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

ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)

Volume 14, 12 Issues, 2017

Download PDF Flyer

Letters in Drug Design & Discovery

This journal supports open access

Aims & ScopeAbstracted/Indexed in

Submit Abstracts Online Submit Manuscripts Online

G. Perry
University of Texas
San Antonio, TX

View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 0.974
5 - Year: 2.25

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

Letters in Drug Design & Discovery, 11(9): 1062-1069.

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.


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.


Acetylcholinesterase, butyrylcholinesterase, lipoxygenase, thiadiazole.

Purchase Online Order Reprints Order Eprints Rights and Permissions

Article Details

Volume: 11
Issue Number: 9
First Page: 1062
Last Page: 1069
Page Count: 8
DOI: 10.2174/1570180811666140529004517
Price: $58

Related Journals

Webmaster Contact: Copyright © 2016 Bentham Science