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EnglishStarting 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.
| Titolo: | Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors |
| Autore/i: | BELLUTI, FEDERICA; PIAZZI, LORNA; BISI, ALESSANDRA; GOBBI, SILVIA; BARTOLINI, MANUELA; CAVALLI, ANDREA; P. Valenti; RAMPA, ANGELA |
| Autore/i Unibo: | |
| Anno: | 2009 |
| Rivista: | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/j.ejmech.2008.02.035 |
| 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. |
| Data prodotto definitivo in UGOV: | 2009-03-30 18:50:59 |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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