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Design and Synthesis of New Imidazo[1,2-B]Pyrazole Derivatives, in Vitro Α-Glucosidase Inhibition, Kinetic and Docking Studies Publisher Pubmed



Peytam F1 ; Adib M1 ; Shourgeshty R1 ; Mohammadikhanaposhtani M2 ; Jahani M1 ; Imanparast S3 ; Faramarzi MA3 ; Mahdavi M4 ; Moghadamnia AA2, 5 ; Rastegar H6 ; Larijani B4
Authors

Source: Molecular Diversity Published:2020


Abstract

Abstract: A new series of imidazo[1,2-b]pyrazole derivatives 4a–o was designed, synthesized, and screened for in vitro α-glucosidase inhibitory activity. All compounds showed high inhibitory activity in the range of IC50 = 95.0 ± 0.5–372.8 ± 1.0 µM as compared to standard drug acarbose (IC50 = 750 ± 1.5 µM) and were also found to be non-cytotoxic. Among the synthesized compounds, the most potent compound was compound 4j with eightfold higher inhibitory activity compared to acarbose. Like acarbose, compound 4j inhibited α-glucosidase in a competitive mode. Molecular modeling studies of the most potent compounds 4j, 4f, 4o, and 4c were also conducted. © 2019, Springer Nature Switzerland AG.
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