@article{article_187280, title={Some urea and thiourea derivatives bearing 1,2,4-triazole ring and their antiacetylcholinesterase activities}, journal={Clinical and Experimental Health Sciences}, volume={4}, pages={85–89}, year={2014}, DOI={10.5455/musbed.20140326030221}, author={Abu Mohsen, Usama and Kocyigit-kaymakcioglu, Bedia and Celen, Ahmet Ozgur and Kaplancikli, Zafer Asim}, keywords={Urea, thiourea, 1, 2, 4-triazole, anti-acetylcholinesterase activity}, abstract={<span>Objective: </span> <span> Twenty different urea and thiourea derivatives were synthesized and evaluated for their ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman’s spectrophotometric method.  </span> <br /> <br /> <span>Methods: </span> <span> Anti-acetylcholinesterase activity was evaluated by using a modification of Ellman’s spectrophotometric method. The spectrophotometric method is based on the reaction of released thiocholine to give a coloured product with a chromogenic reagent 5,5-dithio-bis-(2-nitrobenzoic acid). </span> <br /> <br /> <span>Results: </span> <span> The anti-acetylcholinesterase effects of the compounds (1a-e, 2a-e, 3a-e and 4a-4e) were determined by modified Ellman’s spectrophotometric method. Among these compounds, (4-{[(4-trifluoromethylphenyl)carbamoyl]amino}phenyl)acetic acid (1d), was found as the most active compound. The inhibition percentages were calculated 48.55% at 0.1 mM concentrations for compound 1d.  </span> <br /> <br /> <span>Conclusion: </span> <span> The anti-acetylcholinesterase activity screening indicated that among the tested compounds, 1d bearing 4-trifluoromethyl group on the phenyl ring, showed noteworthy anti-acetylcholinesterase activity. Based on the activity results, it appears that halogen atoms on the phenyl ring have made good contribution to the anti-acetylcholinesterase activity. </span>}, number={2}, publisher={Marmara University}