Synthesis of conformationally-restricted boropeptide thrombin inhibitors

被引：25

作者：

Cacciola, J ^{[1
]}

Fevig, JM ^{[1
]}

Alexander, RS ^{[1
]}

Brittelli, DR ^{[1
]}

Kettner, CA ^{[1
]}

Knabb, RM ^{[1
]}

Weber, PC ^{[1
]}

机构：

[1] DUPONT MERCK PHARMACEUT CO,WILMINGTON,DE 19880

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 03期

关键词：

D O I：

10.1016/0960-894X(96)00016-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of boropeptide thrombin inhibitors was prepared in which the P3 residues of 2 (Ac-(D)-Phe-Pro-boroLys-OH . HCl) and 3 (3-Phenylpropionyl-Pro-borolys-OH . HCl) were replaced by conformationally-restricted, benzoic acid-derived residues 4. The potent binding affinity of the resulting inhibitors such as 10 may be due in part to a unique mode of binding in the thrombin active site.

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页码：301 / 306

页数：6

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