The design of non-peptide human Bradykinin B12 receptor antagonists employing the benzodiazepine peptidomimetic scaffold

被引：52

作者：

Dziadulewicz, EK

Brown, MC

Dunstan, AR

Lee, W

Said, NB

Garratt, PJ

机构：

[1] Novartis Inst Med Sci, London WC1E 6BN, England

[2] Univ London Univ Coll, Dept Chem, London WC1H 0AJ, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 03期

基金：

英国工程与自然科学研究理事会;

关键词：

D O I：

10.1016/S0960-894X(99)00015-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The Bradykinin B-2 receptor antagonist HOE 140 (D-Arg-Arg-Pro-EIyp-Gly-Thi-Ser-D-Tic-Oic-Arg) has been used as a template for the de novo design and synthesis of a small number of non-peptide lead compounds based on the 1,4-benzodiazepin-2-one framework. Two of the compounds have been found to exhibit moderate K-i values of 8.9 and 9.2 mu M at the human Bradykinin B-2 receptor. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：463 / 468

页数：6

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