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The synthesis and evaluation of anti-acetylcholinesterase activity of some 4(3H)-quinazolinone derivatives bearing substituted 1,3,4- thiadiazole

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dc.contributor.authorKARAKUŞ, SEVGİ
dc.contributor.authorsUraz, Mine; Karakus, Sevgi; Abu Mohsen, Usama; Kaplancikli, Zafer Asim; Rollas, Sevim
dc.date.accessioned2022-03-14T08:27:51Z
dc.date.available2022-03-14T08:27:51Z
dc.date.issued2016-09-09
dc.description.abstractIn 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, H-1-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} quinazolin4(3H)-one (5d) can be identified as promising anticholinesterase agents due to their inhibitory effect when compared with donepezil as a reference drug.
dc.identifier.doi10.12991/marupj.259886
dc.identifier.issn1309-0801
dc.identifier.urihttps://hdl.handle.net/11424/241828
dc.identifier.wosWOS:000391177500012
dc.language.isoeng
dc.publisherMARMARA UNIV, FAC MEDICINE
dc.relation.ispartofMARMARA PHARMACEUTICAL JOURNAL
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subject4(3H)-Quinazolinone
dc.subject1,3,4-thiadiazole
dc.subjectanti-acetylcholinesterase activity
dc.subjectVITRO ANTITUMOR-ACTIVITY
dc.subjectACETYLCHOLINESTERASE
dc.subjectQUINAZOLINE
dc.subjectINHIBITORS
dc.titleThe synthesis and evaluation of anti-acetylcholinesterase activity of some 4(3H)-quinazolinone derivatives bearing substituted 1,3,4- thiadiazole
dc.typearticle
dspace.entity.typePublication
local.avesis.idd502cc18-d29f-4cea-bf24-83f423fc9cf8
local.import.packageSS16
local.indexed.atWOS
local.indexed.atSCOPUS
local.indexed.atTRDIZIN
local.journal.numberofpages6
oaire.citation.endPage101
oaire.citation.issue1
oaire.citation.startPage96
oaire.citation.titleMARMARA PHARMACEUTICAL JOURNAL
oaire.citation.volume21
relation.isAuthorOfPublicationc93b8083-3f67-4147-bd81-8587eaba18ad
relation.isAuthorOfPublication.latestForDiscoveryc93b8083-3f67-4147-bd81-8587eaba18ad

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