Synthesis and biological evaluation of 4-(4-alkyl- and Phenylaminocarbonyl)benzoyl)benzoic acid derivatives as nonsteroidal inhibitors of steroid 5α-reductase isozymes 1 and 2

Faculty of Pharmacy

Assiut University

Synthesis and biological evaluation of 4-(4-alkyl- and Phenylaminocarbonyl)benzoyl)benzoic acid derivatives as nonsteroidal inhibitors of steroid 5α-reductase isozymes 1 and 2

Research Authors
Salem, O. I. A.; Schulz, T.; Hartmann, R. W.
Research Department
Department of Pharmaceutical Organic Chemistry
Research Journal
Arch. Pharm. Pharm. Med. Chem
Research Rank
1
Research Vol
(2-3)335
Research Website
http://www.ncbi.nlm.nih.gov/pubmed/12043459
Research Year
2002
Research Member
Ola Ibrahim Abdel Razek Salem
Research Abstract

The synthesis and biological evaluation of 4-(4-(alkyl- and phenylaminocarbonyl)benzoyl)benzoic acids (4a-4d) as non-steroidal inhibitors of steroid 5 alpha-reductase are described. The compounds were tested in vitro for inhibitory activity toward rat and human 5 alpha-reductase isozymes 1 and 2 at a concentration of 10 microM. The most active inhibitor for the human type 2 isozyme was 4-(4-(phenylaminocarbonyl)benzoyl)benzoic acid, compound 4c (IC50 = 0.82 microM).