A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists:: development of a nonhydrolyzable LPA3 receptor-selective antagonist

被引：32

作者：

Heasley, BH

Jarosz, R

Carter, KM

Van, SJ

Lynch, KR

Macdonald, TL

机构：

[1] Univ Virginia, Dept Chem, Charlottesville, VA 22904 USA

[2] Univ Virginia, Dept Pharmacol, Charlottesville, VA 22904 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 15期

关键词：

lysophosphatidic acid receptor antagonist;

D O I：

10.1016/j.bmcl.2004.05.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A recently reported dual LPA(1)/LPA(3) receptor antagonist (1) has been modified so as to modulate the basicity, sterics, and dipole moment of the 2-pyridyl moiety. Additionally, the implications of installing nonhydrolyzable phosphate head group isosteres with regard to antagonist potency and selectivity at LPA receptors is described. This study has resulted in the development of the first nonhydrolyzable and presumably phosphatase-resistant LPA(3)-selective antagonist reported to date. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：4069 / 4074

页数：6

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