Phosphodiesterase 4 inhibitors as airways smooth muscle relaxant agents:: Synthesis and biological activities of triazine derivatives

被引：17
作者：
Leroux, F
van Keulen, BJ
Daliers, J
Pommery, N
Hénichart, JP
机构：
[1] Inst Chim Pharmaceut, F-59006 Lille, France
[2] UCB Pharma Sector, B-1420 Braine Lalleud, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 1999年 / 7卷 / 03期
关键词：
bronchodilators; enzyme inhibitors; substituent effects; antiinflammatories;
D O I：
10.1016/S0968-0896(98)00266-1
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of triazine derivatives was synthesized. The compounds were evaluated for tracheal smooth muscle relaxant and type 4 phosphodiesterase inhibitory activities. A highly significant correlation was observed between the two effects. Two compounds exhibited potent relaxant activity (EC50: 17 and 24 nM) and might be useful for the treatment of asthma. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：509 / 516
页数：8
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