Journal
BIOORGANIC CHEMISTRY
Volume 80, Issue -, Pages 36-42Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.05.021
Keywords
Synthesis; alpha-amylase; Indole; SAR. Thiourea; Docking studies
Funding
- Ministry of Higher Education, Malaysia (MOHE) through the TRG [600-RMI/TRGS5/3 (1/2014)-3]
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In search of potent a-amylase inhibitor we have synthesized eighteen indole analogs (1-18), characterized by NMR and HR-EIMS and screened for alpha-amylase inhibitory activity. All analogs exhibited a variable degree of alpha-amylase inhibition with IC50 values ranging between 2.031 +/- 0.11 and 2.633 +/- 0.05 mu M when compared with standard acarbose having IC50 values 1.927 +/- 0.17 mu M. All compounds showed good alpha-amylase inhibition. Compound 14 was found to be the most potent analog among the series. Structure-activity relationship has been established for all compounds mainly based on bringing about the difference of substituents on phenyl ring. To understand the binding interaction of the most active analogs molecular docking study was performed.
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