Synthesis and Biological Evaluation of 4-(4-(Alkyl- and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-Steroidal Inhibitors of Steroid 5α-Reductase Isozymes 1 and 2

In 2002, researchers at Saarland University synthesized and evaluated 4-(4-(alkyl- and phenylaminocarbonyl)-benzoyl)benzoic acids (4a—4d) as non-steroidal inhibitors of steroid 5α-reductase, an enzyme involved in hair loss. These compounds were tested in vitro for their inhibitory activity toward rat and human 5α-reductase isozymes 1 and 2 at a concentration of 10 μM. The most active inhibitor for the human type 2 isozyme was 4-(4-(phenylaminocarbonyl)benzoyl) benzoic acid, compound 4c, with an IC 50 value of 0.82 μM.