Novel 2-oxoamide inhibitors of human group IVA phospholipase A2

dc.contributor.author	Kokotos, G	en
dc.contributor.author	Kotsovolou, S	en
dc.contributor.author	Six, DA	en
dc.contributor.author	Constantinou-Kokotou, V	en
dc.contributor.author	Beltzner, CC	en
dc.contributor.author	Dennis, EA	en
dc.date.accessioned	2014-06-06T06:45:06Z
dc.date.available	2014-06-06T06:45:06Z
dc.date.issued	2002	en
dc.identifier.issn	00222623	en
dc.identifier.uri	http://dx.doi.org/10.1021/jm025538p	en
dc.identifier.uri	http://62.217.125.90/xmlui/handle/123456789/2252
dc.subject.other	2 oxoamide	en
dc.subject.other	carboxyl group	en
dc.subject.other	norleucine	en
dc.subject.other	phospholipase A2	en
dc.subject.other	phospholipase A2 inhibitor	en
dc.subject.other	unclassified drug	en
dc.subject.other	article	en
dc.subject.other	drug structure	en
dc.subject.other	drug synthesis	en
dc.subject.other	enzyme activity	en
dc.subject.other	enzyme inhibition	en
dc.subject.other	Amides	en
dc.subject.other	Enzyme Inhibitors	en
dc.subject.other	Humans	en
dc.subject.other	Magnetic Resonance Spectroscopy	en
dc.subject.other	Norleucine	en
dc.subject.other	Phospholipases A	en
dc.subject.other	Stereoisomerism	en
dc.subject.other	Structure-Activity Relationship	en
dc.title	Novel 2-oxoamide inhibitors of human group IVA phospholipase A2	en
heal.type	journalArticle	en
heal.identifier.primary	10.1021/jm025538p	en
heal.publicationDate	2002	en
heal.abstract	A novel class of potent human cytosolic phospholipase A2 (GIVA PLA2) inhibitors was developed. These inhibitors were designed to contain the 2-oxoamide functionality and a free carboxyl group. Among the compounds tested, a longchain 2-oxoamide containing L-γ-norleucine was the most potent inhibitor, causing a 50% decrease in GIVA PLA2 activity at 0.009 mole fraction.	en
heal.journalName	Journal of Medicinal Chemistry	en
dc.identifier.issue	14	en
dc.identifier.volume	45	en
dc.identifier.doi	10.1021/jm025538p	en
dc.identifier.spage	2891	en
dc.identifier.epage	2893	en