title: Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2.
abstract: We have synthesised some lipidic diamines and aminoalcohols and examined their behaviour as inhibitors of secretory and cytosolic PLA2. Some structure-activity relationships considerations have been deduced. Compound 14 was a potent and selective inhibitor of cPLA2 and compound 4 showed a dual inhibitory profile against both types of PLA2 while no cytotoxicity at 10 microM on human neutrophils or on murine macrophage line was observed for both.
authors.affiliation: Departmento de Farmacología, Univ. de Valencia, Burjassot, Spain.
authors.forename: R
authors.initials: R
authors.lastname: Lucas
authors.forename: A
authors.initials: A
authors.lastname: Ubeda
authors.forename: M
authors.initials: M
authors.lastname: Payá
authors.forename: M
authors.initials: M
authors.lastname: Alves
authors.forename: E
authors.initials: E
authors.lastname: del Olmo
authors.forename: J L
authors.initials: JL
authors.lastname: López
authors.forename: A
authors.initials: A
authors.lastname: San Feliciano
mesh_terms: D000605:Amino Alcohols / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002460:Cell Line; D003600:Cytosol / Q000201:enzymology*; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008055:Lipids / Q000737:chemistry; D051379:Mice; D010741:Phospholipases A / Q000037:antagonists & inhibitors / Q000378:metabolism*; D054467:Phospholipases A2; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D000605:Amino Alcohols; D003959:Diamines; D008055:Lipids; D011994:Recombinant Proteins; D010741:Phospholipases A; D054467:Phospholipases A2