Journal
BIOORGANIC CHEMISTRY
Volume 76, Issue -, Pages 273-280Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2017.12.001
Keywords
Synthesis; Oxindole; Oxadiazole; alpha-glucosidase; SAR; Molecular docking study
Funding
- Ministry of Higher Education (MOHE) under Fundamental Research Grant Scheme (FRGS) [FRGS/1/2016/STG01/UiTM/02/2]
- Universiti Teknologi MARA under LESTARI grant [500-RMI/DANA /5/3/ lestari (54/2013)]
- Higher Education Commission, Pakistan under National Research Program for Universities [5721]
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Inhibition of alpha-glucosidase is an effective strategy for controlling post-prandial hyperglycemia in diabetic patients. Beside these alpha-glucosidase inhibitors has been also used as anti-obesity and anti-viral drugs. Keeping in view the greater importance of alpha-glucosidase inhibitors here in this study we are presenting oxindole based oxadiazoles hybrid analogs (1-20) synthesis, characterized by different spectroscopic techniques including H-1 NMR and EI-MS and their alpha-glucosidase inhibitory activity. All compounds were found potent inhibitors for the enzyme with IC50 values ranging between 1.25 +/- 0.05 and 268.36 +/- 4.22 mu M when compared with the standard drug acarbose having IC50 value 895.09 +/- 2.04 mu M. Our study identifies novel series of potent alpha-glucosidase inhibitors and further investigation on this may led to the lead compounds. A structure activity relationship has been established for all compounds. The interactions of the active compounds and enzyme active site were established with the help of molecular docking studies. (C) 2017 Elsevier Inc. All rights reserved.
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