Molecular docking studies and biological activities of benzenesulfonamide-based thiourea and thiazolidinone derivatives targeting cholinesterases, α-glucosidase, and α-amylase enzymes

Year 2023, Volume: 10 Issue: 2, 385 - 424, 31.05.2023

Mehtap Tuğrak Sakarya , Halise İnci Gül , Cem Yamalı , Parham Taslımı , Tugba Taskın Tok

https://doi.org/10.18596/jotcsa.1111172

Cited By: 1

Abstract

Alzheimer's disease (AD) and diabetes mellitus (DM) are related to abnormal changes in enzyme activity. While acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are the primary targets in the treatment of Alzheimer's disease (AD), α-glucosidase (α-Gly) and α-amylase (α-Amy) enzymes are known for diabetes mellitus (DM). Here, benzenesulfonamide-based thiourea and thiazolidinone derivatives such as AChE, BChE, α-Gly, and α-Amy inhibitors were reported. The results revealed that compounds 1d and 2c showed promising AChE and BChE inhibition effects. Compound 2a was the most potent inhibitor against α-glycosidase and α-amylase, respectively. Molecular docking studies indicated that the lead compounds' binding energy values and molecular interactions were better than that of tacrine and acarbose. The most bioactive compounds may be considered potent leads for further studies.

Keywords

Thiazolidinone, Benzamide, Alzheimer’s disease, Diabetes Mellitus, Molecular Docking, Synthesis

Supporting Institution

Atatürk Üniversitesi

Project Number

Project Number: TAB-8919

Thanks

The authors would like to thank Ataturk University for financial support (Project Number: TAB-8919) and C. Kazaz (Prof. Dr., Ataturk University), B. Anil (Ph.D., Ataturk University), Serkan Levent (M.Sc. Anadolu University) and Mustafa Gul (Prof. Dr. Ataturk University) for their supports

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