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Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives

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dc.contributor.authorKurt, BELMA
dc.contributor.authorGazioglu, IŞIL
dc.contributor.authorSonmez, Fatih
dc.contributor.authorKucukislamoglu, Mustafa
dc.contributor.institutionauthorZENGİN KURT, BELMA
dc.contributor.institutionauthorGAZİOĞLU, IŞIL
dc.date.accessioned2019-10-05T21:42:46Z
dc.date.available2019-10-05T21:42:46Z
dc.date.issued2015-04-01
dc.description.abstractA newly series of coumarylthiazole derivatives containing aryl urea/thiourea groups were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. The result showed that all the synthesized compounds exhibited inhibitory activity to both cholinesterases. Among them, 1-(4-(8-methoxy-2-oxo-2H-chromen-3-yl)thiazol-2-yl)-3-(4-chlorophenyl)thiourea (f8, IC50 = 4.58 mu M) was found to be the most active compound against AChE, and 1-(4-fluorophenyl)-3-(4-(6-nitro-2-oxo-2H-chromen-3-yl)thiazol-2-yl)urea (e31) exhibited the strongest inhibition against BuChE with IC50 value of 4.93 mu M, which was 3.5-fold more potent than that of galantamine. The selectivity of f8 and e31 were 2.64 and 0.04, respectively. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were investigated for antioxidant activity. Among them, f8, f4 and f6 (IC50 = 1.64, 1.82 and 2.69 mu M, respectively) showed significantly better ABTS cation radical scavenging ability than standard quercetin (IC50 = 15.49 mu M). (C) 2015 Elsevier Inc. All rights reserved.
dc.identifier10.1016/j.urology.2007.04.018
dc.identifier.citationKurt B., Gazioglu I., Sonmez F., Kucukislamoglu M., -Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives-, BIOORGANIC CHEMISTRY, cilt.59, ss.80-90, 2015
dc.identifier.doi10.1016/j.bioorg.2015.02.002
dc.identifier.pubmed25706320
dc.identifier.scopus84923280570
dc.identifier.urihttps://hdl.handle.net/20.500.12645/8026
dc.identifier.wosWOS:000352211900006
dc.language.isoen
dc.titleSynthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameUrology
local.avesis.idc7731c2a-a5fb-415c-926e-521f86485a08
local.avesis.response7902
local.publication.isinternational1
relation.isAuthorOfPublication3fd265b5-fdd8-4c56-949b-deb0303c3db7
relation.isAuthorOfPublication336380d2-70ee-496d-a002-08059f9da500
relation.isAuthorOfPublication.latestForDiscovery336380d2-70ee-496d-a002-08059f9da500
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