Title : Molecular modelling, synthesis and acetylcholinesterase inhibition of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate - Soriano_2010_Bioorg.Med.Chem.Lett_20_2950 |
Author(s) : Soriano E , Samadi A , Chioua M , de los Rios C , Marco-Contelles J |
Ref : Bioorganic & Medicinal Chemistry Lett , 20 :2950 , 2010 |
Abstract :
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. |
PubMedSearch : Soriano_2010_Bioorg.Med.Chem.Lett_20_2950 |
PubMedID: 20350807 |
Inhibitor | PyrTac-5f |
Soriano E, Samadi A, Chioua M, de los Rios C, Marco-Contelles J (2010)
Molecular modelling, synthesis and acetylcholinesterase inhibition of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate
Bioorganic & Medicinal Chemistry Lett
20 :2950
Soriano E, Samadi A, Chioua M, de los Rios C, Marco-Contelles J (2010)
Bioorganic & Medicinal Chemistry Lett
20 :2950