M. Kato et al., PYRROLE BUTYRIC-ACID DERIVATIVES AS INHIBITORS OF STEROID 5-ALPHA-REDUCTASE, Chemical and Pharmaceutical Bulletin, 45(11), 1997, pp. 1767-1776
A series of pyrrole butyric acid derivatives was synthesized and evalu
ated for inhibitory activity on human and rat steroid 5 alpha-reductas
e in vitro and ex vivo. 3-Benzoyl-4-alkylpyrrole-1-butyric acids and 1
-methyl-2-alkyl-3-benzoylpyrrole-5-butyric acid derivatives were effec
tive inhibitors. Structure activity relationships were evaluated among
the 37 compounds synthesized. Compound 37 (HQL-1069) shows potent inh
ibitory activities against both rat and human 5 alpha-reductase.