(E)-phenyl- and -heteroaryl-substituted O-benzoyl- (or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors

A series of (E)-phenyl- and -heteroaryl-substituted O-benzoyl- (or acyl)oximes 3a-n were synthesized for evaluating their human lipoprotein-associated phospholiphase A2 (Lp-PLA2) inhibitory activities. The less lipophilic derivatives 3a-c showed the most potent in vitro inhibitory activity on human...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-03, Vol.15 (5), p.1525-1527
Hauptverfasser:	JEONG, Tae-Sook, MI JEONG KIM, YU, Hana, KYUNG SOON KIM, CHOI, Joong-Kwon, KIM, Sung-Soo, WOO SONG LEE
Format:	Artikel
Sprache:	eng
Schlagworte:	1-Alkyl-2-acetylglycerophosphocholine Esterase Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Medical sciences Molecular Structure Oximes - chemical synthesis Oximes - chemistry Oximes - pharmacology Pharmacology. Drug treatments Phospholipases A - antagonists & inhibitors Phospholipases A2 Structure-Activity Relationship
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Zusammenfassung:	A series of (E)-phenyl- and -heteroaryl-substituted O-benzoyl- (or acyl)oximes 3a-n were synthesized for evaluating their human lipoprotein-associated phospholiphase A2 (Lp-PLA2) inhibitory activities. The less lipophilic derivatives 3a-c showed the most potent in vitro inhibitory activity on human Lp-PLA2.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.11.063