ISSN print edition: 0366-6352
ISSN electronic edition: 1336-9075
Registr. No.: MK SR 9/7
Discovery of 3-(1H-indol-5-yl)-1,2,4-oxidizable derivatives as non-competitive α-glucosidase inhibitors
Zhang, Juan, Ge, Yong-Xi, Fang, Lei, Zhu, Kong-Kai, Liu, Shan-Kui, Wang, Kai-Ming, Jiang, and Cheng-Shi
School of Biological Science and Technology, University of Jinan, Jinan, China
Received: 14 November 2020 Accepted: 28 April 2021
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.
Chemical Papers 75 (9) 4661–4667 (2021)