Diarylsulfonamides as selective, non-peptidic thrombin inhibitors

被引：16

作者：

Weber, IR

Neidlein, R

von der Saal, W

Grams, F

Leinert, H

Strein, K

Engh, RA

Kucznierz, R ^{[1
]}

机构：

[1] Boehringer Mannheim GmbH, Dept Chem, D-68305 Mannheim, Germany

[2] Univ Heidelberg, Inst Pharmaceut Chem, D-69120 Heidelberg, Germany

[3] Max Planck Inst Biochem, D-82152 Martinsried, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(98)00269-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Based on the structures of aminopyridine thrombin inhibitors (1), a series of aminoalkyl- and guanidinoalkyl-substituted diarylsulfonamides were prepared. The most potent derivative, N-[3-(4-guanidinobutoxy)-5-methyl-phenyl]-benzenesulfonamide (6c) had Ki = 0.18 mu M for thrombin and did not inhibit trypsin, plasmin, or factor Xa. Comparison of the X-ray structures of the thrombin / 1b and the thrombin / 6c complexes revealed important aspects which govern the binding of such diarylsulfonamides to thrombin. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1613 / 1618

页数：6

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