Novel 5α-Reductase Inhibitors: Synthesis, Structure-Activity Studies, and Pharmacokinetic Profile of Phenoxybenzoylphenyl Acetic Acids

    December 2005 in “ Journal of Medicinal Chemistry ”
    Ola I. A. Salem, Martin Frotscher, Christiane Scherer, Alexander Neugebauer, Klaus M. Biemel, Martina Streiber, Ruth Maas, Rolf W. Hartmann
    TLDR A brominated phenoxy compound effectively inhibits a human enzyme and shows potential for clinical use.
    The study synthesized and evaluated novel benzoyl benzoic acids and phenylacetic acids as inhibitors of rat and human steroid 5α-reductase isozymes 1 and 2. These compounds were potent and selective inhibitors of the human type 2 enzyme, with IC50 values in the nanomolar range. A phenylacetic acid derivative with bromination in the 4-position of the phenoxy moiety (compound 12) was the strongest inhibitor, comparable to finasteride, with an IC50 of 5 nM. This compound showed good oral absorption, high bioavailability, and a biological half-life of 5.5 hours in rats, indicating its potential for further clinical evaluation.
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