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  • Title: Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.
    Author: Belluti F, Piazzi L, Bisi A, Gobbi S, Bartolini M, Cavalli A, Valenti P, Rampa A.
    Journal: Eur J Med Chem; 2009 Mar; 44(3):1341-8. PubMed ID: 18396354.
    Abstract:
    Starting from a structure-based drug design, new acetylcholinesterase inhibitors were designed and synthesized as analogues of donepezil. The compounds were composed by an aromatic function and a tertiary amino moiety connected by a suitable spacer. In particular, the benzophenone nucleus and the N,N-benzylmethylamine function were selected. The easily accessible three-step synthesis of these compounds resulted to be significantly less difficult and expensive than that of donepezil. Several compounds possess anti-cholinesterase activity in the order of micro and sub-micromolar. Particularly, compounds 1 and 10 were the most potent inhibitors of the series.
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