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