Work

Design, Synthesis and Cholinesterase Inhibitory Activity of Novel 1,3,4-Thiadiazole Derivatives

Year: 2024

Type: article

Abstract: Inhibition of the cholinesterases (AChE and BChE) plays a pivotal role in the symptomatic treatment of Alzheimer’s disease. The present study reports the synthesis and anticholinesterase activity of five novel thiadiazole analogs in search of anti-Alzheimer agents. The structures of the newly synthesized compounds were characterized using 1H NMR, 13C NMR and HRMS. Tested compounds inhibited acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes with IC50 values in the range of 8.250-20.382 μM and 14.143-0.986 μM, respectively. N-(4-Chlorophenyl)-2-[(5-(allylamino)-1,3,4-thiadiazol-2-yl)thio]-N-(3-nitrobenzyl)acetamide (6e) was determined as the most potent inhibitor against both tested enzymes when compared with standard drug tacrine. Molecular docking study was carried out to reveal the binding interactions between compound 6e and the active site of AChE

Source: Cumhuriyet Science Journal

DOI: 10.17776/csj.1449622

Authors: Betül Kaya, Ulviye Acar Çevik, Bilge Çiftci, Mesut Isık, Zafer Asım Kaplancıklı, Şükrü Beydemir

Institutions: Zonguldak Bülent Ecevit University, Anadolu University, Bilecik Şeyh Edebali Üniversitesi

Language: English

Topic: Cholinesterase and Neurodegenerative Diseases

Subfield: Pharmacology

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: diamond

Funder: Anadolu Üniversitesi