Structure–activity relationships in platelet-activating factor (PAF). 11-From PAF-antagonism to phospholipase A 2 inhibition: syntheses and structure–activity …

…, JE Ombetta, CZ Dong, C Redeuilh, F Heymans…

Index: Binisti, Carine; Assogba, Leon; Touboul, Estera; Mounier, Carine; Huet, Jack; Ombetta, Jean-Edouard; Dong, Chang Zhi; Redeuilh, Catherine; Heymans, Francoise; Godfroid, Jean-Jacques European Journal of Medicinal Chemistry, 2001 , vol. 36, # 10 p. 809 - 828

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Citation Number: 36

Abstract

1-Benzoyl-2-alkyl piperazines are strong inhibitors of Group I and II secreted PLA2s. 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 PLA2 ...