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

Koçak, RamazanAkın, Esra TuranKalın, PinarTalaz, OktaySaraçoğlu, NurullahDaştan, ArifGülçin, İlhami2019-12-062019-12-062016Koçak, 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, 2049-2056.0022-152X1943-5193https://dx.doi.org/10.1002/jhet.2558https://hdl.handle.net/11492/2854WOS:000388438000049The 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.enSynthesis of some novel norbornene-fused pyridazines as potent inhibitors of carbonic anhydrase and acetylcholinesteraseArticle53620492056info:eu-repo/semantics/closedAccess2-s2.0-84995629550WOS:00038843800004910.1002/jhet.2558Q2Q3