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- W4362450060 abstract "We have synthesized twelve thiazole-thiourea hybrid derivatives (1-12) and evaluated against acetylcholinesterase and butyrylcholinesterase enzymes. All analogues showed outstanding activities having IC50 values ranged from 0.30 ± 0.05 to 15.40 ± 0.30 µM (AChE) and 0.40 ± 0.05 to 22.70 ± 0.40 µM (BuChE) as compared to standard drug Donepezil (IC50 = 2.16 ± 0.12 & 4.5 ± 0.11 µM respectively). In both cases, analogues 11 (IC50 = 0.30 ± 0.05 & 0.40 ± 0.05 µM) and analogue 12 (IC50 = 0.80 ± 0.05 & 1.10 ± 0.05 µM) withstand first and second most potent among the whole series. Structure activity relationship was carried out for all analogues which mainly depend upon number, nature, position and electron donating/withdrawing effects of the substituent/s on phenyl ring. Molecular docking study was carried out to show the binding interaction of the most potent analogue with the active site of enzyme." @default.
- W4362450060 created "2023-04-05" @default.
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- W4362450060 date "2023-06-01" @default.
- W4362450060 modified "2023-09-29" @default.
- W4362450060 title "Synthesis, in vitro acetylcholinesterase, butyrylcholinesterase activities and in silico molecular docking study of thiazole-thiourea hybrid derivatives" @default.
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- W4362450060 doi "https://doi.org/10.1016/j.cdc.2023.101025" @default.
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