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Page 1
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.
Cheng H, Lundy DeMello KM, Li J, Sakya SM, Ando K, Kawamura K, Kato T, Rafka RJ, Jaynes BH, Ziegler CB, Stevens R, Lund LA, Mann DW, Kilroy C, Haven ML, Nimz EL, Dutra JK, Li C, Minich ML, Kolosko NL, Petras C, Silvia AM, Seibel SB. Cheng H, et al. Among authors: kolosko nl. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2076-80. doi: 10.1016/j.bmcl.2006.01.059. Epub 2006 Feb 7. Bioorg Med Chem Lett. 2006. PMID: 16464588
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
Li J, DeMello KM, Cheng H, Sakya SM, Bronk BS, Rafka RJ, Jaynes BH, Ziegler CB, Kilroy C, Mann DW, Nimz EL, Lynch MP, Haven ML, Kolosko NL, Minich ML, Li C, Dutra JK, Rast B, Crosson RM, Morton BJ, Kirk GW, Callaghan KM, Koss DA, Shavnya A, Lund LA, Seibel SB, Petras CF, Silvia A. Li J, et al. Among authors: kolosko nl. Bioorg Med Chem Lett. 2004 Jan 5;14(1):95-8. doi: 10.1016/j.bmcl.2003.10.004. Bioorg Med Chem Lett. 2004. PMID: 14684306
In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor.
Li J, Lynch MP, Demello KL, Sakya SM, Cheng H, Rafka RJ, Bronk BS, Jaynes BH, Kilroy C, Mann DW, Haven ML, Kolosko NL, Petras C, Seibel SB, Lund LA. Li J, et al. Among authors: kolosko nl. Bioorg Med Chem. 2005 Mar 1;13(5):1805-9. doi: 10.1016/j.bmc.2004.11.048. Bioorg Med Chem. 2005. PMID: 15698798
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
Li J, Bronk BS, Dirlam JP, Blize AE, Bertinato P, Jaynes BH, Hickman A, Miskell C, Pillai UA, Tibbitts JS, Haven ML, Kolosko NL, Barry CJ, Manion TB. Li J, et al. Among authors: kolosko nl. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1996-9. doi: 10.1016/j.bmcl.2007.01.018. Epub 2007 Jan 17. Bioorg Med Chem Lett. 2007. PMID: 17276061