific meeting are November 3rd to November 5th. The participants will be invited speakers and attendees of the annual 2002 AASLD meeting. ..
  61. Asymmetric Synthesis of Amino Acids and Amino Phosphonic Acids
    FRANKLIN DAVIS; Fiscal Year: 2007
    ..The photodesulfmylation of sulfinamides represents an important new protocol, not requiring acids or bases, for the removal of the valuable amine N-sulfinyl protecting group. ..
  62. ASYMMETRIC SYNTHESIS OF BIOACTIVE PRIMARY AMINES
    FRANKLIN DAVIS; Fiscal Year: 2006
    ....