DISCOVERY OF L-740,515, A POTENT THIENOPYRIDINE CYSLT(1) RECEPTOR (LTD(4) RECEPTOR) ANTAGONIST

被引：6

作者：

LABELLE, M

GAREAU, Y

DUFRESNE, C

LAU, CK

BELLEY, M

JONES, TR

LEBLANC, Y

MCAULIFFE, M

MCFARLANE, CS

METTERS, KM

OUIMET, N

PERRIER, H

ROCHETTE, C

SAWYER, N

SLIPETZ, D

XIANG, YB

WANG, Z

PICKETT, CB

FORDHUTCHINSON, AW

YOUNG, RN

ZAMBONI, RJ

机构：

[1] Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Que. H9R 4P8

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 21期

关键词：

D O I：

10.1016/0960-894X(95)00448-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity studies leading to the discovery of a new series of non-quinoline cysLT(1) receptor (LTD(4) receptor) antagonists are described. These studies demonstrated that the quinoline ring system of montelukast(5) may be replaced by an appropriately substituted thienopyridine system, yielding potent compounds. Two other molecular features of montelukast, the terminal phenyl ring substitution and the vinyl link, were also reevaluated. These studies led to the identification of 1 (L-740,515), a compound with optimized in vitro and in vivo biological profiles.

引用

页码：2551 / 2556

页数：6

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