Synthesis of some novel norbornene-fused pyridazines as potent inhibitors of carbonic anhydrase and acetylcholinesterase

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dc.authorid0000-0003-2209-5402en_US
dc.contributor.authorKoçak, Ramazan
dc.contributor.authorAkın, Esra Turan
dc.contributor.authorKalın, Pinar
dc.contributor.authorTalaz, Oktay
dc.contributor.authorSaraçoğlu, Nurullah
dc.contributor.authorDaştan, Arif
dc.contributor.authorGülçin, İlhami
dc.date.accessioned2019-12-06T21:16:15Z
dc.date.available2019-12-06T21:16:15Z
dc.date.issued2016
dc.departmentKMÜ, Kamil Özdağ Fen Fakültesi, Kimya Bölümüen_US
dc.descriptionWOS:000388438000049en_US
dc.description.abstractThe reaction of benzocyclic norbornene derivatives with tetrazines provided the 1,3-dihydropyridazine derivatives as a single product. The dihydropyridazine derivatives have been dehydrogenated with phenyliodine bis(trifluoroacetate) to yield the corresponding pyridazines in a high yield. Two stable diazines, primary product of corresponding 1,4-dihydropyridazine, were also isolated. Structures were then determined by H-1-NMR, and C-13-NMR beside to elemental analyses. The novel pyridazine derivatives (8-9) efficiently inhibited the cytosolic human carbonic anhydrase isoenzymes I and II (hCA I and II). In addition, these novel pyridazine derivatives (8-9) were evaluated for their in vitro acetylcholinesterase inhibitory activity. Ligand-receptor interactions are tested using molecular docking simulations. Obtained docking scores are in good agreement with in vitro results.en_US
dc.description.sponsorshipScientific and Technical Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [112T341]; Ataturk UniversityAtaturk University; Turkish Academy of Science, Turkey, under the BAGEP programen_US
dc.description.sponsorshipAuthors are indebted to The Scientific and Technical Research Council of Turkey (TUBITAK, grant no. 112T341) and Ataturk University for financial supports. Thanks also to Prof. Dr Cavit Kazaz, Res. Assistant Baris Anil, Dr Murat Acar, and Res. Assistant Ufuk Atmaca for NMR experiments and elemental analyses. Additionally, S.D. acknowledges support from Turkish Academy of Science, Turkey, under the BAGEP program.en_US
dc.identifier.citationKoçak, R., Akın, E. T., Kalın, P., Talaz, O., Saraçoğlu, N., Dastan, A., Gülçin, I., ... Durdağı, S. (2016). Synthesis of some novel norbornene-fused pyridazines as potent inhibitors of carbonic anhydrase and acetylcholinesterase. Journal of Heterocyclic Chemistry, 53, 6, 2049-2056.
dc.identifier.doi10.1002/jhet.2558
dc.identifier.endpage2056en_US
dc.identifier.issn0022-152X
dc.identifier.issn1943-5193
dc.identifier.issue6en_US
dc.identifier.scopus2-s2.0-84995629550
dc.identifier.scopusqualityQ2
dc.identifier.startpage2049en_US
dc.identifier.urihttps://dx.doi.org/10.1002/jhet.2558
dc.identifier.urihttps://hdl.handle.net/11492/2854
dc.identifier.volume53en_US
dc.identifier.wosWOS:000388438000049
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Sceince
dc.indekslendigikaynakScopus
dc.institutionauthorTalaz, Oktay
dc.language.isoen
dc.publisherWileyen_US
dc.relation.journalJournal Of Heterocyclic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.titleSynthesis of some novel norbornene-fused pyridazines as potent inhibitors of carbonic anhydrase and acetylcholinesteraseen_US
dc.typeArticle

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