Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites

…, C Fattorusso, M Borriello, B Catalanotti…

文献索引：Gemma, Sandra; Gabellieri, Emanuele; Huleatt, Paul; Fattorusso, Caterina; Borriello, Marianna; Catalanotti, Bruno; Butini, Stefania; De Angelis, Meri; Novellino, Ettore; Nacci, Vito; Belinskaya, Tatyana; Saxena, Ashima; Campiani, Giuseppe Journal of Medicinal Chemistry, 2006 , vol. 49, # 11 p. 3421 - 3425

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被引用次数: 45

摘要

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 ...