Platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists derived from amidinoindoles.

被引：9
|
作者：
Sall, DJ [1 ]
Arfsten, AE [1 ]
Berry, DR [1 ]
Denney, ML [1 ]
Harms, CS [1 ]
McCowan, JR [1 ]
Ray, JK [1 ]
Scarborough, RM [1 ]
Um, SL [1 ]
Utterback, BG [1 ]
Jakubowski, JA [1 ]
机构：
[1] COR THERAPEUT INC, S SAN FRANCISCO, CA 94080 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 01期
关键词：
D O I：
10.1016/0960-894X(95)00563-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of substituted amidinoindoles have been prepared as mimics of the RGD sequence and were studied as antagonists of the platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa). The agents were potent and selective antagonists of GPIIb-IIIa. Compared to their acyclic counterparts, the amidinoindole series bound with 10- to 20-fold greater affinity, indicating the advantages of added conformational restriction and/or hydrophobicity in the basic region of RGD mimics.
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页码：81 / 86
页数：6
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