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5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part III: molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile.
Sakya SM, Hou X, Minich ML, Rast B, Shavnya A, DeMello KM, Cheng H, Li J, Jaynes BH, Mann DW, Petras CF, Seibel SB, Haven ML. Sakya SM, et al. Bioorg Med Chem Lett. 2007 Feb 15;17(4):1067-72. doi: 10.1016/j.bmcl.2006.11.026. Epub 2006 Nov 15. Bioorg Med Chem Lett. 2007. PMID: 17126015
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: sakya sm. 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: sakya sm. Bioorg Med Chem. 2005 Mar 1;13(5):1805-9. doi: 10.1016/j.bmc.2004.11.048. Bioorg Med Chem. 2005. PMID: 15698798
5-heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog.
Sakya SM, DeMello KM, Minich ML, Rast B, Shavnya A, Rafka RJ, Koss DA, Cheng H, Li J, Jaynes BH, Ziegler CB, Mann DW, Petras CF, Seibel SB, Silvia AM, George DM, Lund LA, St Denis S, Hickman A, Haven ML, Lynch MP. Sakya SM, et al. Bioorg Med Chem Lett. 2006 Jan 15;16(2):288-92. doi: 10.1016/j.bmcl.2005.10.006. Epub 2005 Nov 3. Bioorg Med Chem Lett. 2006. PMID: 16275075
5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers.
Sakya SM, Cheng H, Lundy Demello KM, Shavnya A, Minich ML, Rast B, Dutra J, Li C, Rafka RJ, Koss DA, Li J, Jaynes BH, Ziegler CB, Mann DW, Petras CF, Seibel SB, Silvia AM, George DM, Hickman A, Haven ML, Lynch MP. Sakya SM, et al. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1202-6. doi: 10.1016/j.bmcl.2005.11.110. Epub 2005 Dec 27. Bioorg Med Chem Lett. 2006. PMID: 16380252
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: sakya sm. 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
Synthetic approaches to the 2003 new drugs.
Liu KK, Li J, Sakya S. Liu KK, et al. Mini Rev Med Chem. 2004 Dec;4(10):1105-25. doi: 10.2174/1389557043402900. Mini Rev Med Chem. 2004. PMID: 15579116 Review.
Synthetic approaches to the 2004 new drugs.
Li J, Liu KK, Sakya S. Li J, et al. Mini Rev Med Chem. 2005 Dec;5(12):1133-44. doi: 10.2174/138955705774933329. Mini Rev Med Chem. 2005. PMID: 16375759 Review.
42 results