Synthesis and Aldose Reductase-Inhibitory Activity of Benzo[b]furan Derivatives Possessing a Carboxymethylsulfamoyl Group

Yoshitaka OHISHI; Teruo MUKAI; Michiko NAGAHARA; Motoyuki YAJIMA; Norio KAJIKAWA

doi:10.1248/cpb.37.2398

Yoshitaka OHISHI, Teruo MUKAI, Michiko NAGAHARA, Motoyuki YAJIMA, Norio KAJIKAWA

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Keywords: carboxymethylsulfamoyl group, benzo[b]furan, aldose reductase, enzyme inhibition, structure-activity trend

JOURNAL FREE ACCESS

1989 Volume 37 Issue 9 Pages 2398-2405

DOI https://doi.org/10.1248/cpb.37.2398

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Abstract

Various benzo[b]futran derivatives with a carboxymethylsulfamoyl group were prepared and evaluated for aldose reductase-inhibitory potency. Most of the compounds displayed significant inhibitory activities (IC₅₀, 10^-8-10^-7M). Among the test compounds, the compounds having a carboxymethylsulfamoyl group at the 3- or 4-position exhibited the greatest inhibitory potency. Structure-activity trends of the tested compounds are discussed.

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