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Synthesis of some 5,6-diaryl-1,2,4-triazine derivatives and investigation of their cyclooxygenase (COX) inhibitory activity

dc.contributor.authorErtaş, Merve
dc.contributor.authorBiltekin, Sevde Nur
dc.contributor.authorBerk, Barkın
dc.contributor.authorYurttaş, Leyla
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned2022-12-06T09:24:45Z
dc.date.available2022-12-06T09:24:45Z
dc.date.issued2022en_US
dc.identifier.citationErtaş, M., Biltekin, S. N., Berk, B., Yurttaş, L. ve Demirayak, Ş. (2022). Synthesis of some 5,6-diaryl-1,2,4-triazine derivatives and investigation of their cyclooxygenase (COX) inhibitory activity. Phosphorus, Sulfur and Silicon and the Related Elements, 197(11), 1123-1135. https://doi.org/10.1080/10426507.2022.2062756en_US
dc.identifier.issn1042-6507
dc.identifier.issn1563-5325
dc.identifier.urihttps://doi.org/10.1080/10426507.2022.2062756
dc.identifier.urihttps://hdl.handle.net/20.500.12511/10080
dc.description.abstractWithin this study, 20 2-[(5,6-diaryl-1,2,4-triazin-3-yl)thio]-N-(benzo/thiazol-2-yl)acetamide derivatives (4a-4t) were synthesized and COX inhibitory activities of the compounds were investigated. Compounds 4k-4o, which have a 4-methoxyphenyl group within their structures, showed strong inhibitory activity on COX-2 enzyme, even compound 4k, namely 2-{[5,6-bis(4-methoxyphenyl)-1,2,4-triazin-3-yl]thio}-N-(thiazol-2-yl)acetamide exhibited higher selectivity on this enzyme (IC50:3.06 mu M). Molecular docking studies were performed for compound 4k on COX-1 and COX-2 enzymes and the results were found to support the molecule's COX-2 selectivity.en_US
dc.description.sponsorshipAnadolu Universityen_US
dc.language.isoengen_US
dc.publisherTaylor & Francis Ltden_US
dc.rightsinfo:eu-repo/semantics/embargoedAccessen_US
dc.subject1,2,4-Triazineen_US
dc.subjectDiarylheterocylicsen_US
dc.subjectThiazoleen_US
dc.subjectCyclooxygenase Inhibitionen_US
dc.subjectCOX-2 Inhibitoren_US
dc.subjectAnti-Inflammatoryen_US
dc.subjectMolecular Dockingen_US
dc.titleSynthesis of some 5,6-diaryl-1,2,4-triazine derivatives and investigation of their cyclooxygenase (COX) inhibitory activityen_US
dc.typereviewen_US
dc.relation.ispartofPhosphorus, Sulfur and Silicon and the Related Elementsen_US
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalıen_US
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalıen_US
dc.authorid0000-0002-2289-7950en_US
dc.authorid0000-0003-1896-2729en_US
dc.authorid0000-0001-6047-2796en_US
dc.identifier.volume197en_US
dc.identifier.issue11en_US
dc.identifier.startpage1123en_US
dc.identifier.endpage1135en_US
dc.relation.publicationcategoryDiğeren_US
dc.identifier.doi10.1080/10426507.2022.2062756en_US
dc.institutionauthorErtaş, Merve
dc.institutionauthorBiltekin, Sevde Nur
dc.institutionauthorBerk, Barkın
dc.institutionauthorDemirayak, Şeref
dc.identifier.wosqualityQ4en_US
dc.identifier.wos000781711400001en_US
dc.identifier.scopus2-s2.0-85129127120en_US
dc.identifier.scopusqualityQ4en_US


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