A new series of selective COX-2 inhibitors: 5,6-diarylthiazolo[3,2-b][1,2,4]triazoles
A series of 5,6-diarylthiazolo[3,2-b][1,2,4]triazoles was prepared for evaluation of potency and selectivity against human COX-1 and COX-2 enzymes. This lead to the discovery of L-768,277, a potent and selective COX-2 inhibitor that also demonstrated good in vivo activity.
Roy, P; Leblanc, Y; Ball, RG; Brideau, C; Chan, CC; Chauret, N; Cromlish, W; Ethier, D; Gauthier, JY; Gordon, R; Greig, G; Guay, J; Kargman, S; Lau, CK; O'Neill, G; Silva, J; Thérien, M; Van Staden, C; Wong, E; Xu, L; Prasit, P
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