Synthesis, Molecular Modeling and Biological Assessment of Aryloxymethyl 1,3,4-Thiadiazole and 1,2,4-Triazole-5-Thione Derivatives as Potential Cox Inhibitors

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dc.contributor.authorShirzad, Mohammad Musa
dc.contributor.authorOzadali-Sari, Keriman
dc.contributor.authorUnsal-Tan, Oya
dc.contributor.authorHusseini, Abbas Ali
dc.contributor.authorPalaska, Erhan
dc.date.accessioned2024-09-11T19:50:24Z
dc.date.available2024-09-11T19:50:24Z
dc.date.issued2024
dc.departmentİstanbul Gelişim Üniversitesien_US
dc.description.abstractThiadiazole and triazole-5-thione derivatives are five membered heterocyclic compounds showing cyclooxygenase inhibition activities. Based on this observation a series of novel aryloxymethyl 1,3,4-thiadiazole and 1,2,4-triazole-5-thione derivatives were synthesized and their biological activities evaluated. The suggested chemical structure of synthesized compounds was confirmed using FT-IR, Mass, 1H-NMR, and 13C-NMR spectrometric methods and elemental analysis. The biological activity or potency of synthesized compounds was evaluated using a COX inhibitor screening assay kit (Cayman Chemical Company), and indomethacin and NS398 as standard compounds. Compounds 2b and 3b showed good inhibitory activity against COX-2 and COX-1 enzymes respectively. The obtained data indicate that compound 2b is more selective to COX-2 and compound 3b is more selective to COX-1 compared with other synthesized compounds. These two compounds show promising selectivity and could be a starting point for future research in this area.en_US
dc.description.sponsorshipResearch council of Hacettepe University, Institute Health Scienceen_US
dc.description.sponsorshipThis study was supported by grants from the research council of Hacettepe University, Institute Health Science.en_US
dc.identifier.doi10.1007/s11094-024-03136-8
dc.identifier.endpage215en_US
dc.identifier.issn0091-150X
dc.identifier.issn1573-9031
dc.identifier.issue2en_US
dc.identifier.scopus2-s2.0-85197641439en_US
dc.identifier.startpage209en_US
dc.identifier.urihttps://doi.org/10.1007/s11094-024-03136-8
dc.identifier.urihttps://hdl.handle.net/11363/7624
dc.identifier.volume58en_US
dc.identifier.wosWOS:001252346500009en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.relation.ispartofPharmaceutical Chemistry Journalen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz20240903_Gen_US
dc.subjectthiadiazoleen_US
dc.subjecttriazoleen_US
dc.subjectcyclooxygenaseen_US
dc.subjectinflammationen_US
dc.subjectdockingen_US
dc.titleSynthesis, Molecular Modeling and Biological Assessment of Aryloxymethyl 1,3,4-Thiadiazole and 1,2,4-Triazole-5-Thione Derivatives as Potential Cox Inhibitorsen_US
dc.typeArticleen_US

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