Kato M, Komoda K, Namera A, Sakai Y, Okada S, Yamada A, Yokoyama K, Migita E, Minobe Y, Tani T
Medicinal Chemistry Laboratory, Sumitomo Metal Industries, Ltd., Kyoto, Japan.
Chem Pharm Bull (Tokyo). 1997 Nov;45(11):1767-76. doi: 10.1248/cpb.45.1767.
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.