104450-85-3Relevant academic research and scientific papers
Design and synthesis of 5,5′-disubstituted aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors
Malamas, Michael S.,Erdei, Jim,Gunawan, Iwan,Turner, Jim,Hu, Yun,Wagner, Erik,Fan, Kristi,Chopra, Rajiv,Olland, Andrea,Bard, Jonathan,Jacobsen, Steve,Magolda, Ronald L.,Pangalos, Menelas,Robichaud, Albert J.
experimental part, p. 1146 - 1158 (2010/07/02)
The identification of small molecule aminohydantoins as potent and selective human β-secretase inhibitors is reported. These analogues exhibit low nannomolar potency for BACE1, show comparable activity in a cell-based (ELISA) assay, and demonstrate 50 value for BACE1 of 10 nM and exhibited comparable cellular activity (EC 50 = 20 nM) in the ELISA assay. Acute oral administration of (S)-55 at 100 mg/kg resulted in a 69% reduction of plasma Aβ40 at 8 h in a Tg2576 mouse (p 0.001).
Synthesis of Some New Polynuclear Compounds by Cycloaddition Reaction
Samanta, S. R.,Mukherjee, A. K.
, p. 26 - 29 (2007/10/02)
A large number of 7,9-disubstituted derivatives (I) of cyclopentacenaphthylene-8(H)-one and 2,5-disubstituted derivatives (II) of 3,4-diphenylcyclopentadienone have been synthesized by condensing acenaphthaquinone and benzil separately with suitable 1,3-disubstituted propan-2-ones.The 3-(o- and p-methoxytolyl)cyclopentadienones (IX) have been synthesized by Friedel-Crafts reaction of appropriate methyl cresyl ethers and phenacyl chloride.These dienones have been subjected to Diels-Alder reaction with acenaphthylene and a new acetylenic dienophile (V) (whose synthesis is also described in this paper) to yield a large number of polynuclear aromatic compounds having fluoranthene and p-quaterphenyl nuclei, which have been finally characterised by elemental analyses, IR and PMR spectral data.
Synthesis of Some Polyphenylated Aromatic Compounds Using Tetracyclone Derivatives
Samanta, S. R.,Mukherjee, A. K.,Bhattacharya, A. J.
, p. 960 - 961 (2007/10/02)
The 3-(o- and p-methoxytolyl)-2,4,5-triphenylcyclopentadienones (I) have been synthesised and subjected to Diels-Alder reaction with diphenylacetylene and bicyclo-hepta-2,5-diene to give the polyphenylated aromatic hydrocarbons.The products have been characterised by elemental analyses, IR, PMR and UV spectra.
