Editor-in-Chief İlkay Küçükgüzel Associate Editor Aslı Türe Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2020 , Vol 24 , Issue 4
Acetylcholinesterase inhibitory potencies of new pyrazoline derivatives
Mehtap TUĞRAK1,Halise İnci GÜL1,İlhami GÜLÇİN2
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ataturk University, Erzurum, Turkey
2Department of Chemistry, Faculty of Science, Ataturk University, Erzurum, Turkey
DOI : 10.35333/jrp.2020.194 Alzheimer's disease (AD) has no current cure and its mechanism is not fully known, but treatments for symptoms are available. Acetylcholinesterase (AChE) has been reported to be an applicable therapeutic target in patient with AD. Acetylcholinesterase inhibitors (AChEIs) are commonly used for it. For this purpose, novel series of pyrazoline based compounds [2-(3-(4-methoxyphenyl)-5-aryl-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazole, 1-9] were synthesized and AChE inhibitory potencies were reported here. The results indicated that compound 1 (Ki= 0.13±0.004 μM) possessed the highest AChE inhibitory effect in series, which is two times more potent than the reference compound Tacrin (Ki= 0.26±0.045 μM). So, pyrazoline derivative 1 can be considered as a lead inhibitor in designing new AChE inhibitors. Keywords : Acetylcholinesterase; alzheimer disease; benzothiazol; pyrazoline
Marmara University