Synthesis and Study of Some 17a-Aza-D-Homo Steroids as 5α-Reductase Inhibitors
October 2020
in “
Current Drug Discovery Technologies
”
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Studysummary This study investigated various synthesized 5-reductase inhibitors and found that compound 6 had the highest anti-androgenic activity and receptor affinity compared to finasteride, showing potential due to its improved efficacy and bioavailability for further research in treating lower urinary tract symptoms. Our plain-language summary of this paper — not a Tressless recommendation.
The study synthesized and tested esters of 17a-Aza-D-homo-5-androsten-3β-ol as potential 5α-reductase inhibitors (5-ARI), which are used to treat men with lower urinary tract symptoms. The compounds were evaluated for their 5α-reductase inhibitory activity in-vivo by their effect on serum androgen level using ELISA assay procedure. The results showed that the target compounds (6-12) had increased anti-androgenic activity compared to finasteride and control, indicating their effectiveness in inhibiting 5α-reductase. Specifically, compound 6 showed the highest inhibitory activity and greater affinity for the 5-AR receptor, with increased solubility and dissolution compared to finasteride. Therefore, compound 6 has immense potential with improved efficacy and better bioavailability, making it a suitable candidate for further studies and optimal formulation.
