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.
Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors / F. Belluti; L. Piazzi; A. Bisi; S. Gobbi; M. Bartolini; A. Cavalli; P. Valenti; A. Rampa. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 44:(2009), pp. 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.