Design, Synthesis and Antidiabetic Activity of Novel Sulfamoyl Benzamide Derivatives as Glucokinase Activators

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.

  • Page Number : 115-124
  • Keywords
    Antidiabetic activity, Benzamides, Diabetes mellitus, Glucokinase, GK activators, Molecular Docking
  • DOI Number
    10.15415/jptrm.2018.62008
  • Authors
    • Ajmer Singh GrewalChitkara College of Pharmacy, Chitkara University, Rajpura, 140401, Punjab, India
    • Kapil SharmaJan Nayak Ch. Devi Lal Memorial College of Pharmacy, Sirsa, 125055, Haryana, India
    • Sukhbir SinghChitkara College of Pharmacy, Chitkara University, Rajpura, 140401, Punjab, India
    • Vikramjeet SinghDepartment of Pharmaceutical Sciences, GJUS&T, Hisar, 125001, Haryana, India
    • Deepti PanditaAmity Institute of Molecular Medicine & Stem Cell Research, Amity University, Noida, 201303, Uttar Pradesh, India
    • Viney LatherAmity Institute of Pharmacy, Amity University, Noida, 201303, Uttar Pradesh, India

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  • Published Date : 2018-11-02