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• W4210763985 startingPage "195" @default.
• W4210763985 abstract "Butyrylcholinesterase (BChE), a hydrolytic enzyme, is responsible for the termination of the action of acetylcholine besides acetylcholinesterase (AChE) in the synaptic cleft of the brain. The alteration in the enzyme level, in patients with the progression of Alzheimer's disease, makes it a therapeutic target. In the present study, we developed BChE inhibitors through scaffold hopping by exploring two previously reported compounds, i.e., 1,4-bis((4-chlorophenyl) sulfonyl)-3,6-diphenylpiperazine-2,5-dione and N-(2-chlorophenyl)-4-(phenylsulfonamido)benzamide, to afford scaffold and pharmacophore fragments, respectively. The N,2-diphenyl-2-(phenylsulfonamido)acetamide derivatives, thus designed, were synthesised and screened for the inhibition of AChE and BChE enzymes. Compounds 30 and 33 were found to be most active against BChE among the derivatives, with IC50 values of 7.331 ± 0.946 and 10.964 ± 0.936 μM, respectively. The compounds displayed a non-competitive mode of inhibition along with BBB permeability and good cell viability on SH-SY5Y cell line. The molecular docking analysis of the compounds with BChE showed interactions with Trp82, Trp231, Leu286, and His438. The molecular dynamics study revealed the stability of the protein-ligand complexes." @default.
• W4210763985 created "2022-02-08" @default.
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• W4210763985 date "2022-04-01" @default.
• W4210763985 modified "2023-09-27" @default.
• W4210763985 title "Identification of sulfonamide based butyrylcholinesterase inhibitors through scaffold hopping approach" @default.
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• W4210763985 doi "https://doi.org/10.1016/j.ijbiomac.2022.01.136" @default.
• W4210763985 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35090939" @default.
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