Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Email: lddd@benthamscience.org


Synthesis and In vitro Evaluation of Thiadiazole Derivatives as AChE, Bu- ChE and LOX Inhibitors

Author(s): Mehlika Dilek Altintop, Ahmet Ozdemir, Usama Abu Mohsen, Halide Edip Temel, Gulsen Akal n Ciftci and Zafer Asim Kaplancikli

Affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Turkey.

Graphical Abstract:


N'-Benzylidene-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]acetohydrazide derivatives (5a-p) were synthesized to screen for their AChE, BuChE and LOX inhibitory activity. The CCK-8 assay was also carried out to determine their cytotoxicity against NIH/3T3 cells. The most potent AChE inhibitors were found as compounds 5m (49.79% ± 3.08) and 5p (42.39% ± 3.19), whereas the most potent BuChE inhibitor was found as compound 5d (35.15% ± 2.21). Among these derivatives, N'-(3-methoxybenzylidene)-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]acetohydrazide (5p) can be considered as the most promising AChE inhibitor due to its low cytotoxicity to NIH/3T3 cells (IC50 > 500 µg/mL). N'-(4- Methoxybenzylidene)-2-[[5-(phenylamino)-1,3,4-thiadiazol-2-yl]thio]a-cetohydrazide (5n) exhibited weak inhibition on LOX (%20.65 ± 0.08), whilst the other compounds were not active.

Keywords: Acetylcholinesterase, butyrylcholinesterase, lipoxygenase, thiadiazole.

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

Page: [1062 - 1069]
Pages: 8
DOI: 10.2174/1570180811666140529004517