Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Studies on Antidiabetic Agents. III. 5-Arylthiazolidine-2, 4-diones as Potent Aldose Reductase Inhibitors
TAKASHI SOHDAKATSUTOSHI MIZUNOEIKO IMAMIYAHIROYUKI TAWADAKANJI MEGUROYUTAKA KAWAMATSUYUJIRO YAMAMOTO
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Keywords: rat-leus-culture
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1982 Volume 30 Issue 10 Pages 3601-3616

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Abstract

Thiazolidine-2, 4-dione derivatives having one or two substituent (s) such as phenyl, heteryl and alkyl group (s) at the 5-position were synthesized and evaluated as aldose reductase inhibitors. Inhibition by the active compounds of the swelling of the lens in a rat-lens-culture assay was also measured. Among these compounds, a series of 5-(3, 4-dialkoxyphenyl) thiazolidine-2, 4-diones showed pronounced activities in both assays. Structure-activity relationships are discussed and a new approach to the synthesis of 5-arylthiazolidine-2, 4-diones is described.

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© The Pharmaceutical Society of Japan
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