Eight monomeric congeners, related to the multitarget lead candidate memoquin, were prepared and evaluated at multiple targets to determine their profile against Alzheimer's disease. 2-4 bind to AChE with similar low nanomolar affinities and function as effective inhibitors of amyloid aggregation. The most potent monovalent ligand 2 also inhibits BACE-1 in vitro and APP metabolism in primary chicken telencephalic neurons.
Synthesis of Monomeric Derivatives To Probe Memoquin's Bivalent Interactions / Bolognesi ML; Chiriano G; Bartolini M; Mancini F; Bottegoni G; Maestri V; Czvitkovich S; Windisch M; Cavalli A; Minarini A; Rosini M; Tumiatti V; Andrisano V; Melchiorre C.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 54:(2011), pp. 8299-82304. [10.1021/jm200691d]
Synthesis of Monomeric Derivatives To Probe Memoquin's Bivalent Interactions
BOLOGNESI, MARIA LAURA;BARTOLINI, MANUELA;MANCINI, FRANCESCA;MAESTRI, VALENTINA;CAVALLI, ANDREA;MINARINI, ANNA;ROSINI, MICHELA;TUMIATTI, VINCENZO;ANDRISANO, VINCENZA;MELCHIORRE, CARLO
2011
Abstract
Eight monomeric congeners, related to the multitarget lead candidate memoquin, were prepared and evaluated at multiple targets to determine their profile against Alzheimer's disease. 2-4 bind to AChE with similar low nanomolar affinities and function as effective inhibitors of amyloid aggregation. The most potent monovalent ligand 2 also inhibits BACE-1 in vitro and APP metabolism in primary chicken telencephalic neurons.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
