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ID: ALA1147755
Journal: Bioorg Med Chem Lett
Title: 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.
Authors: 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.
Abstract: Structure-activity relationship (SAR) studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-yl]-5-methanesulfonyl (SO(2)Me)/sulfamoyl (SO(2)NH(2))-pyridine derivatives for canine COX enzymes are described. The studies led to the identification of 2e as lead with potent in vitro activity, selectivity, and in vivo activity in dogs and cats.
CiteXplore: 16275075