Kim F McClure

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. ncbi request reprint Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Global Research and Development, Groton, CT 06340, USA
    Drug Metab Dispos 35:848-58. 2007
  2. doi request reprint Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition
    Kevin D Jerome
    Pfizer Global Research and Development, St Louis Laboratories, 700 Chesterfield Pkwy W, Chesterfield, MO 63017, USA
    Bioorg Med Chem Lett 20:469-73. 2010
  3. doi request reprint Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor
    Kim F McClure
    Departments of Medicinal Chemistry, Discovery Biology, Drug Metabolism and Pharmaceutical Sciences, Pfizer Worldwide Research and Development, Groton, CT 06340, United States
    Bioorg Med Chem Lett 23:5410-4. 2013
  4. doi request reprint Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response
    Kim F McClure
    Department of Medicinal Chemistry, Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States
    J Med Chem 54:1948-52. 2011
  5. ncbi request reprint Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase
    Kim F McClure
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, USA
    J Med Chem 48:5728-37. 2005
  6. ncbi request reprint Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development
    Kim F McClure
    Pfizer Global Research and Development, Groton Laboratories, CT 06340, USA
    Bioorg Med Chem Lett 16:4339-44. 2006
  7. ncbi request reprint Benzimidazolone p38 inhibitors
    Mark A Dombroski
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 14:919-23. 2004
  8. doi request reprint Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119
    Etzer Darout
    Departments of Medicinal Chemistry, Discovery Biology, Drug Metabolism, and Pharmaceutical Sciences, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, Connecticut 06340, USA
    J Med Chem 56:301-19. 2013
  9. ncbi request reprint Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors
    Michael A Letavic
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 12:1387-90. 2002
  10. doi request reprint Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists
    Amit S Kalgutkar
    Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 19:1559-63. 2009

Collaborators

Detail Information

Publications19

  1. ncbi request reprint Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Global Research and Development, Groton, CT 06340, USA
    Drug Metab Dispos 35:848-58. 2007
    ..The metabolism studies described herein provide a mechanistic basis for the mutagenicity of 3...
  2. doi request reprint Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition
    Kevin D Jerome
    Pfizer Global Research and Development, St Louis Laboratories, 700 Chesterfield Pkwy W, Chesterfield, MO 63017, USA
    Bioorg Med Chem Lett 20:469-73. 2010
    ..X-ray of the ethylene linked compound 61 confirmed the predicted binding orientation of the scaffold in the p38 enzyme...
  3. doi request reprint Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor
    Kim F McClure
    Departments of Medicinal Chemistry, Discovery Biology, Drug Metabolism and Pharmaceutical Sciences, Pfizer Worldwide Research and Development, Groton, CT 06340, United States
    Bioorg Med Chem Lett 23:5410-4. 2013
    ..Specifically, heteroaryl rings with nitrogen(s) vicinal to the indane linkage provided the most attractive overall properties. ..
  4. doi request reprint Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response
    Kim F McClure
    Department of Medicinal Chemistry, Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States
    J Med Chem 54:1948-52. 2011
    ..We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology...
  5. ncbi request reprint Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase
    Kim F McClure
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, USA
    J Med Chem 48:5728-37. 2005
    ..The computed descriptors for the hydrophobic and pi-pi interaction capacities were the most useful in ranking potency...
  6. ncbi request reprint Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development
    Kim F McClure
    Pfizer Global Research and Development, Groton Laboratories, CT 06340, USA
    Bioorg Med Chem Lett 16:4339-44. 2006
    ..The deficiencies of the lead structure in the series, CP-808844, were overcome by changes to the C4 aryl group and the triazole side-chain culminating in the identification of several potential clinical candidates...
  7. ncbi request reprint Benzimidazolone p38 inhibitors
    Mark A Dombroski
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 14:919-23. 2004
    ..Potent p38 alpha activity comparable to that of several previously reported p38 inhibitors is observed for this novel chemotype...
  8. doi request reprint Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119
    Etzer Darout
    Departments of Medicinal Chemistry, Discovery Biology, Drug Metabolism, and Pharmaceutical Sciences, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, Connecticut 06340, USA
    J Med Chem 56:301-19. 2013
    ..Ultimately, solubility limited absorption and poor exposure reduced further interest in these molecules...
  9. ncbi request reprint Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors
    Michael A Letavic
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 12:1387-90. 2002
    ..Alkyl substituents on the ortho position of the benzyl ether moiety give the most potent inhibition of TNF-alpha release in LPS-treated human whole blood...
  10. doi request reprint Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists
    Amit S Kalgutkar
    Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 19:1559-63. 2009
    ..Plausible hypotheses that can collectively account for the differences in mutagenic response of the two piperazine analogs are discussed...
  11. doi request reprint Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor
    Vincent Mascitti
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Bioorg Med Chem Lett 21:1306-9. 2011
    ..The chemical stability and bioactivation potential are discussed...
  12. doi request reprint Enantioselective hydroarylation of bridged [3.2.1] heterocycles: an efficient entry into the homoepibatidine skeleton
    Ryan A Brawn
    CVMED Chemistry, Pfizer Worldwide Research and Development, 445 Eastern Point Road, Groton, Connecticut 06340, USA
    Org Lett 15:3424-7. 2013
    ..The phosphine ligand structure and the protecting group on the nitrogen both have significant effects on the selectivity and yield of the reactions. ..
  13. doi request reprint From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor
    Kentaro Futatsugi
    Pfizer Worldwide Research and Development, Groton Laboratories, Eastern Point Rd, Groton, CT 06340, United States
    Bioorg Med Chem Lett 23:194-7. 2013
    ..The design is centered on the conformational restriction of the core scaffold, while minimizing the change in spatial relationships of two key pharmacophoric elements (piperidine-carbamate and aryl sulfone)...
  14. ncbi request reprint Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38alpha inhibitor: identification of an active metabolite in preclinical species and human liver micro
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics and Metabolism Department, Pfizer Global Research and Development, Groton, CT 06340, USA
    Biopharm Drug Dispos 27:371-86. 2006
    ....
  15. doi request reprint Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma
    Raman Sharma
    Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, USA
    Chem Res Toxicol 24:2207-16. 2011
    ..To the best of our knowledge, our studies constitute the first report on the involvement of rodent XO in oxidative drug metabolism in plasma...
  16. doi request reprint Intrinsic electrophilicity of a 4-substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine derivative: structural characterization of glutathione conjugates in vitro
    Amit S Kalgutkar
    Pharmacokinetics, Dynamics, and Metabolism Department, Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States
    Chem Res Toxicol 24:269-78. 2011
    ....
  17. ncbi request reprint Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1
    Lawrence A Reiter
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 14:3389-95. 2004
    ..Despite the sparing of MMP-1, pre-clinical and clinical studies revealed that fibrosis in rats and MSS in humans is still produced...
  18. ncbi request reprint An efficient synthesis of bridged heterocycles from an Ir(I) bis-amination/ring-closing metathesis sequence
    Ryan A Brawn
    CVMED Chemistry, Pfizer Worldwide Research and Development, 445 Eastern Point Road, Groton, Connecticut 06340, USA
    Org Lett 14:4802-5. 2012
    ..Exposure of the heterocycles to ring-closing metathesis catalysts leads to the desired bridged heterocyclic systems...
  19. doi request reprint Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor
    Daniel W Kung
    Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 22:4281-7. 2012
    ....