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

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dc.authorid0000-0002-2289-7950
dc.authorid0000-0003-1896-2729
dc.authorid0000-0001-6047-2796
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.issued2022
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalı
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.
dc.description.sponsorshipAnadolu Universityen_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/10.1080/10426507.2022.2062756
dc.identifier.doi10.1080/10426507.2022.2062756
dc.identifier.endpage1135
dc.identifier.issn1042-6507
dc.identifier.issn1563-5325
dc.identifier.issue11
dc.identifier.scopus2-s2.0-85129127120
dc.identifier.scopusqualityQ4
dc.identifier.startpage1123
dc.identifier.urihttps://doi.org/10.1080/10426507.2022.2062756
dc.identifier.urihttps://hdl.handle.net/20.500.12511/10080
dc.identifier.volume197
dc.identifier.wos000781711400001en_US
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorErtaş, Merve
dc.institutionauthorBiltekin, Sevde Nur
dc.institutionauthorBerk, Barkın
dc.institutionauthorDemirayak, Şeref
dc.language.isoen
dc.publisherTaylor & Francis Ltd
dc.relation.ispartofPhosphorus, Sulfur and Silicon and the Related Elementsen_US
dc.relation.publicationcategoryDiğer
dc.rightsinfo:eu-repo/semantics/embargoedAccess
dc.subject1,2,4-Triazine
dc.subjectDiarylheterocylics
dc.subjectThiazole
dc.subjectCyclooxygenase Inhibition
dc.subjectCOX-2 Inhibitor
dc.subjectAnti-Inflammatory
dc.subjectMolecular Docking
dc.titleSynthesis of some 5,6-diaryl-1,2,4-triazine derivatives and investigation of their cyclooxygenase (COX) inhibitory activity
dc.typeReview Article

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