| Literature DB >> 28482265 |
Tayyaba Noreen1, Muhammad Taha2, Syahrul Imran3, Sridevi Chigurupati4, Fazal Rahim5, Manikandan Selvaraj6, Nor Hadiani Ismail3, Jahidul Islam Mohammad7, Hayat Ullah5, Muhammad Tariq Javid5, Faisal Nawaz8, Maryam Irshad1, Muhammad Ali9.
Abstract
Twenty five derivatives of indole carbohydrazide (1-25) had been synthesized. These compounds were characterized using 1H NMR and EI-MS, and further evaluated for their α-amylase inhibitory potential. The analogs (1-25) showed varying degree of α-amylase inhibitory potential. ranging between 9.28 and 599.0µM when compared with standard acarbose having IC50 value 8.78±0.16µM. Six analogs, 25 (IC50=9.28±0.153µM), 22 (IC50=9.79±0.43µM), 4 (IC50=11.08±0.357µM), 1 (IC50=12.65±0.169µM), 8 (IC50=21.37±0.07µM) and 14 (IC50=43.21±0.14µM) showed potent α-amylase inhibition as compared to the standard acarbose (IC50=8.78±0.16µM). 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.Entities:
Keywords: Alpha amylase inhibition; Indole scaffold; Molecular docking; SAR; Synthesis
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Year: 2017 PMID： 28482265 DOI： 10.1016/j.bioorg.2017.04.010
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275