Targeting thrombin and factor VIIa: Design, synthesis, and inhibitory activity of functionally relevant indolizidinones

被引：51

作者：

Hanessian, S

Therrien, E

Granberg, K

Nilsson, I

机构：

[1] Univ Montreal, Dept Chem, Montreal, PQ H3C 3J7, Canada

[2] AstraZeneca R&D Molndal, Med Chem, Molndal, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 20期

基金：

加拿大自然科学与工程研究理事会;

关键词：

D O I：

10.1016/S0960-894X(02)00612-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Guided by molecular modeling, docking experiments, and available X-ray crystal structure data on the serine protease Factor VIIa and thrombin, a series of indolizidinone derivatives was designed and synthesized having diverse functionality at the P-1, P-2, and P-3 sites. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2907 / 2911

页数：5

共 31 条

[1]

AGNELLI G, 1991, THROMB HAEMOSTASIS, V66, P592

[2] The crystal structure of the complex of blood coagulation factor VIIa with soluble tissue factor [J].