1. Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.
- Author
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Belluti F, Piazzi L, Bisi A, Gobbi S, Bartolini M, Cavalli A, Valenti P, and Rampa A
- Subjects
- Benzophenones chemical synthesis, Cholinesterase Inhibitors chemical synthesis, Drug Evaluation, Preclinical, Humans, Magnetic Resonance Spectroscopy, Models, Molecular, Spectrometry, Mass, Electrospray Ionization, Acetylcholinesterase drug effects, Benzophenones chemistry, Benzophenones pharmacology, Cholinesterase Inhibitors chemistry, Cholinesterase Inhibitors pharmacology
- 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.
- Published
- 2009
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