Optimization of the β-aminoester class of factor Xa inhibitors.: Part 1:: P4 and side-chain modifications for improved in vitro potency

被引：17

作者：

Czekaj, M ^{[1
]}

Klein, SI ^{[1
]}

Guertin, KR ^{[1
]}

Gardner, CJ ^{[1
]}

Zulli, AL ^{[1
]}

Pauls, HW ^{[1
]}

Spada, AP ^{[1
]}

Cheney, DL ^{[1
]}

Brown, KD ^{[1
]}

Colussi, DJ ^{[1
]}

Chu, V ^{[1
]}

Leadley, RJ ^{[1
]}

Dunwiddie, CT ^{[1
]}

机构：

[1] Aventis Pharmaceut, Drug Innovat & Approval, Bridgewater, NJ 08807 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(02)00212-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A systematic modification of the C3 side-chain of the beta-aminoester class of factor Xa inhibitors and a survey Of P-4 variations is described. These changes have resulted in the identification of sub-nanomolar inhibitors with improved selectivity versus related proteases. Coagulation parameters (i.e., APTT doubling concentrations) are also improved. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1667 / 1670

页数：4

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