Design, synthesis and evaluation of diaryl γ-dihydropyrone derivatives as cyclocurcumin mimetics and inhibitors of the aggregation of amyloid β
A structure activity relationship study of cyclocurcumin-derived, diaryl γ-dihydropyrone-based inhibitors of amyloid β aggregation is described. Optimization of the diaryl γ-dihydropyrone framework and two phenolic rings resulted in the identification of diaryl γ-dihydropyrone type cyclocurcumin analogue AY1511, which exhibited potent anti-amyloid β aggregation activity (leading to nanorod-like fragments), sufficient water solubility, and low cytotoxicity.
Cyclization vs. elimination reactions of 5-Aryl-5-hydroxy 1,3-diones: One-pot synthesis of 2-Aryl-2,3-dihydro-4H-pyran-4-ones
2-Aryl-2,3-dihydro-4H-pyran-4-ones were prepared in one step by cyclocondensation of 1,3-diketone dianions with aldehydes. The use of HCl (10%) for the aqueous workup proved to be very important to avoid elimination reactions of the 5-aryl-5-hydroxy 1,3-d
Khera, Rasheed Ahmad,Ahmad, Rasheed,Ullah, Ihsan,Abid, Obaid-Ur-Rahman,Fatunsin, Olumide,Sher, Muhammad,Villinger, Alexander,Langer, Peter
experimental part
p. 1705 - 1715
(2010/12/20)
One-pot synthesis of 6-aryl-2,3-dihydro-4H-pyran-4-ones by cyclocondensation of 1,3-diketone dianions with aldehydes
6-Aryl-2,3-dihydro-4H-pyran-4-ones were prepared in one step by cyclocondensation of 1,3-diketone dianions with aldehydes. The use of hydrochloric acid (10%) for the aqueous work-up proved to be very important.
Ahmad, Rasheed,Khera, Rasheed Ahmad,Villinger, Alexander,Langer, Peter
experimental part
p. 3020 - 3022
(2009/09/28)
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