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.
F. Belluti, L. Piazzi, A. Bisi, S. Gobbi, M. Bartolini, A. Cavalli, et al. (2009). Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 44, 1341-1348 [10.1016/j.ejmech.2008.02.035].
Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors
BELLUTI, FEDERICA;PIAZZI, LORNA;BISI, ALESSANDRA;GOBBI, SILVIA;BARTOLINI, MANUELA;CAVALLI, ANDREA;RAMPA, ANGELA
2009
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
