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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
Author(s) -
Salem Ola I. A.,
Schulz Tobias,
Hartmann Rolf W.
Publication year - 2002
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/1521-4184(200203)335:2/3<83::aid-ardp83>3.0.co;2-3
Subject(s) - benzoic acid , isozyme , steroid , chemistry , reductase , enzyme , alkyl , stereochemistry , in vitro , biological activity , chemical synthesis , biochemistry , organic chemistry , hormone
The synthesis and biological evaluation of 4‐(4‐(alkyl‐ and phenylaminocarbonyl)‐benzoyl)benzoic acids ( 4a—4d ) as non‐steroidal inhibitors of steroid 5α‐reductase are described. The compounds were tested in vitro for 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 (IC 50 = 0.82 μM).