Synthesis and In vitro Evaluation of Thiadiazole Derivatives as AChE, Bu- ChE and LOX Inhibitors
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.
Keywords: Acetylcholinesterase, butyrylcholinesterase, lipoxygenase, thiadiazole.
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.
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