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.

引用

页码：81 / 86

页数：6

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