Abstract: In this study, we synthesized benzodioxol carboxamide derivatives and investigated their
antidiabetic potential. The synthesized compounds (Ia-Ic and IIa-IId) underwent characterization
via HRMS, 1H-, 13CAPT-NMR, and MicroED. Their efficacy against -amylase was assessed
in vitro, while MTS assays were employed to gauge cytotoxicity across cancer and normal cell lines.
Additionally, the antidiabetic impact of compound IIc was evaluated in vivo using a streptozotocininduced
diabetic mice model. Notably, IIa and IIc displayed potent alpha-amylase inhibition (IC50
values of 0.85 and 0.68 uM, respectively) while exhibiting a negligible effect on the Hek293t
normal cell line (IC50 > 150 uM), suggesting their safety. Compound IId demonstrated significant
activity against four cancer cell lines (26–65 uM). In vivo experiments revealed that five doses of IIc
substantially reduced mice blood glucose levels from 252.2 mg/dL to 173.8 mg/dL in contrast to
the control group. The compelling in vitro anticancer efficacy of IIc and its safety for normal cells
underscores the need for further in vivo assessment of this promising compound. This research
highlights the potential of benzodioxol derivatives as candidates for the future development of
synthetic antidiabetic drugs.

Title

Biomolecules

Publisher

Multidisciplinary Digital Publishing Institute (MDPI)

Publisher Country

Switzerland

Indexing

Thomson Reuters

Impact Factor

5.5

Publication Type

Prtinted only

Volume

13

Year

2023

Pages

1-16