| Literature DB >> 28160945 |
Faryal Chaudhry1, Sadia Naureen2, Rahila Huma3, Ayesha Shaukat4, Mariya Al-Rashida5, Nadia Asif2, Mohammad Ashraf6, Munawar Ali Munawar7, Misbahul Ain Khan8.
Abstract
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 IC50 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.Entities:
Keywords: Diabetes; Docking; Imidazolylpyrazoles; Multicomponent reaction; α-Glucosidase inhibition
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Year: 2017 PMID: 28160945 DOI: 10.1016/j.bioorg.2017.01.017
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275