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Page 1
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. 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
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: li c. 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
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. Among authors: li j. 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. Among authors: li c, li j. 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: li c, li j. 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
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. Among authors: li j. 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
Comparative structure-activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition.
Sakya SM, Shavnya A, Cheng H, Li C, Rast B, Li J, Koss DA, Jaynes BH, Mann DW, Petras CF, Seibel SB, Haven ML, Lynch MP. Sakya SM, et al. Among authors: li c, li j. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1042-5. doi: 10.1016/j.bmcl.2007.12.025. Epub 2008 Jan 7. Bioorg Med Chem Lett. 2008. PMID: 18182290
Synthetic approaches to the 2009 new drugs.
Liu KK, Sakya SM, O'Donnell CJ, Flick AC, Li J. Liu KK, et al. Among authors: li j. Bioorg Med Chem. 2011 Feb 1;19(3):1136-54. doi: 10.1016/j.bmc.2010.12.038. Epub 2010 Dec 24. Bioorg Med Chem. 2011. PMID: 21256756 Review.
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