ChemInform Abstract: 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

Autor:	Jean-Edouard Ombetta, Françoise Heymans, Chang-Zhi Dong, Jean-Jacques Godfroid, Léon Assogba, Estera Touboul, Catherine Redeuilh, Carine Binisti, Jack Huet, Carine Mounier
Rok vydání:	2010
Předmět:	biology Platelet-activating factor Stereochemistry General Medicine Piperazine chemistry.chemical_compound Phospholipase A2 chemistry Amide Lipophilicity biology.protein Structure–activity relationship Moiety lipids (amino acids peptides and proteins) Sulfamide
Zdroj:	ChemInform. 33
ISSN:	1522-2667 0931-7597
Popis:	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, 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 PLA2s.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::53a2236f1aa7156e945647a3cbefc4d3 https://doi.org/10.1002/chin.200212268 Zobrazit plný text záznamu Plný text