Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications

被引：24

作者：

Plummer, JS ^{[1
]}

Berryman, KA

Cai, C

Cody, WL

DiMaio, J

Doherty, AM

Edmunds, JJ

He, JX

Holland, DR

Levesque, S

Kent, DR

Narasimhan, LS

Rubin, JR

Rapundalo, ST

Siddiqui, MA

Susser, AJ

St-Denis, Y

Winocour, PD

机构：

[1] Parke Davis Pharmaceut Res, Ann Arbor, MI 48105 USA

[2] BioChem Therapeut Inc, Laval, PQ H7V 4A7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(98)00613-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors is described. We have explored the SAR with modifications to the pi site. The introduction of arginine mimetics at the pi site led to potent and selective thrombin inhibitors. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

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页码：3409 / 3414

页数：6

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