Chaudhry Faryal, Naureen Sadia, Huma Rahila, Shaukat Ayesha, Al-Rashida Mariya, Asif Nadia, Ashraf Mohammad, Munawar Munawar Ali, Khan Misbahul Ain
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. 2017 Apr;71:102-109. doi: 10.1016/j.bioorg.2017.01.017. Epub 2017 Jan 23.
Under three different reaction conditions (conventional heating, microwave irradiations and amino acid catalysis), a series of imidazolylpyrazoles (2a-2k) were synthesized in good to excellent yields from a mixture of three precursors: aryl(hetaryl)pyrazole-4-carbaldehydes (1a-1k), benzil and ammonium acetate. α-Glucosidase inhibition assay revealed a new class of highly potent agents wherein each compound displayed significant inhibitory potentials (in terms of percentage inhibition and relative IC values) as compared to that of the reference drug (Acarbose). Moreover, molecular modelling of most potent compounds 2h, 2j and 2k also helped in understanding the structure and activity relationship.
在三种不同的反应条件（常规加热、微波辐射和氨基酸催化）下，由三种前体：芳基（杂芳基）吡唑-4-甲醛（1a - 1k）、联苯甲酰和醋酸铵的混合物合成了一系列咪唑基吡唑（2a - 2k），产率良好至优异。α-葡萄糖苷酶抑制试验揭示了一类新型的高效药物，其中与参考药物（阿卡波糖）相比，每种化合物都表现出显著的抑制潜力（以抑制百分比和相对IC值衡量）。此外，对最有效的化合物2h、2j和2k进行分子建模也有助于理解结构与活性的关系。
