Targeting Alzheimer’s disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238 was written by Rizzo, Stefano;Bartolini, Manuela;Ceccarini, Luisa;Piazzi, Lorna;Gobbi, Silvia;Cavalli, Andrea;Recanatini, Maurizio;Andrisano, Vincenza;Rampa, Angela. And the article was included in Bioorganic & Medicinal Chemistry in 2010.Formula: C6H12BrCl The following contents are mentioned in the article:
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, mols. 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 biol. 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 inhibition of AChE-induced Aβ aggregation with respect to the reference compounds They also showed activity against self-aggregation of Aβ42 peptide, the most amyloidogenic form of amyloid produced in AD brains, while the reference compounds resulted completely ineffective. This study involved multiple reactions and reactants, such as 1-Bromo-6-chlorohexane (cas: 6294-17-3Formula: C6H12BrCl).
1-Bromo-6-chlorohexane (cas: 6294-17-3) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Formula: C6H12BrCl
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics