119111-63-6Relevant articles and documents
Sphingosine Analogs, Compositions, and Methods Related Thereto
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Paragraph 0205, (2014/10/29)
The disclosure relates to compounds, pharmaceutical compositions, and methods of treating or preventing disease. In certain embodiments, the disclosure relates to methods of treating an infection or cancer comprising administering a pharmaceutical composition disclosed herein to a subject in need thereof. In a typical embodiment, one administers a pharmaceutical composition comprising sphingosine or a sphingosine analog to a subject at risk for, exhibiting symptoms of or diagnosed with a malaria infection.
MK2 INHIBITORS AND USES THEREOF
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Paragraph 00646, (2014/10/03)
The present invention provides compounds, compositions thereof, and methods of using the same.
Sphingolipid analogues inhibit development of malaria parasites
Meyer, Esmeralda V. S.,Holt, Jason J.,Girard, Kathryn R.,Ballie, Mark T.,Bushnev, Anatoliy S.,Lapp, Stacey,Menaldino, David S.,Arrendale, Richard F.,Reddy, G. Prabhakar,Evers, Taylor J.,Howard, Randy B.,Culver, Deborah G.,Liotta, Dennis C.,Galinski, Mary R.,Natchus, Michael G.
supporting information; scheme or table, p. 43 - 47 (2012/04/04)
Plasmodium-infected erythrocytes have been shown to employ sphingolipids from both endogenous metabolism as well as existing host pools. Therapeutic agents that limit these supplies have thus emerged as intriguing, mechanistically distinct putative targets for the treatment of malaria infections. In an initial screen of our library of sphingolipid pathway modulators for efficacy against two strains of the predominant human malaria species Plasmodium falciparum and Plasmodium knowlesi, a series of orally available, 1-deoxysphingoid bases were found to possess promising in vitro antimalarial activity. To better understand the structural requirements that are necessary for this observed activity, a second series of modified analogues were prepared and evaluated. Initial pharmacokinetic assessments of key analogues were investigated to evaluate plasma and red blood cell concentrations in vivo.
Decarboxylation of 1-Aminocyclopropanecarboxylic Acid and Its Derivatives
Vaidyanathan, Ganesan,Wilson, Joseph W.
, p. 1810 - 1815 (2007/10/02)
The question of whether the title compounds could be decarboxylated to cyclopropanone derivatives was answered in the affirmative by the following observations. (1) Compound 11a was decarboxylated by 1,2,3-indantrione in acetonitrile, benzene, or methanol.The initially formed intermediate could be trapped by N-phenylmaleimide (to form 3), by diethyl azodicarboxylate (to form an unstable adduct), by ninhydrin itself (to form 5) or by a proton (in methanol, to form 8). (2) Compound 11d was decarboxylated by phenylbis(trifluoroacetato-O)iodine to yield carbinolamine 12d.cis-2,3-Dideuterio-11d yielded cis-2,3-dideuterio-12d under the same conditions. (3) ACC was decarboxylated by phenanthroquinone to yield oxazole 9, probably by way of oxazoline 10.
