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Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer-s disease

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dc.contributor.authorKurt, BELMA
dc.contributor.authorGazioglu, IŞIL
dc.contributor.authorBASILE, Livia
dc.contributor.authorSonmez, Fatih
dc.contributor.authorGINEX, Tiziana
dc.contributor.authorKucukislamoglu, Mustafa
dc.contributor.authorGUCCIONE, Salvatore
dc.contributor.institutionauthorZENGİN KURT, BELMA
dc.contributor.institutionauthorGAZİOĞLU, IŞIL
dc.date.accessioned2019-10-05T21:14:30Z
dc.date.available2019-10-05T21:14:30Z
dc.date.issued2015-09-18
dc.description.abstractNew benzofuranylthiazole derivatives containing the aryl urea moiety were synthesized and evaluated in vitro as dual acetylcholinesterase (AChE)-butyrylcholinesterase (BuChE) inhibitors. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were assayed. The result showed that all the synthesized compounds exhibited inhibitory activity on both AChE and BuChE with 1-(4-(5-bromobenzofuran-2-yl)thiazol-2-yl)-3-(2fluorophenyl)urea (e25, IC50 value of 3.85 mu M) and 1-(4-iodophenyl)-3-(4-(5-nitrobenzofuran-2-yl) thiazol-2-yl)urea (e38, IC50 value of 2.03 mu M) as the strongest inhibitors against AChE and BuChE, respectively. Compound e38 was 8.5-fold more potent than galanthamine. The selectivity index of e25 and e38 was 2.40 and 0.37 against AChE and BuChE, respectively. Compound e2, e4 and ell (IC50 = 0.2, 0.5 and 1.13 mu M, respectively) showed a better ABTS cation radical scavenging ability than the standard quercetin (IC50 = 1.18 AM). Best poses of compounds e38 on BuChE and e25 on AChE indicate that the thiazole ring and the amidic moiety are important sites of interaction with both ChEs. In addition, the benzofuran ring and phenyl ring are anchored to the side chains of both enzymes by pi-pi(pi-pi) interactions. (C) 2015 Elsevier Masson SAS. All rights reserved.
dc.identifier10.4174/jkss.2013.84.1.61
dc.identifier.citationKurt B., Gazioglu I., BASILE L., Sonmez F., GINEX T., Kucukislamoglu M., GUCCIONE S., -Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer-s disease-, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.102, ss.80-92, 2015
dc.identifier.pubmed26244990
dc.identifier.urihttps://hdl.handle.net/20.500.12645/6849
dc.language.isoen
dc.titlePotential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer-s disease
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameJOURNAL OF THE KOREAN SURGICAL SOCIETY
local.avesis.idab1f2696-aa29-4f81-aadd-77c15f54d330
local.avesis.response6725
relation.isAuthorOfPublication3fd265b5-fdd8-4c56-949b-deb0303c3db7
relation.isAuthorOfPublication336380d2-70ee-496d-a002-08059f9da500
relation.isAuthorOfPublication.latestForDiscovery336380d2-70ee-496d-a002-08059f9da500
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