Pyrrole Butyric Acid Derivatives as Inhibitors of Steroid 5α-Reductase

Masaya KATO; Keiko KOMODA; Akira NAMERA; Yusuke SAKAI; Satoshi OKADA; Akira YAMADA; Kouichi YOKOYAMA; Emiko MIGITA; Yasushi MINOBE; Tadato TANI

doi:10.1248/cpb.45.1767

Masaya KATO, Keiko KOMODA, Akira NAMERA, Yusuke SAKAI, Satoshi OKADA, Akira YAMADA, Kouichi YOKOYAMA, Emiko MIGITA, Yasushi MINOBE, Tadato TANI

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Keywords: 5α-reductase inhibitor, benign prostate hypertrophy, pyrrole derivative

JOURNAL FREE ACCESS

1997 Volume 45 Issue 11 Pages 1767-1776

DOI https://doi.org/10.1248/cpb.45.1767

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Abstract

A series of pyrrole butyric acid derivatives was synthesized and evaluated for inhibitory activity on human and rat steroid 5α-reductase in vitro and ex vivo. 3-Benzoyl-4-alkylpyrrole-1-butyric acids and 1-methyl-2-alkyl-3-benzoylpyrrole-5-butyric acid derivatives were effective inhibitors. Structure activity relationships were evaluated among the 37 compounds synthesized. Compound 37 (HQL-1069) shows potent inhibitory activities against both rat and human 5α-reductase.

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