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, suggesting a potentially beneficial profile useful for the treatment of ischemic heart disease.