119111-63-6Relevant articles and documents
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.
