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2,4-Dinitrophenyl hydrazone derivatives as potent alpha amylase inhibitors
Indian Journal of Chemistry, Section B ( IF 0.456 ) Pub Date : 2021-02-11
Muhammad Yousaf, Amir Hassan, Shakeel Ahmad, M Idrees, M Adil, Huma Zia, Mirajul Haq, Shah Faisal, Kainat

In our current study thirteen new 2,4-dinitrophenyl hydrazone derivatives 1–13 have been evaluated for alpha amylase activity. The molecular docking results indicate that compounds potentially bind in the catalytic site of the enzyme with excellent result. Molecular Operating Environment (MOE) software was used for docking study. 2,4-Dinitrophenyl hydrazone 1-13 have been obtained under reflux conditions by reacting dinitrophenyl hydrazine in methanol with different aromatic as well as aliphatic aldehydes in the presence of acetic acid act as a catalyst. The current results have shown that compounds 5 (IC50 =12.16µg/mL), 6 (IC50 =15.03µg/mL), and 12 (IC50 =16.42 µg/mL) have been found to be the more potent alpha amylase inhibitors as compared to the standard acarbose (IC50 = 42.47µg/mL). These compounds may provide better leads for alpha amylase inhibitor and further assessment of these compounds can be of great help in the discovery of new antidiabetic drugs.

中文翻译:

2,4-二硝基苯基衍生物作为有效的α淀粉酶抑制剂

在我们目前的研究中,已经评估了13种新的2,4-二硝基苯基衍生物1-13的α淀粉酶活性。分子对接结果表明化合物潜在地结合在酶的催化位点,具有优异的结果。分子操作环境(MOE)软件用于对接研究。通过在甲醇中使二硝基苯基肼在甲醇中与不同的芳族以及脂族醛在乙酸的存在下反应,在回流条件下获得了2,4-二硝基苯基1-13。目前的结果表明,化合物5(IC 50 = 12.16 µ g / mL),化合物6(IC 50与标准阿卡波糖(IC 50 = 42.47 µg / mL)相比,已发现15 mg (= 15.03 µg / mL)和12种(IC 50 = 16.42 µg / mL)是更有效的α淀粉酶抑制剂。这些化合物可能为α淀粉酶抑制剂提供更好的线索,进一步评估这些化合物可能对发现新的抗糖尿病药物有很大帮助。
更新日期:2021-02-11
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