Inhibition of secretory phospholipase A2•2-synthesis and structure-activity relationship studies of 4,5-dihydro-3-(4-tetradecyloxybenzyl)-1,2,4-4H-oxadiazol-5-one (PMS1062) derivatives specific for group II enzyme

被引：29

作者：

Dong, CZ

Ahamada-Himidi, A

Plocki, S

Aoun, D

Touaibia, M

Habich, NMB

Huet, J

Redeuilh, C

Ombetta, JE

Godfrold, JJ

Massicot, F

Heymans, F

机构：

[1] Univ Paris 07, Lab Pharmacochim Mol, Unite Pharmacochim Mol & Syst Membranaires, EA2381, F-75251 Paris, France

[2] Univ Paris 05, Fac Pharm, Toxicol Lab, F-75270 Paris, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 06期

关键词：

phospholipase A(2); SAR; oxadiazolone; specific inhibitor;

D O I：

10.1016/j.bmc.2005.01.016

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：

We have recently reported the discovery of a series of specific inhibitors of human group IIA phospholipase A(2) (hGIIA PLA(2)) to display promising in vitro and in vivo properties. Here we describe the influence of different structural modifications on the specificity and potency against hGIIA PLA(2) versus porcine group IB PLA(2). The SAR results, as well as the log P and pK(a) values of oxadiazolone determined in this work, provide important information towards the comprehension of the mode of action of this kind of compounds. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1989 / 2007

页数：19

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