一系列非喹啉类半胱氨酰白三烯1受体拮抗剂：顺尔宁吡啶类似物的构效关系研究

A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.

作者信息

Guay D, Gauthier J Y, Dufresne C, Jones T R, McAuliffe M, McFarlane C, Metters K M, Prasit P, Rochette C, Roy P, Sawyer N, Zamboni R

机构信息

Merck Frosst Center for Therapeutic Research, Québec, Canada.

出版信息

Bioorg Med Chem Lett. 1998 Mar 3;8(5):453-8. doi: 10.1016/s0960-894x(98)00051-1.

DOI:10.1016/s0960-894x(98)00051-1

PMID:9871597

Abstract

The structure-activity relationship of a series of styrylpyridine analogs of MK-0476 (montelukast, Singulair) is described. This work has led to the identification of a number of potent and orally active cysLT1 receptor (LTD4 receptor) antagonists including 2ab (L-733,321) as an optimized candidate.

摘要

描述了一系列MK-0476（孟鲁司特，顺尔宁）的苯乙烯基吡啶类似物的构效关系。这项工作已导致鉴定出许多强效且口服活性的半胱氨酰白三烯1型受体（LTD4受体）拮抗剂，其中包括2ab（L-733,321）作为优化候选物。