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 2017 , Vol 21 , Issue 1
The Synthesis and Evaluation of Anti-Acetylcholinesterase Activity of Some 4(3H)-Quinazolinone Derivatives Bearing Substituted 1,3,4- Thiadiazole
Mine Uraz1, Sevgi Karakuş1, Usama Abu Mohsen2, Zafer Asım Kaplancıklı3, Sevim Rollas1
1Department of Pharmaceutical Chemistry, Marmara University, Faculty of Pharmacy, Istanbul, Turkey
2Department of Pharmaceutical Chemistry, Al-Azhar University, Faculty of Pharmacy,Gaza, Palestine
3Department of Pharmaceutical Chemistry, Anadolu University, Faculty of Pharmacy, Eskişehir, Turkey
DOI : 10.12991/marupj.259886 In the present study, a series of 4(3H)-quinazolinone derivatives (5a-f) were synthesized through the cylization reaction of substituted 1,3,4-thiadiazoles containing an aromatic primary amin and anthranilic acid in the presence of acetic anhydride and acetic acid. The structures of the synthesized compounds were confirmed by elemental analysis, IR, 1H-NMR and mass spectroscopic (5b and 5f) methods. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman"s spectrophotometric method. Compounds 2-methyl-3-{4-[5-(ethylamino)-1,3,4-thiadiazol- 2-yl]phenyl}quinazolin-4(3H)-one (5b) and 2-methyl-3-{4-[5- (cyclohexylamino)-1,3,4-thiadiazol-2-yl]phenyl}quinazolin- 4(3H)-one (5d) can be identified as promising anticholinesterase agents due to their inhibitory effect when compared with donepezil as a reference drug. Keywords : 4(3H)-Quinazolinone, 1,3,4-thiadiazole, antiacetylcholinesterase activity
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