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

doi:10.1002/1521-4184(200203)335:2/3<83::AID-ARDP83>3.0.CO;2-3

Paper

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

Published Mar 1, 2002 · Ola I. A. Salem, T. Schulz, R. Hartmann

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Abstract

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).

In Vitro Study

Study Snapshot

4(4(phenylaminocarbonyl)benzoyl)benzoic acids show potential as non-steroidal inhibitors of steroid 5reductase, with compound 4c being the most active for human type 2 isozyme.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

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

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References

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