Synthesis of 1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole Analogues As Novel Antiplatelet Agents

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2001 Oct 19

PMID 11606139

Citations 19

Authors

F Y Lee

J C Lien

L J Huang

T M Huang

S C Tsai

C M Teng

C C Wu

F C Cheng

S C Kuo

Affiliations

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Abstract

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.

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