Alzheimer’s disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiology. To confront AD, an innovative strategy is to design single chemical entities able to simultaneously modulate more than one target. Here, we present compounds that inhibit acetylcholinesterase and NMDA receptor activity. Furthermore, these compounds inhibit AChE-induced beta-aggregation and display antioxidant properties, emerging as lead candidates for treating AD.
Inhibition of Acetylcholinesterase, Beta-Amyloid Aggregation, and NMDA Receptors in Alzheimer's Disease: A Promising Direction for the Multi-target-Directed Ligands Gold Rush / M. Rosini; E. Simoni; M. Bartolini; A. Cavalli; L. Ceccarini; N. Pascu; D. W. McClymont; A. Tarozzi; M. L. Bolognesi; A. Minarini; V. Tumiatti; V. Andrisano; I. R. Mellor; C. Melchiorre. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 51:(2008), pp. 4381-4384. [10.1021/jm800577j]
Inhibition of Acetylcholinesterase, Beta-Amyloid Aggregation, and NMDA Receptors in Alzheimer's Disease: A Promising Direction for the Multi-target-Directed Ligands Gold Rush
ROSINI, MICHELA;SIMONI, ELENA;BARTOLINI, MANUELA;CAVALLI, ANDREA;CECCARINI, LUISA;TAROZZI, ANDREA;BOLOGNESI, MARIA LAURA;MINARINI, ANNA;TUMIATTI, VINCENZO;ANDRISANO, VINCENZA;MELCHIORRE, CARLO
2008
Abstract
Alzheimer’s disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiology. To confront AD, an innovative strategy is to design single chemical entities able to simultaneously modulate more than one target. Here, we present compounds that inhibit acetylcholinesterase and NMDA receptor activity. Furthermore, these compounds inhibit AChE-induced beta-aggregation and display antioxidant properties, emerging as lead candidates for treating AD.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
