含甲基的查耳酮化合物的合成、生物活性研究和分子模型研究

Bedriye Seda Kurşun Aktar
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引用次数: 0

摘要

4-piperazineacetophenone 与带有 CH3 基团的不同醛类进行克莱森-施密特缩合,合成了一系列查尔酮衍生物。考察了合成化合物的抗胆碱酯酶(AChE 和 BChE)抑制活性和抗糖尿病(α-淀粉酶和 α-糖苷酶)抑制活性。化合物 1 是 AChE(16.29±0.44 IC50 µM)、BChE(10.19±0.04 IC50 µM)和α-淀粉酶(105.51±0.24 IC50 µM)抑制活性最强的分子;化合物 5 则是α-葡萄糖苷酶抑制活性最强的分子。对所有分子进行了硅学和分子对接研究。根据分子对接结果,发现所有分子的活性都高于参考化合物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, Biological Activity Studies And Molecular Modeling Studies Of Chalcone Compounds With Methyl Group
A series of chalcone derivatives were synthesized as a result of the Claisen-Schmidt condensation of different aldehydes with CH3 groups with 4-piperazineacetophenone. Anticholinesterase (AChE and BChE) inhibitory activity and antidiabetes (α-amylase and α-glucosidaze) inhibitory activities of the synthesized compounds were examined. While compound 1 is the most active molecule in AChE (16.29±0.44 IC50 µM), BChE (10.19±0.04 IC50 µM) and α-amylase (105.51±0.24 IC50 µM) inhibitor activities; Compound 5 was found to be the most active molecule in α-glucosidase inhibitor activity. In silico and molecular docking studies of all molecules were performed. According to molecular docking results, all molecules were found to be more active than the reference compounds.
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