Document Report Card

ID: ALA1125410

Journal: J Med Chem

Title: Selective irreversible inhibitors of aldose reductase.

Authors: Smar MW, Ares JJ, Nakayama T, Itabe H, Kador PF, Miller DD.

Abstract: A series of 5-substituted-1,3-dioxo-1H-benz[de]isoquinoline-2(3H)-acetic acid analogues have been examined as irreversible inhibitors of aldose reductase. The 5-alpha-bromoacetamide and 5-alpha-iodoacetamide analogues 5 and 6 gave irreversible inhibition of aldose reductase while the 5-alpha-chloroacetamide analogue 3 did not show this type of inhibition. Protection studies indicate that irreversible inhibitions are occurring at the inhibitor binding site. Comparative irreversible inhibition studies with rat lens aldose reductase (RLAR) and rat kidney aldehyde reductase (RKALR) indicate that 5-alpha-haloacetamide analogues 5 and 6 are much more effective inhibitors of RLAR.

CiteXplore: 1552504

DOI: 10.1021/jm00084a017