Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.

Article Details

Citation

Copy to clipboard

Belluti F, Piazzi L, Bisi A, Gobbi S, Bartolini M, Cavalli A, Valenti P, Rampa A

Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.

Eur J Med Chem. 2009 Mar;44(3):1341-8. doi: 10.1016/j.ejmech.2008.02.035. Epub 2008 Mar 8.

PubMed ID

18396354 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Donepezil	Acetylcholinesterase	IC 50 (nM)	20	N/A	N/A	Details