Q4 · MEDICINE
Article
Author: Yamada, Akira ; Yokoyama, Kouichi ; Namera, Akira ; Migita, Emiko ; Sakai, Yusuke ; Okada, Satoshi ; Komoda, Keiko ; Tani, Tadato ; Kato, Masaya ; Minobe, Yasushi
A series of pyrrole butyric acid derivatives was synthesized and evaluated for inhibitory activity on human and rat steroid 5 alpha-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 5 alpha-reductase.