| Title : Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites - Gemma_2006_J.Med.Chem_49_3421 |
| Author(s) : Gemma S , Gabellieri E , Huleatt P , Fattorusso C , Borriello M , Catalanotti B , Butini S , De Angelis M , Novellino E , Nacci V , Belinskaya T , Saxena A , Campiani G |
| Ref : Journal of Medicinal Chemistry , 49 :3421 , 2006 |
|
Abstract :
We describe herein the development of novel huperzine A-tacrine hybrids characterized by 3-methylbicyclo[3.3.1]non-3-ene scaffolds. These compounds were specifically designed to establish tight interactions, through different binding modes, with the midgorge recognition sites of human acetylcholinesterase (hAChE: Y72, D74) and human butyrylcholinesterase (hBuChE: N68, D70) and their catalytic or peripheral sites. Compounds 5a-c show a markedly improved biological profile relative to tacrine and huperzine A. |
| PubMedSearch : Gemma_2006_J.Med.Chem_49_3421 |
| PubMedID: 16722663 |
Gemma S, Gabellieri E, Huleatt P, Fattorusso C, Borriello M, Catalanotti B, Butini S, De Angelis M, Novellino E, Nacci V, Belinskaya T, Saxena A, Campiani G (2006)
Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites
Journal of Medicinal Chemistry
49 :3421
Gemma S, Gabellieri E, Huleatt P, Fattorusso C, Borriello M, Catalanotti B, Butini S, De Angelis M, Novellino E, Nacci V, Belinskaya T, Saxena A, Campiani G (2006)
Journal of Medicinal Chemistry
49 :3421