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

Author information

TAKAYUKI NAMIKI
YUKIHISA BABA
YASUTAKA SUZUKI
MOTOAKI NISHIKAWA
KOZO SAWADA
YOSHIKUNI ITOH
TERUO OKU
YOSHIHIKO KITAURA
MASASHI HASHIMOTO
Author's Organization：
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
(Present address)Pfizer Central Research
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,

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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