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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.
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
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: rafka rj.
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
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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: rafka rj.
Bioorg Med Chem. 2005 Mar 1;13(5):1805-9. doi: 10.1016/j.bmc.2004.11.048.
Bioorg Med Chem. 2005.
PMID: 15698798
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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: rafka rj.
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
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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: rafka rj.
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
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Mild decarboxylative activation of malonic acid derivatives by 1,1'-carbonyldiimidazole.
Lafrance D, Bowles P, Leeman K, Rafka R.
Lafrance D, et al.
Org Lett. 2011 May 6;13(9):2322-5. doi: 10.1021/ol200575c. Epub 2011 Apr 13.
Org Lett. 2011.
PMID: 21488674
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An analytical method for the analysis of tulathromycin, an equilibrating triamilide, in bovine and porcine plasma and lung.
Gáler D, Hessong S, Beato B, Risk J, Inskeep P, Weerasinghe C, Schneider RP, Langer C, LaPerle J, Renouf D, Bessire A, Español E, Rafka R, Ragan C, Boettner W, Murphy T, Keller D, Benchaoui H, Nowakowski MA.
Gáler D, et al.
J Agric Food Chem. 2004 Apr 21;52(8):2179-91. doi: 10.1021/jf0351624.
J Agric Food Chem. 2004.
PMID: 15080618
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