Synthesis and Biological Evaluation of 4-(4-(Alkyl-and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-steroidal Inhibitors of Steroid 5alpha-Reductase Isozymes 1 and 2.
The synthesis and biological evaluation of 4-(4-(alkyl- and phenylaminocarbonyl)-benzoyl)benzoic acids (4a-4d) as non-steroidal inhibitors of steroid 5alpha-reductase are described. The compounds were tested in vitro for inhibitory activity toward rat and human 5alpha-reductase isozymes 1 and 2 at a concentration of 10 &mgr;M.The most active inhibitor for the human type 2 isozyme was 4-(4-(phenylaminocarbonyl)benzoyl) benzoic acid, compound 4c (IC (50) = 0.82 &mgr;M).
Salem
Ola I. A.
OI
8.5 Pharmaceutical and Medicinal Chemistry, Saarland University, P.O.Box 15 11 50, D-66041 Saarbrücken, Germany.
Schulz
Tobias
T
Hartmann
Rolf W.
RW