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- W4313488297 abstract "Aldose reductase (AR) is a crucial enzyme of the polyol pathway through which glucose is metabolized under conditions of hyperglycemia related to diabetes. A series of novel acetic acid derivatives containing quinazolin-4(3H)-one ring (1-22) was synthesized and tested for in vitro AR inhibitory effect. All the target compounds exhibited nanomolar activity against the target enzyme, and all compounds displayed higher activity as compared to the reference drug epalrestat. Among them, Compound 19, named 2-(4-[(2-[(4-methylpiperazin-1-yl)methyl]-4-oxoquinazolin-3(4H)-ylimino)methyl]phenoxy)acetic acid, displayed the strongest inhibitory effect with a KI value of 61.20 ± 10.18 nM. Additionally, these compounds were investigated for activity against L929, nontumoral fibroblast cells, and MCF-7, breast cancer cells using the MTT assay. Compounds 16 and 19 showed lower toxicity against the normal L929 cells. The synthesized compounds' (1-22) absorption, distribution, metabolism, and excretion properties were also evaluated. Molecular docking simulations were used to look into the possible binding mechanisms of these inhibitors against AR." @default.
- W4313488297 created "2023-01-06" @default.
- W4313488297 creator A5031761636 @default.
- W4313488297 creator A5058620708 @default.
- W4313488297 creator A5081967794 @default.
- W4313488297 creator A5085107620 @default.
- W4313488297 creator A5085545567 @default.
- W4313488297 date "2023-01-04" @default.
- W4313488297 modified "2023-10-16" @default.
- W4313488297 title "Novel acetic acid derivatives containing quinazolin‐4(3<i>H</i>)‐one ring: Synthesis, in vitro, and in silico evaluation of potent aldose reductase inhibitors" @default.
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