Synthesis of Some Novel Norbornene‐Fused Pyridazines as Potent Inhibitors of Carbonic Anhydrase and Acetylcholinesterase |
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| Authors: | Ramazan Kocak Esra Turan Akın Pınar Kalın Oktay Talaz Nurullah Saracoglu Arif Dastan Ilhami Gülcin Serdar Durdagi |
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| Affiliation: | 1. Department of Chemistry, Faculty of Sciences, Atatürk University, Erzurum, Turkey;2. Department of Chemistry, Faculty of Kamil Ozdag Sciences, Karamanoglu Mehmetbey University, Karaman, Turkey;3. Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia;4. Department of Biophysics, School of Medicine, Bahcesehir University, Istanbul, Turkey |
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| Abstract: | The 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 1H‐NMR, and 13C‐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. |
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