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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. © 2006 American Chemical Society.

Gemma, S., Gabellieri, E., Huleatt, P., Fattorusso, C., Borriello, M., Catalanotti, B., et al. (2006). Discovery of Huperzine A/Tacrine Hybrids as Potent Inhibitors of Human Cholinesterases Targeting Their Mid-gorge Recognition Sites. JOURNAL OF MEDICINAL CHEMISTRY, 49(11), 3421-3425 [10.1021/jm060257t].

Discovery of Huperzine A/Tacrine Hybrids as Potent Inhibitors of Human Cholinesterases Targeting Their Mid-gorge Recognition Sites

Gemma, Sandra;Gabellieri, Emanuele;Butini, Stefania;Nacci, Vito;Campiani, Giuseppe
2006-01-01

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. © 2006 American Chemical Society.
2006
JOURNAL OF MEDICINAL CHEMISTRY
Gemma, S., Gabellieri, E., Huleatt, P., Fattorusso, C., Borriello, M., Catalanotti, B., et al. (2006). Discovery of Huperzine A/Tacrine Hybrids as Potent Inhibitors of Human Cholinesterases Targeting Their Mid-gorge Recognition Sites. JOURNAL OF MEDICINAL CHEMISTRY, 49(11), 3421-3425 [10.1021/jm060257t].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/3542
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