期刊
BIOORGANIC CHEMISTRY
卷 77, 期 -, 页码 586-592出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.01.033
关键词
Synthesis; Coumarin; alpha-Glucosidase inhibition; Molecular docking study; SAR
资金
- Ministry of Higher Education (MOHE) [FRGS/1/2015/SG05/UiTM/02/6]
- Universiti Teknologi MARA [600-RMI/FRGS 5/3 (135/2015)]
We have synthesized seventeen Coumarin based derivatives (1-17), characterized by (HNMR)-H-1, (CNMR)-C-13 and EI-MS and evaluated for alpha-glucosidase inhibitory potential. Among the series, all derivatives exhibited outstanding alpha-glucosidase inhibition with IC50 values ranging between 1.10 +/- 0.01 and 36.46 +/- 0.70 mu M when compared with the standard inhibitor acarbose having IC50 value 39.45 +/- 0.10 mu M. The most potent derivative among the series is derivative 3 having IC50 value 1.10 +/- 0.01 mu M, 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. (C) 2018 Elsevier Inc. All rights reserved.
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