Synthesis of 1-benzyl-3-(5′-hydroxymethyl-2′-furyl)indazole analogues as novel antiplatelet agents

被引：127
作者：
Lee, FY
Lien, JC
Huang, LJ
Huang, TM
Tsai, SC
Teng, CM
Wu, CC
Cheng, FC
Kuo, SC [1 ]
机构：
[1] China Med Coll, Grad Inst Pharmaceut Chem, Taichung, Taiwan
[2] Yung Shin Pharmaceut Ind Co Ltd, Taichung, Taiwan
[3] Natl Taiwan Univ, Coll Med, Inst Pharmacol, Hsinchu, Taiwan
[4] Tajen Inst Technol, Dept Pharm, Pingtung, Taiwan
[5] MSD Pharma Serv Taiwan LTD, Taipei, Taiwan
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 22期
关键词：
D O I：
10.1021/jm010001h
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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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页码：3746 / 3749
页数：4
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