Synthesis of barbiturate-based methionine aminopeptidase-1 inhibitors.
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.
Haldar
Manas K
MK
Department of Pharmaceutical Sciences, North Dakota State University, 1401 Albrecht Boulevard, Fargo, ND 58105, USA.
Scott
Michael D
MD
Sule
Nitesh
N
Srivastava
D K
DK
Mallik
Sanku
S
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
D001463:Barbiturates; D011480:Protease Inhibitors; D000626:Aminopeptidases; D063208:Methionyl Aminopeptidases; C032232:barbituric acid