AI Article Synopsis

  • Diabetes, characterized by high blood sugar levels (hyperglycemia), can lead to serious health issues like blood vessel and nerve damage if uncontrolled.
  • Researchers synthesized a new series of indoline-2,3-dione-based benzene sulfonamide derivatives and tested their effectiveness against enzymes α-glucosidase and α-amylase, which are linked to glucose metabolism.
  • Among 16 compounds, three demonstrated strong inhibitory effects with IC values closely comparable to the standard drug acarbose, suggesting these derivatives could be promising candidates for diabetes treatment.

Article Abstract

Diabetes is also known as a critical and noisy disease. Hyperglycemia, that is, increased blood glucose level is a common effect of uncontrolled diabetes, and over a period of time can cause serious effects on health such as blood vessel damage and nervous system damage. However, many attempts have been made to find suitable and beneficial solutions to overcome diabetes. Considering this fact, we synthesized a novel series of indoline-2,3-dione-based benzene sulfonamide derivatives and evaluated them against α-glucosidase and α-amylase enzymes. Out of the synthesized sixteen compounds (), only three compounds showed better results; the IC value was in the range of 12.70 ± 0.20 to 0.90 ± 0.10 μM for α-glucosidase against acarbose 11.50 ± 0.30 μM and 14.90 ± 0.20 to 1.10 ± 0.10 μM for α-amylase against acarbose 12.20 ± 0.30 μM. Among the series, only three compounds showed better inhibitory potential such as analogues (0.90 ± 0.10 μM for α-glucosidase and 1.10 ± 0.10 μM for α-amylase), (1.10 ± 0.10 μM for α-glucosidase and 1.30 ± 0.10 μM for α-amylase), and (1.20 ± 0.10 μM for α-glucosidase and 1.60 ± 0.10 μM for α-amylase). Molecular modeling was performed to determine the binding affinity of active interacting residues against these enzymes, and it was found that benzenesulfonohydrazide derivatives can be indexed as suitable inhibitors for diabetes mellitus.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10157847PMC
http://dx.doi.org/10.1021/acsomega.3c01130DOI Listing

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