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Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.
Duplantier AJ, Dombroski MA, Subramanyam C, Beaulieu AM, Chang SP, Gabel CA, Jordan C, Kalgutkar AS, Kraus KG, Labasi JM, Mussari C, Perregaux DG, Shepard R, Taylor TJ, Trevena KA, Whitney-Pickett C, Yoon K. Duplantier AJ, et al. Among authors: kalgutkar as. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3708-11. doi: 10.1016/j.bmcl.2011.04.077. Epub 2011 Apr 24. Bioorg Med Chem Lett. 2011. PMID: 21565499
Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.
McClure KF, Letavic MA, Kalgutkar AS, Gabel CA, Audoly L, Barberia JT, Braganza JF, Carter D, Carty TJ, Cortina SR, Dombroski MA, Donahue KM, Elliott NC, Gibbons CP, Jordan CK, Kuperman AV, Labasi JM, Laliberte RE, McCoy JM, Naiman BM, Nelson KL, Nguyen HT, Peese KM, Sweeney FJ, Taylor TJ, Trebino CE, Abramov YA, Laird ER, Volberg WA, Zhou J, Bach J, Lombardo F. McClure KF, et al. Among authors: kalgutkar as. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4339-44. doi: 10.1016/j.bmcl.2006.05.056. Epub 2006 Jun 12. Bioorg Med Chem Lett. 2006. PMID: 16759861
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.
Wishka DG, Walker DP, Yates KM, Reitz SC, Jia S, Myers JK, Olson KL, Jacobsen EJ, Wolfe ML, Groppi VE, Hanchar AJ, Thornburgh BA, Cortes-Burgos LA, Wong EH, Staton BA, Raub TJ, Higdon NR, Wall TM, Hurst RS, Walters RR, Hoffmann WE, Hajos M, Franklin S, Carey G, Gold LH, Cook KK, Sands SB, Zhao SX, Soglia JR, Kalgutkar AS, Arneric SP, Rogers BN. Wishka DG, et al. Among authors: kalgutkar as. J Med Chem. 2006 Jul 13;49(14):4425-36. doi: 10.1021/jm0602413. J Med Chem. 2006. PMID: 16821801
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 microsomes.
Kalgutkar AS, Hatch HL, Kosea F, Nguyen HT, Choo EF, McClure KF, Taylor TJ, Henne KR, Kuperman AV, Dombroski MA, Letavic MA. Kalgutkar AS, et al. Biopharm Drug Dispos. 2006 Nov;27(8):371-86. doi: 10.1002/bdd.520. Biopharm Drug Dispos. 2006. PMID: 16944451
174 results