Synthesis and biological evaluation of novel bromophenol derivatives as carbonic anhydrase inhibitors

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dc.authorid0000-0002-7770-0473en_US
dc.contributor.authorAkbaba, Yusuf
dc.contributor.authorBalaydın, Halis Türker
dc.contributor.authorMenzek, Abdullah
dc.contributor.authorGöksu, Süleyman
dc.contributor.authorŞahin, Ertan
dc.contributor.authorEkinci, Deniz
dc.date.accessioned2021-12-07T05:48:34Z
dc.date.available2021-12-07T05:48:34Z
dc.date.issued2013
dc.departmentAÇÜ, Eğitim Fakültesi, Temel Eğitim Bölümüen_US
dc.description.abstractHere, we provide an alternative synthesis of the natural bromophenol 3,4-dibromo-5-(2,3-dibromo-4,5-dihydroxybenzyl)-6-(ethoxymethyl) benzene-1,2-diol (3) and the first synthesis of (4,5-dihydroxy-2methylphenyl)( 3,4-dihydroxyphenyl) methanone (18) and its brominated derivatives 19-21. The compounds were characterized and tested against the two most studied members of the pH regulatory enzyme family, carbonic anhydrase (CA). The inhibitory potencies of the novel compounds and two natural bromophenols 2, 3 were analyzed at the human isoforms hCA I and hCA II as targets and the K-I values were calculated. The K-I values of the novel compounds were measured in the range of 13.7-32.7 mu M for the hCA I isozyme and 0.65-1.26 mu M for the hCA II isozyme. The structurally related compound 14 was also tested in order to understand the structure-activity relationship, and the clinically used sulfonamide acetazolamide (AZA) was tested for comparison reasons. All of the compounds exhibited competitive inhibition with 4-nitrophenylacetate as substrate. The compounds showed strong inhibitory activity against hCA I, being more effective as compared to the clinically used AZA (K-I: 36.2 mu M), but rather less activity against hCA II.
dc.identifier.citationAkbaba, Y., Balaydın, H. T., Menzek, A., Göksu, S., Şahin, E., & Ekinci, D. (2013). Synthesis and biological evaluation of novel bromophenol derivatives as carbonic anhydrase inhibitors. Archiv der Pharmazie, 346(6), 447-454.en_US
dc.identifier.doi10.1002/ardp.201300054
dc.identifier.endpage454en_US
dc.identifier.issue6en_US
dc.identifier.scopusqualityQ1
dc.identifier.startpage447en_US
dc.identifier.urihttps://hdl.handle.net/11494/3587
dc.identifier.volume346en_US
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorBalaydin, Halis Türker
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofArchiv der Pharmazie
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.relation.tubitakTBAG-107T348
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectBrominationen_US
dc.subjectBromophenolsen_US
dc.subjectCarbonic anhydrase inhibitorsen_US
dc.subjectNatural productsen_US
dc.titleSynthesis and biological evaluation of novel bromophenol derivatives as carbonic anhydrase inhibitorsen_US
dc.typeArticle

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