Synthesis and Evaluation of 2'-Substituted 4-(4'-Carboxy-or 4'-carboxymethylbenzylidene)-N-acylpiperidines: Highly Potent and in Vivo Active Steroid 5α-Reductase …

F Picard, S Barassin, A Mokhtarian…

文献索引：Picard, Franck; Barassin, Stephan; Mokhtarian, Armand; Hartmann, Rolf W. Journal of Medicinal Chemistry, 2002 , vol. 45, # 16 p. 3406 - 3417

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被引用次数: 26

摘要

Sixteen compounds derived from N-acyl-4-benzylidenepiperidine-4'-carboxylic acids were synthesized and evaluated for inhibition of rat and human steroid 5α-reductase isozymes types 1 and 2. In the dicyclohexylacetyl series, fluorination in the 2-position of the benzene nucleus (15), exchange of the carboxy group by a carboxymethyl moiety (20), and combination of both structural modifications (25) led to highly active inhibitors of the ...