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- W2895355796 abstract "Based on the structural analysis of tricyclic scaffolds as butyrylcholinesterase (BuChE) inhibitors, a series of pyrazolo[1,5-c][1,3]benzoxazin-5(5H)-one derivatives were designed, synthesized and evaluated for their acetylcholinesterase (AChE) and BuChE inhibitory activity. Compounds with 5-carbonyl and 7- or/and 9-halogen substitutions showed potential BuChE inhibitory activity, among which compounds 6a, 6c and 6g showed the best BuChE inhibition (IC50 = 1.06, 1.63 and 1.63 µM, respectively). The structure-activity relationship showed that the 5-carbonyl and halogen substituents significantly influenced BuChE activity. Compounds 6a and 6g were found nontoxic, lipophilic and exhibited remarkable neuroprotective activity and mixed-type inhibition against BuChE (Ki = 7.46 and 3.09 µM, respectively). Docking studies revealed that compound 6a can be accommodated into BuChE via five hydrogen bonds, one Pi-Sigma interaction and three Pi-Alkyl interactions." @default.
- W2895355796 created "2018-10-12" @default.
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- W2895355796 date "2018-01-01" @default.
- W2895355796 modified "2023-10-15" @default.
- W2895355796 title "Design, synthesis and biological evaluation of tricyclic pyrazolo[1,5-<i>c</i>][1,3]benzoxazin-5(5<i>H</i>)-one scaffolds as selective BuChE inhibitors" @default.
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- W2895355796 doi "https://doi.org/10.1080/14756366.2018.1488696" @default.
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