Antioxidant activity of novel diosgenin derivatives: Synthesis, biological evaluation, and in silico ADME prediction

Steroids(2022)

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摘要
•A series of novel diosgenin derivatives substituted at C3 position with various organic acids: cinnamic, nicotinic, 4–acetylbenzoic, 4–hydroxybenzoic, 4–aminobenzoic or (3–carboxy–1–oxopropyl)aminobenzoic were synthesized.•Predicted in silico, pharmacokinetic properties of the new compounds were in compliance with drug–likeness criteria for all derivatives.•All they can be considered as innoxious to normal human skin fibroblast (NHDF) at 5 µM concentration.•Compounds: 1, 2, 8, and 9 resulted no lytic activity (<5.0% of human red blood cells hemolysis rates), while the compound 5 exhibited hemolysis at the level of 6.4%.•Analogue 8 (substituted with p–aminobenzoic acid) displayed a highest antioxidant activity among all tested compounds with 61.6% blocking of induced lipid oxidation.
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关键词
Diosgenin,Diosgenin derivatives,Antioxidant activity,ADME
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