Experimental Evaluation of 3-Meta-Pyridine-1,2,4-Oxadiazole Derivative of Deoxycholic Acid as a Prototype of 5-Alpha-Reductase Inhibitors in In Silico and In Vivo Models

    February 2023 in “ Russian Journal of Bioorganic Chemistry ”
    Yulia V. Meshkova, Dmitry S. Baev, И. В. Сорокина, Irina I. Popadyuk, Oksana V. Salomatina, Н. А. Жукова, Т. Г. Толстикова, Нариман Ф. Салахутдинов
    TLDR The new compound may be a safer alternative to finasteride for prostate protection.
    The study investigates a novel 5-α-reductase inhibitor derived from deoxycholic acid, designed to minimize the side effects of current drugs like finasteride. The compound, incorporating a 3-meta-pyridine-1,2,4-oxadiazole fragment, showed similar binding energy to 5-AR as finasteride in molecular docking studies. In vivo experiments on Wistar rats revealed that the compound, at 20 mg/kg, provided prostate protection comparable to finasteride at 10 mg/kg, while also reducing prostate proliferation. Notably, the new compound demonstrated lower toxicity, with an LD50 of over 1500 mg/kg in CD-1 mice, compared to 1060 mg/kg for finasteride, indicating its potential as a safer alternative for further preclinical trials.
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