The design and synthesis of thrombin inhibitors: Analogues of MD805 containing non-polar surrogates for arginine at the P1 position

被引：10

作者：

Baettig, U ^{[1
]}

Brown, L ^{[1
]}

Brundish, D ^{[1
]}

Dell, C ^{[1
]}

Furzer, A ^{[1
]}

Garman, S ^{[1
]}

Janus, D ^{[1
]}

Kane, PD ^{[1
]}

Smith, G ^{[1
]}

Walker, CV ^{[1
]}

Cockcroft, XL ^{[1
]}

Ambler, J ^{[1
]}

Mitchelson, A ^{[1
]}

Talbot, MD ^{[1
]}

Tweed, M ^{[1
]}

Wills, N ^{[1
]}

机构：

[1] Novartis Horsham Res Ctr, Horsham RH12 4AB, W Sussex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(00)00282-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of monocyclic and bicyclic amino acids have been synthesised and incorporated into thrombin inhibitors based on CGH728, an analogue of the Mitsubishi compound MD805. Benzthiazolylalanine (Bta) was found to be a good non-polar substitute for arginine at the P1 position, yielding compounds with low nanomolar potency and good selectivity for thrombin. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1563 / 1566

页数：4

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