Research Article | Volume: 11, Supplement 1, March, 2021

Design, synthesis, and evaluation of some novel N-benzothiazol-2-yl benzamide derivatives as allosteric activators of human glucokinase

Sandeep Arora Ajmer Singh Grewal Neelam Sharma Kunal Arora Ervon Dhalio Sukhbir Singh   

Open Access   

Published:  Feb 11, 2021

DOI: 10.7324/JAPS.2021.11s104

Some newer benzamide analogues of N-benzothiazol-2-yl were prepared and assessed for human glucokinase (GK) activation accompanied by molecular docking investigations for predicting the bonding connections of the these derivatives with residues in the allosteric site of GK. Among the derivatives synthesized, 6 and 7 strongly increased the catalytic action of GK (GK activation fold about 2.0 compared to control) in vitro. The outcomes of in vitro assay were supported by the molecular docking investigations of these analogues with allosteric site residues of the GK protein. Derivatives investigated in the present study can afford few lead compounds for the discovery of harmless and strong allosteric GK activating compounds for the management of type 2 diabetes.

Keyword:     Benzamides benzothiazole derivatives docking glucokinase GK activators in silico GK assay


Arora S, Grewal AS, Sharma N, Arora K, Dhalio E, Singh S. Design, synthesis, and evaluation of some novel N-benzothiazol-2-yl benzamide derivatives as allosteric activators of human glucokinase. J Appl Pharm Sci, 2021; 11 (Supp 1):038–047.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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