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

TAKAYUKI NAMIKI; YUKIHISA BABA; YASUTAKA SUZUKI; MOTOAKI NISHIKAWA; KOZO SAWADA; YOSHIKUNI ITOH; TERUO OKU; YOSHIHIKO KITAURA; MASASHI HASHIMOTO

doi:10.1248/cpb.36.1404

TAKAYUKI NAMIKI, YUKIHISA BABA, YASUTAKA SUZUKI, MOTOAKI NISHIKAWA, KOZO SAWADA, YOSHIKUNI ITOH, TERUO OKU, YOSHIHIKO KITAURA, MASASHI HASHIMOTO

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Keywords: structure-activity relationship

JOURNAL FREE ACCESS

1988 Volume 36 Issue 4 Pages 1404-1414

DOI https://doi.org/10.1248/cpb.36.1404

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Abstract

Various analogues of WF-3681 (1a), 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.

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