title: A novel transition state analog inhibitor of guanase based on azepinomycin ring structure: Synthesis and biochemical assessment of enzyme inhibition.
abstract: Synthesis and biochemical inhibition studies of a novel transition state analog inhibitor of guanase bearing the ring structure of azepinomycin have been reported. The compound was synthesized in five-steps from a known compound and biochemically screened against the rabbit liver guanase. The compound exhibited competitive inhibition profile with a K(i) of 16.7±0.5μM.
authors.affiliation: Laboratory for Drug Design & Synthesis, Department of Chemistry & Biochemistry, University of Maryland, Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA.
authors.forename: Saibal
authors.initials: S
authors.lastname: Chakraborty
authors.forename: Niti H
authors.initials: NH
authors.lastname: Shah
authors.forename: James C
authors.initials: JC
authors.lastname: Fishbein
authors.forename: Ramachandra S
authors.initials: RS
authors.lastname: Hosmane
mesh_terms: D000818:Animals; D001381:Azepines / Q000737:chemistry* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006148:Guanine Deaminase / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D008099:Liver / Q000201:enzymology; D011817:Rabbits; D013329:Structure-Activity Relationship
chemical_list: D001381:Azepines; D004791:Enzyme Inhibitors; C054358:azepinomycin; D006148:Guanine Deaminase