Synthesis of monomeric derivatives to probe memoquin's bivalent interactions

Maria Laura Bolognesi; Gian Paolo Chiriano; Manuela Bartolini; Francesca Mancini; Giovanni Bottegoni; Valentina Maestri; Stefan Czvitkovich; Manfred Windisch; Andrea Cavalli; Anna Minarini; Michela Rosini; Vincenzo Tumiatti; Vincenza Andrisano; Carlo Melchiorre

doi:10.1021/jm200691d

Synthesis of monomeric derivatives to probe memoquin's bivalent interactions

Maria Laura Bolognesi^*, Gian Paolo Chiriano, Manuela Bartolini, Francesca Mancini, Giovanni Bottegoni, Valentina Maestri, Stefan Czvitkovich, Manfred Windisch, Andrea Cavalli, Anna Minarini, Michela Rosini, Vincenzo Tumiatti, Vincenza Andrisano, Carlo Melchiorre

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

27 Citations (Scopus)

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. (Figure presented)

Original language	English
Pages (from-to)	8299-8304
Number of pages	6
Journal	Journal of Medicinal Chemistry
Volume	54
Issue number	24
DOIs	https://doi.org/10.1021/jm200691d
Publication status	Published - 22 Dec 2011
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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Bolognesi, M. L., Chiriano, G. P., Bartolini, M., Mancini, F., Bottegoni, G., Maestri, V., Czvitkovich, S., Windisch, M., Cavalli, A., Minarini, A., Rosini, M., Tumiatti, V., Andrisano, V., & Melchiorre, C. (2011). Synthesis of monomeric derivatives to probe memoquin's bivalent interactions. Journal of Medicinal Chemistry, 54(24), 8299-8304. https://doi.org/10.1021/jm200691d

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Bolognesi, ML, Chiriano, GP, Bartolini, M, Mancini, F, Bottegoni, G, Maestri, V, Czvitkovich, S, Windisch, M, Cavalli, A, Minarini, A, Rosini, M, Tumiatti, V, Andrisano, V & Melchiorre, C 2011, 'Synthesis of monomeric derivatives to probe memoquin's bivalent interactions', Journal of Medicinal Chemistry, vol. 54, no. 24, pp. 8299-8304. https://doi.org/10.1021/jm200691d

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T1 - Synthesis of monomeric derivatives to probe memoquin's bivalent interactions

AU - Bolognesi, Maria Laura

AU - Chiriano, Gian Paolo

AU - Bartolini, Manuela

AU - Mancini, Francesca

AU - Bottegoni, Giovanni

AU - Maestri, Valentina

AU - Czvitkovich, Stefan

AU - Windisch, Manfred

AU - Cavalli, Andrea

AU - Minarini, Anna

AU - Rosini, Michela

AU - Tumiatti, Vincenzo

AU - Andrisano, Vincenza

AU - Melchiorre, Carlo

PY - 2011/12/22

Y1 - 2011/12/22

N2 - 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. (Figure presented)

AB - 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. (Figure presented)

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JO - Journal of Medicinal Chemistry

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ER -

Synthesis of monomeric derivatives to probe memoquin's bivalent interactions

Abstract

ASJC Scopus subject areas

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