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

NA Meanwell, MJ Rosenfeld, JJK Wright…

文献索引：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

全文：HTML全文

被引用次数: 33

摘要

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 ...