Synthesis, Docking and Antidiabetic Activity of Some Newer Benzamide Derivatives as Potential Glucokinase Activators

Title:Synthesis, Docking and Antidiabetic Activity of Some Newer Benzamide Derivatives as Potential Glucokinase Activators

Volume: 14 Issue: 5

Author(s): Rohit Singh, Viney Lather*, Deepti Pandita, Vikramjeet Judge, Karthikeyan N. Arumugam and Ajmer Singh Grewal

Affiliation:

• Department of Pharmaceutical Chemistry, JCDM College of Pharmacy, Sirsa, 125055,India

Keywords: Antidiabetic activity, benzamides, type 2 diabetes, glucokinase, glucokinase activators.

Abstract: Background: Glucokinase activators (GKAs) are the new class of candidate drugs which act on glucokinase (GK) enzyme and show their hypoglycaemic activity.

Objective: The present work was planned to synthesize and evaluate the antidiabetic activity of a series of newer benzamide derivatives as potential GKAs.

Method: This work involved synthesis of newer benzamide derivatives from benzoic acid and their evaluation by docking studies to determine the binding interactions for the best fit conformations in the binding site of GK enzyme. Based on the results of docking studies, the selected molecules were tested for their antidiabetic activity in the animal model.

Results: Amongst the synthesized molecules, compounds 14 and 20 with phenyl-substituted thiazole moiety on amide nitrogen, exhibited highest activity in vivo. The results of the in vivo antidiabetic studies were found to be consistent with those of docking studies.

Conclusion: These newly synthesized molecules thus can be treated as the initial hits for the development of new, safe, effective and orally bioavailable GKAs as therapeutic agents for the treatment of diabetic disorders.

Cite this article as:

Singh Rohit, Lather Viney*, Pandita Deepti, Judge Vikramjeet, Arumugam N. Karthikeyan and Grewal Singh Ajmer, Synthesis, Docking and Antidiabetic Activity of Some Newer Benzamide Derivatives as Potential Glucokinase Activators, Letters in Drug Design & Discovery 2017; 14 (5) . https://dx.doi.org/10.2174/1570180813666160819125342

DOI https://dx.doi.org/10.2174/1570180813666160819125342	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X