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Targeting Alzheimer’s disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238 by Stefano Rizzo; Manuela Bartolini; Luisa Ceccarini; Lorna Piazzi; Silvia Gobbi; Andrea Cavalli; Maurizio Recanatini; Vincenza Andrisano; Angela Rampa is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Targeting Alzheimer’s disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238 about?
We report on a series of hybrid compounds structurally derived from donepezil and AP2238. This study was aimed at improving the activities of the reference compounds, donepezil and AP2238, and at broadening the range of activities of new derivatives as, due to the multifactorial nature of AD, molecules that modulate the activity of a single protein target are unable to significantly modify the progression of the disease. In particular, the indanone core from donepezil was linked to the phenyl-N-methylbenzylamino moiety from AP2238, through a double bond that was kept to evaluate the role of a lower flexibility in the biological activities. Moreover, SAR studies were performed to evaluate the role of different substituents in position 5 or 6 of the indanone ring in the interaction with the PAS, introducing also alkyl chains of different lengths carrying different amines at one end. Derivatives 21 and 22 proved to be the most active within the series and their potencies against AChE were in the same order of magnitude of the reference compounds. Compounds 15, 21-22, with a 5-carbon alkyl chain bearing an amino moiety at one end, better contacting the PAS, remarkably improved the inhi
Who reads Targeting Alzheimer’s disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Stefano Rizzo; Manuela Bartolini; Luisa Ceccarini; Lorna Piazzi; Silvia Gobbi; Andrea Cavalli; Maurizio Recanatini; Vincenza Andrisano; Angela Rampa
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2010
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)