Aminophosphonate endothelin converting enzyme inhibitors : potency-enhancing and selectivity-improving modifications of phosphoramidon

Abstract A series of α-aminophosphonic acid derivatives and a series of phosphoramidate derivatives have been synthesized and evaluated as inhibitors of a phosphoramidon-sensitive metalloproteinase endothelin converting enzyme (ECE). Some of these compounds exhibit potent ECE inhibitory activity. The most potent inhibitor ( XIIb ) is about 10 times as potent as phosphoramidon.