title: Benzodiazepine-based selective inhibitors of mitochondrial F1F0 ATP hydrolase.
abstract: A series of benzodiazepine-based inhibitors of mitochondrial F(1)F(0) ATP hydrolase were prepared and evaluated for their ability to selectively inhibit the enzyme in the forward direction. Compounds from this series showed excellent potency and selectivity for ATP hydrolase versus ATP synthase, suggesting a potentially beneficial profile useful for the treatment of ischemic heart disease.
authors.affiliation: Department of Discovery Chemistry, Bristol-Myers Squibb, Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. lawrence.hamann@bms.com
authors.forename: Lawrence G
authors.initials: LG
authors.lastname: Hamann
authors.forename: Charles Z
authors.initials: CZ
authors.lastname: Ding
authors.forename: Arthur V
authors.initials: AV
authors.lastname: Miller
authors.forename: Cort S
authors.initials: CS
authors.lastname: Madsen
authors.forename: Paulina
authors.initials: P
authors.lastname: Wang
authors.forename: Philip D
authors.initials: PD
authors.lastname: Stein
authors.forename: Andrew T
authors.initials: AT
authors.lastname: Pudzianowski
authors.forename: David W
authors.initials: DW
authors.lastname: Green
authors.forename: Hossain
authors.initials: H
authors.lastname: Monshizadegan
authors.forename: Karnail S
authors.initials: KS
authors.lastname: Atwal
mesh_terms: D000255:Adenosine Triphosphate / Q000378:metabolism*; D000818:Animals; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000494:pharmacology*; D002417:Cattle; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D008928:Mitochondria / Q000201:enzymology*; D025261:Mitochondrial Proton-Translocating ATPases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D001569:Benzodiazepines; D000255:Adenosine Triphosphate; D025261:Mitochondrial Proton-Translocating ATPases