title: Synthesis of barbiturate-based methionine aminopeptidase-1 inhibitors.
abstract: The syntheses of a new class of barbiturate-based inhibitors for human and Escherichia Coli methionine aminopeptidase-1 (MetAP-1) are described. Some of the synthesized inhibitors show selective inhibition of the human enzyme with high potency.
authors.affiliation: Department of Pharmaceutical Sciences, North Dakota State University, 1401 Albrecht Boulevard, Fargo, ND 58105, USA.
authors.forename: Manas K
authors.initials: MK
authors.lastname: Haldar
authors.forename: Michael D
authors.initials: MD
authors.lastname: Scott
authors.forename: Nitesh
authors.initials: N
authors.lastname: Sule
authors.forename: D K
authors.initials: DK
authors.lastname: Srivastava
authors.forename: Sanku
authors.initials: S
authors.lastname: Mallik
mesh_terms: D000626:Aminopeptidases / Q000037:antagonists & inhibitors*; D001463:Barbiturates / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D018360:Crystallography, X-Ray; D004926:Escherichia coli / Q000201:enzymology*; D006801:Humans; D063208:Methionyl Aminopeptidases; D008956:Models, Chemical; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D001463:Barbiturates; D011480:Protease Inhibitors; D000626:Aminopeptidases; D063208:Methionyl Aminopeptidases; C032232:barbituric acid