Combined In Vitro and Computational Investigations on Synthesized Sulfonamide-Based Antidiabetic Agents

Area of Science:

• Medicinal Chemistry
• Pharmacology

Background:

• Diabetes mellitus is a growing global health concern with increasing prevalence.
• Existing antidiabetic medications can cause long-term adverse effects, necessitating novel therapeutic agents.

Purpose of the Study:

• To synthesize and characterize novel sulfonamide derivatives for potential antidiabetic activity.
• To evaluate the in vitro and in silico antidiabetic potential and safety of synthesized compounds.

Main Methods:

• Synthesis of sulfonamide derivatives via condensation reactions.
• Structural elucidation using spectroscopic methods (IR, 1H-NMR, 13C-NMR).
• In vitro enzyme inhibition assays (α-amylase, α-glucosidase) and cytotoxicity screening.

Main Results:

• Successful synthesis and characterization of sulfonamide derivatives containing amide, azomethine, and sulfonyl groups.
• Most derivatives exhibited excellent safety profiles in cytotoxicity tests.
• The p-TSA-c-d derivative showed potent inhibition of α-amylase and α-glucosidase (IC50 ~46.54 μM), surpassing acarbose.
• Molecular docking studies elucidated enzyme inhibition mechanisms.

Conclusions:

• Synthesized sulfonamide derivatives are promising candidates for novel antidiabetic therapies.
• Further in vivo studies are warranted to explore their therapeutic efficacy.