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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
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
Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation.
Kalgutkar AS, Dalvie DK, Aubrecht J, Smith EB, Coffing SL, Cheung JR, Vage C, Lame ME, Chiang P, McClure KF, Maurer TS, Coelho RV Jr, Soliman VF, Schildknegt K. Kalgutkar AS, et al. Drug Metab Dispos. 2007 Jun;35(6):848-58. doi: 10.1124/dmd.106.013649. Epub 2007 Mar 7. Drug Metab Dispos. 2007. PMID: 17344339
A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif.
Kalgutkar AS, Driscoll J, Zhao SX, Walker GS, Shepard RM, Soglia JR, Atherton J, Yu L, Mutlib AE, Munchhof MJ, Reiter LA, Jones CS, Doty JL, Trevena KA, Shaffer CL, Ripp SL. Kalgutkar AS, et al. Chem Res Toxicol. 2007 Dec;20(12):1954-65. doi: 10.1021/tx700270r. Epub 2007 Oct 13. Chem Res Toxicol. 2007. PMID: 17935300
167 results