Synthesis and biological evaluation of some 1-naphthol derivatives as antioxidants, acetylcholinesterase, and carbonic anhydrase inhibitors

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dc.contributor.authorErdogan, Musa
dc.contributor.authorKose, Leyla Polat
dc.contributor.authorEssiz, Selcuk
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2024-03-13T10:30:34Z
dc.date.available2024-03-13T10:30:34Z
dc.date.issued2021
dc.departmentİstanbul Beykent Üniversitesien_US
dc.description.abstractA series of some naphthol derivatives 4a-f, 5a,f, 6a, and 7a,b (six novel ones: 4c,d, 5a, 6a, 7a,b) bearing F, Cl, Br, OMe, and dioxole substituents at different positions of the aromatic rings was designed, synthesized, and characterized. The naphthol derivatives were synthesized in three steps, namely the addition reaction of furan via Diels-Alder cycloaddition reaction, copper(II) trifluoromethanesulfonate (Cu(OTf)(2))-catalyzed aromatization reaction, and the bromination reaction, respectively. The structures of the newly obtained compounds (4c,d, 5a, 6a, 7a,b) were characterized by spectroscopic techniques. In addition, some biological activity studies were investigated under in vitro conditions. Inhibition studies of these compounds were performed on human carbonic anhydrase (hCA) I and II isoenzymes purified from human erythrocytes as a biological evaluation. Moreover, their potential antioxidant and antiradical activities were studied by analytical methods like ABTS(center dot+) and DPPH center dot scavenging, and it was determined that some molecules showed good activity. Also, inhibition of acetylcholinesterase (AChE), which is a marker of many degenerative neurological diseases, was tested and the results were discussed. Excellent enzyme inhibition results were recorded for most of the molecules. These 1-naphthol derivatives were found as effective inhibitors for hCA I, hCA II, and AChE with K-i values ranging from 0.034 +/- 0.54 to 0.724 +/- 0.18 mu M for hCA I, 0.172 +/- 0.02 to 0.562 +/- 0.21 mu M for hCA II, and 0.096 +/- 0.01 to 0.177 +/- 0.02 mu M for AChE.en_US
dc.identifier.doi10.1002/ardp.202100113
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue8en_US
dc.identifier.pmid34080709en_US
dc.identifier.scopus2-s2.0-85107026437en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.1002/ardp.202100113
dc.identifier.urihttps://hdl.handle.net/20.500.12662/3434
dc.identifier.volume354en_US
dc.identifier.wosWOS:000657365200001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofArchiv Der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subject1-naphtholsen_US
dc.subjectacetylcholinesteraseen_US
dc.subjectantioxidant activityen_US
dc.subjectcarbonic anhydraseen_US
dc.titleSynthesis and biological evaluation of some 1-naphthol derivatives as antioxidants, acetylcholinesterase, and carbonic anhydrase inhibitorsen_US
dc.typeArticleen_US

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