Journal
BIOORGANIC CHEMISTRY
Volume 71, Issue -, Pages 102-109Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2017.01.017
Keywords
Imidazolylpyrazoles; alpha-Glucosidase inhibition; Diabetes; Multicomponent reaction; Docking
Funding
- Higher Education Commission of Pakistan
- IRSIP
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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. alpha-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. (C) 2017 Elsevier Inc. All rights reserved.
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