Microwave Assisted Synthesis of BenzilideneBenzylamine and Its Acetylcholinesterase and Butyrylcholinesterase Activity

H. Ullah, K. Zaman, M. Ismail
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引用次数: 2

Abstract

BenzilideneBenzylamine the derivative of Schiff bases contain azomethine group already used widely for industrial purposes and have wide range of biological activities. Benzilidene Benzylamine were synthesized by microwave irradiation reacting different aromatic and aniline purified pure crystal, 85% yield obtained reaction monitor by TLC. The Anticholinesterase activity utilized spectrophotometric Ellman assay for determination of butyrylcholinesterase and acetylcholinesterase. The synthesis compound 1 – 6 showed a wide range of inhibitory activity the compound 3((E)-N-(4-fluorobenzylidene)aniline) at 1000µg/mL, 71.62±0.74 percent inhibitory acetylcholinesterase potential while compound 6 ((E)-4 ((phenylimino)methyl) benzaldehyde) at 500 and 1000 µg/mL at IC50 show 71.68±0.22, 77.84±0.32 percent inhibitory potential comparatively greater than standard Galanthamine at 62.5µg/mL, 74.10±0.90 at IC50. The butyrylcholinesterase activity of compound 6 ((E)-4 ((phenylimino)methyl)benzaldehyde) at 1000 µg/mL, show 75.83±1.07 percent inhibitory potential which is similar to standard compound at 62.5µg/mL concentration of 75.45±0.90 percent butyrylcholinesterase inhibitory activity.
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微波辅助合成苄基二苄胺及其乙酰胆碱酯酶和丁基胆碱酯酶活性
亚苄基亚苄基胺是席夫碱的衍生物,含有甲亚胺基团,具有广泛的生物活性。采用微波辐照的方法,使不同的芳香族和苯胺纯化的纯结晶反应合成了亚苄基苯胺,用薄层色谱法测定了85%的收率。应用分光光度法测定丁酰胆碱酯酶和乙酰胆碱酯酶的抗胆碱酯酶活性。合成的化合物1-6显示出宽范围的抑制活性,化合物3(((E)-N-(4-氟亚苄基)苯胺)在1000µg/mL时对乙酰胆碱酯酶的抑制率为71.62±0.74%,而化合物6(((E)-4((苯基亚氨基)甲基)苯甲醛)在500和1000µg/mL时在IC50时显示出71.68±0.22,77.84±0.32%的抑制潜力相对高于62.5µg/mL时的标准加兰他敏,在IC50时为74.10±0.90。化合物6((E)-4((苯基亚氨基)甲基)苯甲醛)在1000µg/mL浓度下的丁酰胆碱酯酶活性显示出75.83±1.07%的抑制潜力,这与标准化合物在62.5µg/mL的浓度下的75.45±0.90%的丁酰胆碱酯酶抑制活性相似。
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6 weeks
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