Journal
BIOORGANIC CHEMISTRY
Volume 72, Issue -, Pages 248-255Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2017.04.010
Keywords
Synthesis; Indole scaffold; Alpha amylase inhibition; Molecular docking; SAR
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 [600-RMI/DANA/5/3/lestari (54/2013)]
- Higher Education Commission of Pakistan under the National Research Program for Universities [5721]
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Twenty five derivatives of indole carbohydrazide (1-25) had been synthesized. These compounds were characterized using H-1 NMR and EI-MS, and further evaluated for their a-amylase inhibitory potential. The analogs (1-25) showed varying degree of alpha-amylase inhibitory potential. ranging between 9.28 and 599.0 mu M when compared with standard acarbose having IC50 value 8.78 +/- 0.16 mu M. Six analogs, 25 (IC50 = 9.28 +/- 0.153 mu M), 22 (IC50 = 9.79 +/- 0.43 mu M), 4 (IC50 = 11.08 +/- 0.357 mu M), 1 (IC50 = 12.65 +/- 0.169 mu M), 8 (IC50 = 21.37 +/- 0.07 mu M) and 14 (IC50 = 43.21 +/- 0.14 mu M) showed potent alpha-amylase inhibition as compared to the standard acarbose (IC50 = 8.78 +/- 0.16 mu M). All other analogs displayed good to moderate inhibitory potential. Structure-activity relationship was established through the interaction of the active compounds with enzyme active site with the help of docking studies. (C) 2017 Elsevier Inc. All rights reserved.
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