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.
Bolognesi ML, Chiriano G, Bartolini M, Mancini F, Bottegoni G, Maestri V, et al. (2011). Synthesis of Monomeric Derivatives To Probe Memoquin's Bivalent Interactions. JOURNAL OF MEDICINAL CHEMISTRY, 54, 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.
