Synthesis and Aldose Reductase-Inhibitory Activities of Structural Analogues of WF-3681, a Novel Aldose Reductase Inhibitor

Abstract

Various analogues of WF-3681 (la), a novel aldose reductase inhibitor, were synthesized and examined for aldose reductase-inhibitory activity. It was found that the carboxylic acid function is necessary and the side-chain length is important for the activity. Furthermore, the lipophilicities of the benzene ring and the enol ether group are significant for increasing the activity. © 1988, The Pharmaceutical Society of Japan. All rights reserved.