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 … Rolf W. Hartmann
    Studysummary In this study, novel substituted benzoyl benzoic acids and phenylacetic acids were potent and selective inhibitors of human steroid 5alpha-reductase type 2, with one compound showing promising bioavailability in rats for potential clinical evaluation.
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    Research cited in this study 4

    1. Marked Suppression of Dihydrotestosterone in Men with Benign Prostatic Hyperplasia by Dutasteride, a Dual 5α-Reductase Inhibitor ˜The œJournal of clinical endocrinology and metabolism/Journal of clinical endocrinology & metabolism · 2004
    2. Synthesis and Evaluation of 2'-Substituted 4-(4'-Carboxy- or 4'-Carboxymethylbenzylidene)-N-Acylpiperidines: Highly Potent and In Vivo Active Steroid 5α-Reductase Type 2 Inhibitors Journal of Medicinal Chemistry · 2002
    3. 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 Archiv Der Pharmazie · 2002
    4. Species Differences in Prostatic Steroid 5α-Reductases of Rat, Dog, and Human Endocrinology · 1985