Benzodiazepine-based selective inhibitors of mitochondrial F1F0 ATP hydrolase

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, sug...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-02, Vol.14 (4), p.1031-1034
Hauptverfasser:	HAMANN, Lawrence G, DING, Charles Z, MILLER, Arthur V, MADSEN, Cort S, WANG, Paulina, STEIN, Philip D, PUDZIANOWSKI, Andrew T, GREEN, David W, MONSHIZADEGAN, Hossain, ATWAL, Karnail S
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Triphosphate - metabolism Animals Benzodiazepines - chemical synthesis Benzodiazepines - pharmacology Biological and medical sciences Cardiovascular system Cattle Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Medical sciences Miscellaneous Mitochondria - enzymology Mitochondrial Proton-Translocating ATPases - antagonists & inhibitors Mitochondrial Proton-Translocating ATPases - metabolism Pharmacology. Drug treatments Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.11.052