Synthesis and Biological Evaluation of New Dihydrofuro[3,2-Ib/I]piperidine Derivatives as Potent Iα/I-Glucosidase Inhibitors

Inhibition of glycoside hydrolases has widespread application in the treatment of diabetes. Based on our previous findings, a series of dihydrofuro[3,2-b]piperidine derivatives was designed and synthesized from D- and L-arabinose. Compounds 32 (IC[sub.50] = 0.07 μM) and 28 (IC[sub.50] = 0.5 μM) show...

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Published inMolecules (Basel, Switzerland) Vol. 29; no. 5
Main Authors Wang, Haibo, Huang, Xiaojiang, Pan, Yang, Zhang, Guoqing, Tang, Senling, Shao, Huawu, Jiao, Wei
Format Journal Article
LanguageEnglish
Published MDPI AG 01.03.2024
Subjects
Diabetes therapy
Enzymes
Glucose metabolism
Hydrolases
Type 2 diabetes
China
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Summary:Inhibition of glycoside hydrolases has widespread application in the treatment of diabetes. Based on our previous findings, a series of dihydrofuro[3,2-b]piperidine derivatives was designed and synthesized from D- and L-arabinose. Compounds 32 (IC[sub.50] = 0.07 μM) and 28 (IC[sub.50] = 0.5 μM) showed significantly stronger inhibitory potency against α-glucosidase than positive control acarbose. The study of the structure–activity relationship of these compounds provides a new clue for the development of new α-glucosidase inhibitors.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules29051179