Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl) aniline derivatives targeting acetylcholinesterase, beta-amyloid aggregation and oxidative stress to treat Alzheimer's disease

Srivastava Pavan; Tripathi Prabhash Nath; Sharma PiyooshShrivastava Sushant Kumar

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Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl) aniline derivatives targeting acetylcholinesterase, beta-amyloid aggregation and oxidative stress to treat Alzheimer's disease

机译：Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl) aniline derivatives targeting acetylcholinesterase, beta-amyloid aggregation and oxidative stress to treat Alzheimer's disease

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Novel hybrids N-(4-phenoxybenzyl) aniline were designed, synthesized, and evaluated for their potential AChE inhibitory activity along with antioxidant potential. The inhibitory potential (IC50) of synthesized analogs was evaluated against human cholinesterases (hAChE and hBChE) using Ellman's method. Among all the tested compounds, 42 with trimethoxybenzene substituent showed maximum hAChE inhibition with the competitive type of enzyme inhibition (IC50 = 1.32 mu M; Ki = 0.879 mu M). Further, parallel artificial membrane permeation assay (PAMPA-BBB) showed favorable BBB permeability by most of the synthesized compounds. Meanwhile, compound 42 also inhibited AChE-induced A beta aggregation (39.5-66.9%) in thioflavin T assay. The in vivo behavioral studies showed dose-dependent improvement in learning and memory by compound 42. The ex vivo studies also affirmed the significant AChE inhibition and antioxidant potential of compound 42 in brain homogenates.

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来源
《Bioorganic and medicinal chemistry》 |2019年第16期|3650-3662|共13页
作者
Srivastava Pavan; Tripathi Prabhash Nath; Sharma PiyooshShrivastava Sushant Kumar;
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作者单位

Bananas Hindu Univ, Indian Inst Technol, Dept Pharmaceut Engn & Technol, Varanasi 221005, Uttar;

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正文语种英语
中图分类药学;
关键词
Acetylcholinesterase; Butyrylcholinesterase; Beta-Amyloid; N-Benzylaniline; Molecular hybridization;

Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl) aniline derivatives targeting acetylcholinesterase, beta-amyloid aggregation and oxidative stress to treat Alzheimer's disease

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