Synthesis of novel substituted quinoline derivatives as diabetics II inhibitors and along with their in-silico studies

In this article, 26 compounds of substituted quinoline derivatives were synthesized and their alpha- glucosidase inhibition activity against the alpha-glucosidase enzyme was investigated. The screening results revealed that most of the synthesized substituted quinoline compounds demonstrated moderate to very good alpha-glucosidase inhibitory activity when compared to the first-line drug Acarbose (standard). The IC50 values were obtained in the range of 21.71-375.00 mu M. Amongst the substituted functionalized quinoline derivatives, compounds 10b, 10d, 11c-11d, 17b-17c , and 18c-18d displayed very promising results. The single crystal X-ray diffraction of compound 12 unambiguously confirmed its structure. This study has unravelled a new series of substituted quinoline derivatives as good inhibitors of alpha-glucosidase enzyme. All the active hits were docked in the active site of alpha-glucosidase to investigate their mode of bind-ing. We conclude that the newly introduced substituents are important for interaction affecting as they demonstrate the potential of these compounds for alpha-glucosidase inhibitors.(c) 2022 Elsevier B.V. All rights reserved.

Automated summary

In this study, 26 compounds of substituted quinoline derivatives were synthesized and their alpha-glucosidase inhibition activity was investigated. Most of the synthesized compounds showed good inhibitory activity against alpha-glucosidase, and some exhibited very promising results. Compound 12's structure was confirmed through single crystal X-ray diffraction. The study revealed a new series of substituted quinoline derivatives as potential inhibitors of alpha-glucosidase.