Synthesis and Biological Evaluation of 3-Tetrazolo Steroidal Analogs: Novel Class of 5α-Reductase Inhibitors

    December 2015 in “ Bioorganic & Medicinal Chemistry ”
    Saurabh Aggarwal, Manoj Kumar Mahapatra, Rajnish Kumar, Tilak Raj Bhardwaj, Rolf W. Hartmann, Jörg Haupenthal, Manoj Kumar
    TLDR 3-tetrazolo steroidal analogs can strongly inhibit the enzyme linked to hair loss.
    The study focused on synthesizing and evaluating 3-tetrazolo steroidal analogs as a novel class of 5α-reductase inhibitors. These compounds were tested for their ability to inhibit human 5α-reductase, an enzyme involved in the conversion of testosterone to dihydrotestosterone, which is linked to conditions like hair loss. The analogs demonstrated varying levels of inhibitory activity, with IC50 values ranging from 40 nM to 547 nM. The most potent compound, BDBM50334788, showed an IC50 of 40 nM, indicating strong inhibition of the enzyme. The research provided insights into the potential of these analogs as therapeutic agents for conditions related to 5α-reductase activity.
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