Development of new donepezil analogs: synthesis, biological screening and in silico study rational
نویسندگان
چکیده
Abstract Fifteen new benzothiophene-based compounds were designed, synthesized, and evaluated as potential anti-Alzheimer agents. Most of the synthesized exhibited remarkable AChE inhibitory activity effectively inhibited self-mediated ?-amyloid protein in vitro. Compound 3g (IC 50 = 72.488 ± 3.69 ?M) showed a significant effect exceeding that donepezil 87.414 4.46 ?M). Furthermore, compound 3j 0.498 0.02 best comparable to 0.404 0.03 The vivo evaluation promising ( ) confirmed memory improvement scopolamine-induced impairment model mice. molecular docking simulation Torpedo californica- Tc AChE) active site good agreement with obtained screening results. silico ADMET other physicochemical parameters also reported.
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ژورنال
عنوان ژورنال: Medicinal Chemistry Research
سال: 2022
ISSN: ['1554-8120', '1054-2523']
DOI: https://doi.org/10.1007/s00044-022-02941-8