Synthesis and pharmacological evaluation of new cysLT(1) receptor antagonists

被引：9

作者：

Griera, R

Armengol, M

Reyes, A

Alvarez, M

Palomer, A

Cabre, F

Pascual, J

Garcia, M

Mauleon, D

机构：

[1] UNIV BARCELONA,FAC FARM,LAB QUIM ORGAN,E-08028 BARCELONA,SPAIN

[2] LABS MENARINI SA,R&D DEPT,BADALONA,SPAIN

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1997年 / 32卷 / 7-8期

关键词：

leukotriene D-4; antagonist; 4-quinolone; acylsulfonamide; molecular modelling;

D O I：

10.1016/S0223-5234(97)83282-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This paper describes the synthesis and pharmacological evaluation of three series of compounds 4a-b, 13a-k and 19, structurally related to the known potent cysLT(1) receptor antagonists RG-12553, ICI-204219 and ONO-1078, respectively. The common structural feature of these new series is the presence of a 4-quinolone nucleus acting as a template for substitution of the aromatic nucleus present in the prototype antagonists. We describe the evolution of these series leading to antagonists with potency at nanomolar concentrations in vitro.

引用

页码：547 / 570

页数：24

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