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

    Yulia V. Meshkova, Dmitry S. Baev, И. В. Сорокина, Irina I. Popadyuk, Oksana V. Salomatina, Н. А. Жукова, Т. Г. Толстикова, Нариман Ф. Салахутдинов
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    Studysummary In an animal study, researchers observed that a newly synthesized deoxycholic acid derivative showed similar prostate protection effects to finasteride in Wistar rats while being less toxic.
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    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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