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

Autor:	Chang-Zhi Dong, Azali Ahamada-Himidi, Stéphanie Plocki, Darina Aoun, Mohamed Touaibia, Nadia Meddad-Bel Habich, Jack Huet, Catherine Redeuilh, Jean-Edouard Ombetta, Jean-Jacques Godfroid, France Massicot, Françoise Heymans
Rok vydání:	2004
Předmět:	Alkylation Stereochemistry Clinical Biochemistry Pharmaceutical Science In Vitro Techniques Biochemistry Chemical synthesis Phospholipases A Inhibitory Concentration 50 Structure-Activity Relationship Phospholipase A2 In vivo Drug Discovery medicine Structure–activity relationship Humans Enzyme Inhibitors Molecular Biology Oxazoles chemistry.chemical_classification Phospholipase A biology Molecular Structure Chemistry Organic Chemistry Phospholipases A2 Enzyme Mechanism of action Enzyme inhibitor biology.protein Molecular Medicine lipids (amino acids peptides and proteins) medicine.symptom
Zdroj:	Bioorganicmedicinal chemistry. 13(6)
ISSN:	0968-0896
Popis:	We have recently reported the discovery of a series of specific inhibitors of human group IIA phospholipase A2 (hGIIA PLA2) 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 PLA2 versus porcine group IB PLA2. The SAR results, as well as the log P and pKa values of oxadiazolone determined in this work, provide important information towards the comprehension of the mode of action of this kind of compounds.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbc2d4dbf8f1c4c30b4b98483d28af17 https://pubmed.ncbi.nlm.nih.gov/15727853 Zobrazit plný text záznamu Full Text from ScienceDirect