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American Chemical Society, Journal of Medicinal Chemistry, 11(49), p. 3421-3425, 2006

DOI: 10.1021/jm060257t

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Discovery of Huperzine A−Tacrine Hybrids as Potent Inhibitors of Human Cholinesterases Targeting Their Midgorge Recognition Sites

Journal article published in 2006 by Sandra Gemma ORCID, Emanuele Gabellieri, Paul Huleatt, Caterina Fattorusso ORCID, Marianna Borriello, Bruno Catalanotti, Stefania Butini ORCID, Meri De Angelis, Ettore Novellino, Vito Nacci, Tatyana Belinskaya, ‖ and Ashima Saxena, Giuseppe Campiani
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This paper is available in a repository.

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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.