- Molecular modelling, synthesis and acetylcholinesterase inhibition of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate
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In silico analysis of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate (2) predicts that this molecule should be successfully docked in the PAS, and easily accommodated in the CAS of AChE. The synthesis and the AChE/BuChE inhibition studies are reported, confirming that compound 2 is a potent and selective AChE inhibitor, and consequently, a new lead compound for further development into new dual CAS/PAS cholinergic agents for the treatment of Alzheimer's disease.
- Soriano, Elena,Samadi, Abdelouahid,Chioua, Mourad,Ríos, Cristóbal de los,Marco-Contelles, José
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- Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives
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1,8-Naphthyridine derivatives related to 17 (ITH4012), a neuroprotective compound reported by our research group, have been synthesized. In general, they have shown better inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) than mo
- De Los Ríos, Cristóbal,Egea, Javier,Marco-Contelles, José,León, Rafael,Samadi, Abdelouahid,Iriepa, Isabel,Moraleda, Ignacio,Gálvez, Enrique,García, Antonio G.,López, Manuela G.,Villarroya, Mercedes,Romero, Alejandro
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