The complex etiology of Alzheimer’s disease (AD) prompts scientists to develop multitarget strategies to combat causes and symptoms. We therefore designed, synthesized, and tested new hybrid molecules linking a benzofuran ring to a N-methyl-N-benzylamine through a heptyloxy chain, affording a series of potential multifunctional drugs for AD. The cholinesterase inhibitory activity was extended to the inhibition of Abeta fibril formation for 1, 3, and 5. Compound 3 showed an additional neuroprotective effect.
S. Rizzo, C. Riviere, L. Piazzi, A. Bisi, S. Gobbi, M. Bartolini, et al. (2008). Benzofuran-Based Hybrid Compounds for the Inhibition of Cholinesterase Activity, Abeta Amyloid Aggregation, and Abeta Neurotoxicity. JOURNAL OF MEDICINAL CHEMISTRY, 51, 2883-2886 [10.1021/jm8002747].
Benzofuran-Based Hybrid Compounds for the Inhibition of Cholinesterase Activity, Abeta Amyloid Aggregation, and Abeta Neurotoxicity
RIZZO, STEFANO;PIAZZI, LORNA;BISI, ALESSANDRA;GOBBI, SILVIA;BARTOLINI, MANUELA;ANDRISANO, VINCENZA;MORRONI, FABIANA;TAROZZI, ANDREA;RAMPA, ANGELA
2008
Abstract
The complex etiology of Alzheimer’s disease (AD) prompts scientists to develop multitarget strategies to combat causes and symptoms. We therefore designed, synthesized, and tested new hybrid molecules linking a benzofuran ring to a N-methyl-N-benzylamine through a heptyloxy chain, affording a series of potential multifunctional drugs for AD. The cholinesterase inhibitory activity was extended to the inhibition of Abeta fibril formation for 1, 3, and 5. Compound 3 showed an additional neuroprotective effect.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
