388072-84-2Relevant academic research and scientific papers
Synthesis and in vivo antimalarial evaluation of novel hydroxyethylamine derivatives
Souza, Mariana Concei??o De,Gon?alves-Silva, Triciana,Moreth, Marcele,Gomes, Claudia R. B.,Kaiser, Carlos Roland,Henriques, Maria Das Gra?as Muller De Oliveira,Souza, Marcus V. N. De
experimental part, p. 266 - 272 (2012/08/08)
A series of hydroxyethylamines has been synthesized from the reaction of (2S,3S )Boc-phenylalanine epoxide with alkyl amines in good yields and evaluated for their in vivo antimalarial activity in mice. Compound 4g presented better activity then the reference artesunate in percentage of inhibition of parasitemia in treated P. berghei-infected mice and compare to the activity of artesunate in the survival of mice 14 days after infection. In addiction, no hemolytic activity was found, which supports that inhibition of parasitemia is due to antimalarial activity. The compound 4g inhibited the differentiation to schizonts suggesting that parasite metabolism is a possible target of 4g. These results indicate that this class of compound possesses promising perspectives for the development of new antimalarial drugs.
BETA-SECRETASE INHIBITING COMPOUNDS HAVING OXO-DIHYDRO-PYRAZOLE MOIETY
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Page/Page column 41, (2009/04/25)
Disclosed are compounds represented by Formula (I) as defined in the specification, or pharmaceutically acceptable salts or isomers thereof, and a pharmaceutical composition for inhibiting beta-secretase activity comprising a therapeutically effective amo
BETA-SECRETASE INHIBITING COMPOUNDS
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Page/Page column 60, (2009/04/25)
Disclosed are compounds represented by Formula (I) as defined in the specification, or pharmaceutically acceptable salts or isomers thereof, and a pharmaceutical composition for inhibiting beta-secretase activity comprising a therapeutically effective amount of the same.
HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page 105, (2010/02/07)
The present invention relates to novel hydroxyethylamine compounds of formula (I): (I) having Asp2 (-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated-amyloid levels or-amyloid deposits, particularly Alzheimer's disease.
TRICYCLIC INDOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF ALZHEIMER’S DISEASE
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Page 36, (2010/02/09)
The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β- amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1)
Stachel, Shawn J.,Coburn, Craig A.,Steele, Thomas G.,Jones, Kristen G.,Loutzenhiser, Elizabeth F.,Gregro, Alison R.,Rajapakse, Hemaka A.,Lai, Ming-Tain,Crouthamel, Ming-Chih,Xu, Min,Tugusheva, Katherine,Lineberger, Janet E.,Pietrak, Beth L.,Espeseth, Amy S.,Shi, Xiao-Ping,Chen-Dodson, Elizabeth,Holloway, M. Katharine,Munshi, Sanjeev,Simon, Adam J.,Kuo, Lawrence,Vacca, Joseph P.
, p. 6447 - 6450 (2007/10/03)
We describe the development of cell-permeable β-secretase inhibitors that demonstratively inhibit the production of the secreted amino terminal fragment of an artificial amyloid precursor protein in cell culture. In addition to potent inhibition in a cell
