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Design and evaluation of chalconeimine derivatives as ?-amylase inhibitors.

ABSTRACT: Alpha-amylase is a known target for type II diabetes. Therefore, it is of interest to design ?-amylase inhibitors based on hydrazone scaffold. The structure of these hybrids was confirmed by spectroscopic analysis (IR, 1H-and 13C NMR). All the compounds have potential inhibitory properties as shown by in vitro ?-amylase inhibition activity. The compound 5-((1Z,3Z)-3-(benzo[d][1,3]dioxol-5-yl)-3-((2-chloropyridin-3- yl)imino)prop-1-en-1-yl)-2-(difluoromethoxy)phenol(4a) in 100 µg/mL concentration showed a high inhibition of 85.23%. In vitro ?-amylase inhibition was further supported by docking studies of compound against the active site of pig pancreatic ?-amylase (PDB ID: 3L2M). Docking studies revealed that the bonding interactions found between the compound and human pancreatic ?-amylase are similar to those responsible for ?-amylase inhibition by acarbose.

SUBMITTER: Balu P

PROVIDER: S-EPMC6704331 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature

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Design and evaluation of chalconeimine derivatives as α-amylase inhibitors.

Balu Prithivirajan P Jas Jebastin Sonia JS Govindaraj Marimuthu M

Bioinformation 20190731 7

Alpha-amylase is a known target for type II diabetes. Therefore, it is of interest to design α-amylase inhibitors based on hydrazone scaffold. The structure of these hybrids was confirmed by spectroscopic analysis (IR, <sup>1</sup>H-and <sup>13</sup>C NMR). All the compounds have potential inhibitory properties as shown by in vitro α-amylase inhibition activity. The compound 5-((1Z,3Z)-3-(benzo[d][1,3]dioxol-5-yl)-3-((2-chloropyridin-3- yl)imino)prop-1-en-1-yl)-2-(difluoromethoxy)phenol(4a) in 1 ...[more]

PMID: 31485138

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