Synthesis of 1-Benzyl-3-(5‘-hydroxymethyl-2‘-furyl)indazole Analogues as Novel Antiplatelet Agents
作者:Fang-Yu Lee、Jin-Cherng Lien、Li-Jiau Huang、Tsang-Miao Huang、Sheng-Chung Tsai、Che-Ming Teng、Chin-Chung Wu、Fong-Chi Cheng、Sheng-Chu Kuo
DOI:10.1021/jm010001h
日期:2001.10.1
1-Benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole (28, YC-1) was selected as the lead compound for systemic structural modification. After screening for antiplatelet activity, SARs of YC-1 analogues were established. Among these potent active derivatives, compounds 29, 30, 31, 44, and 45 functioned as potent activators of sGC and inhibitors of PDE5 with potency comparable to that of YC-1. In addition, compound 58 was found to be a selective and potent inhibitor of protease-activated receptor type 4 (PAR4)-dependent platelet activation.