Structure-activity relationships associated with 3, 4, 5-triphenyl-1H-pyrazole-1-nonanoic acid, a nonprostanoid prostacyclin mimetic

NA Meanwell, MJ Rosenfeld, JJK Wright…

Index: Meanwell, Nicholas A.; Rosenfeld, Michael J.; Wright, J. J. Kim; Brassard, Catherine L.; Buchanan, John O.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 2 p. 389 - 397

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Citation Number: 33

Abstract

A series of phenylated pyrazoloalkanoic acid derivatives were synthesized and evaluated as inhibitors of ADP-induced human platelet aggregation. 3, 4, 5-Triphenyl-1H-pyrazole-l- nonanoic acid (Sa), with an ICs0 of 0.4 pM, was the most potent inhibitor identified in this study. Biochemical studies determined that 8d increased intraplatelet cAMP accumulation and stimulated platelet membrane-bound adenylate cyclase in a concentration-dependent ...