Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists

被引：56

作者：

Ahn, HS ^{[1
]}

Arik, L ^{[1
]}

Boykow, G ^{[1
]}

Burnett, DA ^{[1
]}

Caplen, MA ^{[1
]}

Czarniecki, M ^{[1
]}

Domalski, MS ^{[1
]}

Foster, C ^{[1
]}

Manna, M ^{[1
]}

Stamford, AW ^{[1
]}

Wu, YS ^{[1
]}

机构：

[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(99)00339-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2073 / 2078

页数：6

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