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Discovery of 3-(1H-indol-5-yl)-1,2,4-oxidizable derivatives as non-competitive α-glucosidase inhibitors

Juan Zhang, Yong-Xi Ge, Lei Fang, Kong-Kai Zhu, Shan-Kui Liu, Kai-Ming Wang, and Cheng-Shi Jiang

School of Biological Science and Technology, University of Jinan, Jinan, China

 

E-mail: chm_liusk@ujn.edu.cn

Received: 14 November 2020  Accepted: 28 April 2021

Abstract:

In this study, indolyl-1,2,4-oxidizable derivatives were synthesized and in vitro evaluated as new class of non-competitive α-glucosidase inhibitors. Most of the compounds showed better inhibitory activity than reference drug (acarbose), with compound 35 being the most potent inhibitor. Kinetic analysis indicated that compound 35 had non-competitive inhibition on α-glucosidase, and fluorescence quenching experiment confirmed the direct binding of 35 to α-glucosidase. Besides, some selected compounds had no effect on cell viability of human normal hepatocyte (LO2) and human liver cancer (HepG2) cells. Thus, this work provides a new chemotype for developing novel drugs against type 2 diabetes.

Keywords: Indolyl-1,2,4-oxadiazole; Α-glucosidase inhibitor; Non-competitive; Cytotoxicity; Diabetes

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-021-01687-8

 

Chemical Papers 75 (9) 4661–4667 (2021)

Monday, February 26, 2024

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