Publication: The synthesis and evaluation of anti-acetylcholinesterase activity of some 4(3H)-quinazolinone derivatives bearing substituted 1,3,4- thiadiazole
Loading...
Date
2017
Journal Title
Journal ISSN
Volume Title
Publisher
Abstract
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, 1
H-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.
Description
Keywords
4(3H)-Quinazolinone, 1,3,4-thiadiazole, antiacetylcholinesterase activity.