ADVERTISEMENT

Home|Journals|Articles by Year|Audio Abstracts
 

Original Article



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.




Abstract
Cited by 5 Articles

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.

Key words: Benzamides, Benzothiazole derivatives, Docking, Glucokinase, GK activators, In silico, In vitro GK assay.






Full-text options


Share this Article


Online Article Submission
• ejmanager.com


ejPort - eJManager.com
Author Tools
 About BiblioMed
License Information
Terms & Conditions
Privacy Policy
 Contact Us

The articles in Bibliomed are open access articles licensed under Creative Commons Attribution 4.0 International License (CC BY), which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.