| Literature DB >> 29477126 |
Muhammad Taha1, Syed Adnan Ali Shah2, Muhammad Afifi3, Syahrul Imran4, Sadia Sultan3, Fazal Rahim5, Khalid Mohammed Khan6.
Abstract
We have synthesized seventeen Coumarin based derivatives (1-17), characterized by 1HNMR, 13CNMR and EI-MS and evaluated for α-glucosidase inhibitory potential. Among the series, all derivatives exhibited outstanding α-glucosidase inhibition with IC50 values ranging between 1.10 ± 0.01 and 36.46 ± 0.70 μM when compared with the standard inhibitor acarbose having IC50 value 39.45 ± 0.10 μM. The most potent derivative among the series is derivative 3 having IC50 value 1.10 ± 0.01 μM, which are many folds better than the standard acarbose. The structure activity relationship (SAR) was mainly based upon by bring about difference of substituent's on phenyl part. Molecular docking studies were carried out to understand the binding interaction of the most active compounds.Entities:
Keywords: Coumarin; Molecular docking study; SAR; Synthesis; α-Glucosidase inhibition
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Year: 2018 PMID: 29477126 DOI: 10.1016/j.bioorg.2018.01.033
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275