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Chem Pharm Bull (Tokyo) ; 45(11): 1767-76, 1997 Nov.
Article in English | MEDLINE | ID: mdl-9396152

ABSTRACT

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.


Subject(s)
5-alpha Reductase Inhibitors , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Pyrroles/chemical synthesis , Pyrroles/pharmacology , Animals , Fibroblasts , Humans , In Vitro Techniques , Magnetic Resonance Spectroscopy , Male , Molecular Conformation , Prostate/drug effects , Prostate/enzymology , Rats , Rats, Wistar , Structure-Activity Relationship
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