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Title: Design, Synthesis and Antidiabetic Activity of Novel Sulfamoyl Benzamide Derivatives as Glucokinase Activators
Authors: Grewal, Ajmer Singh
Sharma, Kapil
Singh, Sukhbir
Singh, Vikramjeet
Pandita, Deepti
Lather, Viney
Keywords: Antidiabetic activity
Diabetes mellitus
GK activators
Molecular Docking
Issue Date: 2-Nov-2018
Publisher: Chitkara University Publications
Abstract: The present work has been planned to design, synthesize and evaluate the antidiabetic potential of a series of sulfamoyl benzamide derivatives as potential glucokinase (GK) activators. A new series of sulfamoyl benzamide derivatives was synthesized starting from 3-nitrobenzoic acid and characterized. In silico docking studies were performed to determine the binding interactions for the best fit conformations in the allosteric site of GK enzyme. Based on the results of in silico studies, the selected molecules were tested for their antidiabetic activity in animal studies (alloxan induced diabetic animal model). Compound 7 exhibited highest antidiabetic activity in animal studies. The results of in vivo antidiabetic activity studies were found to be in parallel to that of docking studies. These newly synthesized sulfamoyl benzamide derivatives thus can be treated as the initial hits for the development of novel, safe, effective and orally bioavailable GK activators as therapeutic agents for the treatment of type 2 diabetes.
ISSN: Print 2321-2217
Online 2321-2225
Appears in Collections:JPTRM Volume 6 Number 2 (November - 2018)

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