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dc.contributor.authorNural, Yahya
dc.contributor.authorÖzdemir, Sadin
dc.contributor.authorYalçın, Mustafa Serkan
dc.contributor.authorDemir, Bünyamin
dc.contributor.authorAtabey, Hasan
dc.contributor.authorSeferoğlu, Zeynel
dc.contributor.authorEce, Abdulilah
dc.date.accessioned2021-12-06T09:11:10Z
dc.date.available2021-12-06T09:11:10Z
dc.date.issued2022en_US
dc.identifier.issn0960-894X
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2021.128453
dc.identifier.urihttps://hdl.handle.net/20.500.12445/1616
dc.description.abstractIn this study, a series of bis– and tetrakis–1,2,3–triazole derivatives were synthesized using copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry in 73–95% yield. The bis– and tetrakis–1,2,3–triazoles exhibited significant DNA cleavage activity while the tetrakis–1,2,3–triazole analog 6g completely degraded the plasmid DNA. Molecular docking simulations suggest that compound 6g acts as minor groove binder of DNA by binding through several noncovalent interactions with base pairs. All bis- and tetrakis–1,2,3-triazole derivatives were screened for antibacterial activity against E. coli, B. cereus, S. aureus, P. aeruginosa, E. hirae, L. pneumophila subsp. pneumophila strains and antifungal activity against microfungus C. albicans and C. tropicalis strains. Compound 4d exhibited the best antibacterial activity among bis–1,2,3–triazoles against E. coli and E. hirae, while 6c exhibited the best antibacterial activity among tetrakis–1,2,3–triazoles against E. hirae. Furthermore, the best antifungal activity against C. albicans and C. tropicalis was reported for the compound 5, while 6d displayed the best antifungal activity against C. tropicalis and C. albicans. Reasonable iron chelating activities and DPPH radical scavenging abilities were found for some of the compounds. Finally, the acid dissociation constants (pKa) of the bis–1,2,3–triazoles were also determined with the help of HYPERQUAD program using the data obtained from potentiometric titrations. The reported data here concludes that the bis- and tetrakis-1,2,3- triazoles are important cores that should be considered for further development of especially new anticancer agents acting through the DNA cleavage activity.en_US
dc.language.isoengen_US
dc.publisherElsevieren_US
dc.relation.isversionofhttps://doi.org/10.1016/j.bmcl.2021.128453en_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.rightsAttribution-NonCommercial-NoDerivs 3.0 United States*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/3.0/us/*
dc.subjectBisen_US
dc.subjectTriazole/Tetrakisen_US
dc.subjectDNA-Cleavage/Molecular Dockingen_US
dc.subjectAntioxidanten_US
dc.subjectAntimicrobialen_US
dc.subjectAcid Dissociation Constanten_US
dc.titleNew bis and tetrakis 1,2,3 triazole derivatives synthesis, DNA cleavage, molecular docking, antimicrobial, antioxidant activity and acid dissociation constantsen_US
dc.typearticleen_US
dc.relation.journalBioorganic and Medicinal Chemistry Lettersen_US
dc.contributor.departmentEczacılık Fakültesien_US
dc.identifier.volume55en_US
dc.identifier.startpage1en_US
dc.identifier.endpage7en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US


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