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

Authors : Mehtap TUĞRAK SAKARYA, Halise İnci GÜL, Cem YAMALI, Parham TASLIMI, Tugba TASKIN TOK

Pages : 385-424

Doi:10.18596/jotcsa.1111172

View : 99 | Download : 127

Publication Date : 2023-05-31

Article Type : Research Paper

Abstract :Alzheimer\`s disease insert ignore into journalissuearticles values(AD); and diabetes mellitus insert ignore into journalissuearticles values(DM); are related to abnormal changes in enzyme activity. While acetylcholinesterase insert ignore into journalissuearticles values(AChE); and butyrylcholinesterase insert ignore into journalissuearticles values(BChE); are the primary targets in the treatment of Alzheimer\`s disease insert ignore into journalissuearticles values(AD);, α-glucosidase insert ignore into journalissuearticles values(α-Gly); and α-amylase insert ignore into journalissuearticles values(α-Amy); enzymes are known for diabetes mellitus insert ignore into journalissuearticles values(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, Alzheimers disease, Diabetes Mellitus, Molecular Docking, Synthesis