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k Microwave assisted synthesis of novel hybrid tacrine-sulfonamide derivatives and investigation of their antioxidant and anticholinesterase activities

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dc.contributor.authorUlus, Ramazan
dc.contributor.authorKurt, BELMA
dc.contributor.authorGazioglu, IŞIL
dc.contributor.authorKaya, Muharrem
dc.contributor.institutionauthorZENGİN KURT, BELMA
dc.contributor.institutionauthorGAZİOĞLU, IŞIL
dc.date.accessioned2019-10-05T12:56:55Z
dc.date.available2019-10-05T12:56:55Z
dc.date.issued2017-02-01
dc.description.abstractA novel series of tacrine derivatives containing sulfonamide group were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. The result showed that all the synthesized tacrine-sulfonamides (VIIIa-o) exhibited inhibitory activity on both cholinesterases. VIIIg showed the highest inhibitory activity on AChE IC50 = 0.009 mu M. This value is 220-fold greater than that of galantamine (IC50 = 2.054 mu M) and 6-fold greater than tacrine (IC50 = 0.055 mu M). VIIIf displayed the strongest inhibition of BuChE (IC50 = 2.250 mu M), which is close to donepezil (IC50 = 2.680 mu M) and 8-fold greater than that of galantamine (IC50 = 18.130 mu M) Furthermore, all of the synthesized tacrine derivatives showed higher inhibition of BuChE than that of galantamine. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were investigated for the antioxidant activity. Among them, VIIIb (IC50 = 94.390 +/- 2.310 mu M) showed significantly better ABTS cation radical scavenging ability than all of the new synthesized compounds. (C) 2017 Published by Elsevier Inc.
dc.identifier
dc.identifier.citationUlus R., Kurt B., Gazioglu I., Kaya M., -k Microwave assisted synthesis of novel hybrid tacrine-sulfonamide derivatives and investigation of their antioxidant and anticholinesterase activities-, BIOORGANIC CHEMISTRY, cilt.70, ss.245-255, 2017
dc.identifier.doi10.1016/j.bioorg.2017.01.005
dc.identifier.pubmed28153340
dc.identifier.scopus85010987034
dc.identifier.urihttps://hdl.handle.net/20.500.12645/1000
dc.identifier.wosWOS:000397808700028
dc.language.isoen
dc.titlek Microwave assisted synthesis of novel hybrid tacrine-sulfonamide derivatives and investigation of their antioxidant and anticholinesterase activities
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameINTERNATIONAL OPHTHALMOLOGY
local.avesis.id17407adf-7e6d-4bc1-8c4b-501d4f4c909a
local.avesis.response870
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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