Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors

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dc.contributor.authorGulcan, Hayrettin Ozan
dc.contributor.authorUnlu, Serdar
dc.contributor.authorEsiringu, Ilker
dc.contributor.authorErcetin, Tugba
dc.contributor.authorSahin, Yasemin
dc.contributor.authorOz, Demet
dc.contributor.authorSahin, Mustafa Fethi
dc.date.accessioned2026-02-06T18:37:18Z
dc.date.issued2014
dc.departmentDoğu Akdeniz Üniversitesi
dc.description.abstractHydroxylated 6H-benzo[c]chromen-6-one derivatives (i.e., urolithins) are the main bioavailable metabolites, and biomarkers of ellagitannins present in various nutrition. Although these dietaries, the sources of urolithins, are employed in folk medicine as cognitive enhancer in the treatment of Alzheimer's Disease, urolithins have negligible potential to inhibit acetylcholinesterase and butyrylcholinesterase enzymes, the validated targets of Alzheimer's Disease. Therefore, within this research, a series of 6H-benzo[c]chromen- 6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives has been designed, synthesized, and their biological activities were evaluated as potential acetylcholinesterase and butyrylcholinesterase inhibitors. The compounds synthesized exerted comparable activity in comparison to rivastigmine, galantamine, and donepezil both in in vitro and in vivo studies. (C) 2014 Elsevier Ltd. All rights reserved.
dc.description.sponsorshipScientific and Technological Research Council of Turkey [3100373]
dc.description.sponsorshipThe support provided by Scientific and Technological Research Council of Turkey (i.e., Project No: 3100373) is gratefully acknowledged. The authors also would like to thank Dr. Manfred Windisch, the president of JSW Life Sciences (i.e., a pre-clinical and clinical drug development organization, a member of QPS Clinical Research in Austria), for his guidance in in vivo studies. The authors have declared no conflict of interest.
dc.identifier.doi10.1016/j.bmc.2014.08.016
dc.identifier.endpage5154
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.issue19
dc.identifier.orcid0000-0002-9503-5841
dc.identifier.pmid25189690
dc.identifier.scopus2-s2.0-84907541193
dc.identifier.scopusqualityQ1
dc.identifier.startpage5141
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2014.08.016
dc.identifier.urihttps://hdl.handle.net/11129/12399
dc.identifier.volume22
dc.identifier.wosWOS:000341883700002
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakPubMed
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherPergamon-Elsevier Science Ltd
dc.relation.ispartofBioorganic & Medicinal Chemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_WoS_20260204
dc.subject6H-Benzo[c]chromen-6-ones
dc.subjectAcetylcholinesterase
dc.subjectButyrylcholinesterase
dc.subjectAlzheimer's Disease
dc.subjectPassive avoidance test
dc.titleDesign, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors
dc.typeArticle

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