Editor-in-Chief İlkay Küçükgüzel Associate Editor Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Marmara Pharmaceutical Journal 2016 , Vol 20 , Issue 1
Synthesis and cholinesterase inhibitory activity of some phenylacetamide derivatives bearing 1H-pyrazole or 1H-1,2,4-triazole
Ayse Hande TARIKOGULLARI1, Murat CIZMECIOGLU1, Merve SAYLAM1, Sulunay PARLAR1, Vildan ALPTUZUN1, Zeynep SOYER1
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ege University, Bornova, Izmir 35100, Turkey DOI : 10.12991/mpj.2016202105828 A group of N-phenylacetamide derivatives bearing five membered heterocyclic rings, pyrazole or 1,2,4-triazole, were synthesized to investigate their cholinesterase inhibitory activities. Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities were evaluated by using Ellman"s spectroscopic method. Results indicated that all of the compounds displayed moderate and selective AChE inhibitory activity and the most active compound was 2-(1H-1,2,4-triazole-1-yl)-N-(3-methoxyphenyl)acetamide with an IC50 value of 6.68 mM. Docking studies were also carried out for the most active compound. Keywords : Alzheimer"s disease, pyrazole, 1,2,4-triazole, acetamide, cholinesterase inhibitory activity
Marmara University