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dc.contributor.authorEkiz, Makbule
dc.contributor.authorTutar, Ahmet
dc.contributor.authorÖkten, Salih
dc.contributor.authorBütün, Burcu
dc.contributor.authorKoçyiğit, Ümit M.
dc.contributor.authorTaslimi, Parham
dc.contributor.authorTopçu, Gülaçtı
dc.date.accessioned2019-05-06T13:16:32Z
dc.date.available2019-05-06T13:16:32Z
dc.date.issued2018-09
dc.identifier.urihttps://onlinelibrary.wiley.com/doi/full/10.1002/ardp.201800167
dc.identifier.urihttp://hdl.handle.net/11772/1153
dc.description.abstractWe report the synthesis of bromoindenoquinolines (15a-f) by Friedlander reactions in low yields (13-50%) and the conversion of the corresponding phenyl-substituted indenoquinoline derivatives 16-21 in high yields (80-96%) by Suzuki coupling reactions. To explore the structure-activity relationship (SAR), their inhibition potentials to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase cyctosolic (hCA I and II) enzymes were determined. Monophenyl (16-18) indenoquinolines significantly inhibited the AChE and BChE enzymes in ranges of IC50 37-57nM and 84-93nM, respectively, compared with their starting materials 15a-c and reference compounds (galanthamine and tacrine). On the other hand, these novel arylated indenoquinoline-based derivatives were effective inhibitors of the BChE, hCA I and II, BChE and AChE enzymes with K-i values in the range of 37 +/- 2.04 to 88640 +/- 1990nM for AChE, 120.94 +/- 37.06 to 1150.95 +/- 304.48nM for hCA I, 267.58 +/- 98.05 to 1568.16 +/- 438.67nM for hCA II, and 84 +/- 3.86 to 144120 +/- 2910nM for BChE. As a result, monophenyl indenoquinolines 16-18 may have promising anti-Alzheimer drug potential and 3,8-dibromoindenoquinoline amine (15f) can be novel hCA I and hCA II enzyme inhibitors.en_US
dc.language.isoengen_US
dc.publisherWileyen_US
dc.relation.isversionof10.1002/ardp.201800167en_US
dc.rightsinfo:eu-repo/semantics/restrictedAccessen_US
dc.subjectSARen_US
dc.subjectAcetylcholinesteraseen_US
dc.subjectBromoindenoquinolinesen_US
dc.subjectButyrylcholinesteraseen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectEnzyme inhibitionen_US
dc.subjectPhenyl indenoquinolinesen_US
dc.titleSynthesis, characterization, and SAR of arylated indenoquinoline‐based cholinesterase and carbonic anhydrase inhibitorsen_US
dc.typearticleen_US
dc.relation.journalArchiv der Pharmazieen_US
dc.contributor.departmentBartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümüen_US
dc.identifier.volume351en_US
dc.identifier.issue9en_US
dc.identifier.startpagee1800167en_US


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