Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan; Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan.
Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan.
Bioorg Chem. 2019 Feb;82:267-273. doi: 10.1016/j.bioorg.2018.10.047. Epub 2018 Oct 24.
Herein, substituted imidazole-pyrazole hybrids (2a-2n) were prepared via a multi component reaction employing pyrazole-4-carbaldehydes (1a-1d), ammonium acetate, benzil and arylamines as reactants. All the new compounds were characterized through their spectral and elemental analyses. Further these compounds were tested against α-glucosidase enzyme. The compounds 2k, 2l and 2n possessed good inhibition potencies, however, compounds 2f (IC value: 25.19 ± 0.004 μM) and 2m (IC value: 33.62 ± 0.03 μM) were the most effective compounds of the series. Furthermore, molecular docking helped to understand the binding interactions of 2f and 2m with the understudy yeast's α-glucosidase enzyme.
在此,通过多组分反应,使用吡唑-4-甲醛(1a-1d)、乙酸铵、苯偶姻和芳胺作为反应物,制备了取代的咪唑-吡唑杂合体(2a-2n)。所有新化合物均通过光谱和元素分析进行了表征。进一步,这些化合物被测试了对α-葡萄糖苷酶的抑制活性。化合物 2k、2l 和 2n 具有良好的抑制活性,然而,化合物 2f(IC 值:25.19 ± 0.004 μM)和 2m(IC 值:33.62 ± 0.03 μM)是该系列中最有效的化合物。此外,分子对接有助于理解 2f 和 2m 与研究中的酵母α-葡萄糖苷酶的结合相互作用。