Synthesis, Cytotoxicity and In Vitro α-Glucosidase Inhibition of New N-Substituted Glitazone and Rhodanine Derivatives

Tshiluka, N. R.; Bvumbi, Mpelegeng Victoria; Mnyakeni-Moleele, Simon S.

doi:10.1134/s106816202302022x

Cited by 1 publication

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“…α-Glucosidase, a crucial membrane-bound enzyme in the small intestine, is one of the most important therapeutic targets for diabetes [ 5 , 6 , 7 ]. It is responsible for the hydrolysis of glycosidic linkage bonds of carbohydrates, especially disaccharides and polysaccharides, thereby releasing absorbable monosaccharides, which are absorbed to cause postprandial hyperglycemia [ 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

Anti-α-Glucosidase, SAR Analysis, and Mechanism Investigation of Indolo[1,2-b]isoquinoline Derivatives

Liu

et al. 2023

Molecules

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To find potential α-glucosidase inhibitors, indolo[1,2-b]isoquinoline derivatives (1–20) were screened for their α-glucosidase inhibitory effects. All derivatives presented potential α-glucosidase inhibitory effects with IC50 values of 3.44 ± 0.36~41.24 ± 0.26 μM compared to the positive control acarbose (IC50 value: 640.57 ± 5.13 μM). In particular, compound 11 displayed the strongest anti-α-glucosidase activity, being ~186 times stronger than acarbose. Kinetic studies found that compounds 9, 11, 13, 18, and 19 were all reversible mix-type inhibitors. The 3D fluorescence spectra and CD spectra results revealed that the interaction between compounds 9, 11, 13, 18, and 19 and α-glucosidase changed the conformational changes of α-glucosidase. Molecular docking and molecular dynamics simulation results indicated the interaction between compounds and α-glucosidase. In addition, cell cytotoxicity and drug-like properties of compound 11 were also investigated.

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Section: Introductionmentioning

confidence: 99%

Anti-α-Glucosidase, SAR Analysis, and Mechanism Investigation of Indolo[1,2-b]isoquinoline Derivatives

Liu

et al. 2023

Molecules

View full text Add to dashboard Cite

show abstract

Synthesis, Cytotoxicity and In Vitro α-Glucosidase Inhibition of New N-Substituted Glitazone and Rhodanine Derivatives

Cited by 1 publication

References 24 publications

Anti-α-Glucosidase, SAR Analysis, and Mechanism Investigation of Indolo[1,2-b]isoquinoline Derivatives

Anti-α-Glucosidase, SAR Analysis, and Mechanism Investigation of Indolo[1,2-b]isoquinoline Derivatives

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