In Vitro Cytotoxicity of Methano[1,2,4]Triazolo-[1,5-C][1,3,5]Benzoxadiazocine Derivatives and Their Effects on Nitrite and Prostaglandin E2 (PGE2) Levels

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dc.authorid0000-0001-6373-5221en_US
dc.contributor.authorDoğan, İnci Selin
dc.contributor.authorGümüş, Mustafa Kemal
dc.contributor.authorGorobets, Nikolay Yu
dc.contributor.authorReis, Rengin
dc.contributor.authorOrak, Duygu
dc.contributor.authorSipahi, Hande
dc.contributor.authorSarı, Suat
dc.contributor.authorChebanov, Valentyn A.
dc.date.accessioned2022-09-30T08:04:02Z
dc.date.available2022-09-30T08:04:02Z
dc.date.issued2022
dc.departmentAÇÜ, Artvin Meslek Yüksekokulu, Laboratuvar Teknolojisi Bölümüen_US
dc.description.abstractBiological activity of the Biginelli type heterocycles is extremely broad and provides a suitable platform for the discovery of potent small drug-like molecules. Such activity of 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives is widely known, whereas their oxygen-bridged analogs, benzoxadiazocines, are presented quite rarely in the literature. In this study, a series of new methano[1,2,4]triazolo[1,5-c][1,3,5]benzoxadiazocine derivatives (3a-3j) were evaluated in vitro for their activities and molecular docking features. According to the molecular docking study, COX-2 and PGE(2)S appeared as likely targets responsible for the reduced PGE(2) levels caused by the title compounds. The cytotoxicity of compounds 3a-3g, 3j was evaluated on RAW 264.7 murine macrophage cell line by MTT assay after treatment for 24 h with various doses (25, 50, 100 mu M) of these compounds. Then, compounds admitting cell viability higher than 70% were tested for their anti-inflammatory activity at non-toxic doses by evaluating the nitrite level of cell supernatants with the Griess reagent. Compounds 3c and 3f demonstrated significant inhibition of nitrite production (by 29 and 25%, respectively) at 100 mu M (p < 0.05). These compounds significantly inhibited PGE(2) production, thus suggesting analgesic activity.
dc.identifier.citationDoğan, İ. S., Gümüş, M. K., Gorobets, N. Y., Reis, R., Orak, D., Sipahi, H., ... & Chebanov, V. A. (2022). In Vitro Cytotoxicity of Methano [1, 2, 4] Triazolo-[1, 5-C][1, 3, 5] Benzoxadiazocine Derivatives and Their Effects on Nitrite and Prostaglandin E2 (PGE2) Levels. Pharmaceutical Chemistry Journal.en_US
dc.identifier.doi10.1007/s11094-022-02708-w
dc.identifier.scopusqualityQ4
dc.identifier.urihttps://hdl.handle.net/11494/4255
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorGümüş, Mustafa Kemal
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.relation.ispartofPharmaceutical Chemistry Journal
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectanti-inflammatory activityen_US
dc.subjectanalgesicen_US
dc.subjectBiginelli reactionen_US
dc.subjectin vitro cytotoxicityen_US
dc.subjectmolecular dockingen_US
dc.subjectnitrite levelen_US
dc.subjectPGE(2)en_US
dc.titleIn Vitro Cytotoxicity of Methano[1,2,4]Triazolo-[1,5-C][1,3,5]Benzoxadiazocine Derivatives and Their Effects on Nitrite and Prostaglandin E2 (PGE2) Levelsen_US
dc.typeArticle

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