Structure-activity relationships in platelet-activating factor (PAF).: 11-From PAF-antagonism to phospholipase A2 inhibition:: syntheses and structure-activity relationships in 1-arylsulfamido-2-alkylpiperazines

被引：20

作者：

Binisti, C

Assogba, L

Touboul, E

Mounier, C

Huet, J

Ombetta, JE

Dong, CZ

Redeuilh, C

Heymans, F

Godfroid, JJ

机构：

[1] Univ Paris 07, Mol Pharmacol Lab, F-75251 Paris 05, France

[2] Inst Pasteur, Unite Venins, F-75724 Paris, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 36卷 / 10期

关键词：

phospholipase A(2) inhibitor; structure-activity relationships; piperazine;

D O I：

10.1016/S0223-5234(01)01274-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1-Benzoyl-2-alkyl piperazines are strong inhibitors of Group I and II secreted PLA(2)s. An improvement of their activity was obtained by replacing the amide function by a sulfamide and by introduction of electrodonor substituents on the para position of the benzenesulfonyl moiety. Neither the position on one of the carbon of the piperazine ring nor the absolute configuration of this carbon have an effect on the affinity for one or the other group of PLA(2), but the lipophilicity remains for these series an essential parameter. In addition structure-activity relationships allow new hypothesis on interaction of these piperazine derivatives with the catalytic site of PLA(2)s. (C) 2001 Editions scientifiques et medicales Elsevier SAS.

引用

页码：809 / 828

页数：20

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