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

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

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 5 , 2017

Become EABM
Become Reviewer

Graphical Abstract:


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.

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

Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 14
ISSUE: 5
Year: 2017
Page: [540 - 553]
Pages: 14
DOI: 10.2174/1570180813666160819125342
Price: $65

Article Metrics

PDF: 35
HTML: 3
PRC: 1