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Spirotetrahydro β-Carbolines (Spiroindolones): A New Class of Potent and Orally Efficacious Compounds for the Treatment of Malaria

[Image: see text] The antiplasmodial activity of a series of spirotetrahydro β-carbolines is described. Racemic spiroazepineindole (1) was identified from a phenotypic screen on wild type Plasmodium falciparum with an in vitro IC(50) of 90 nM. Structure−activity relationships for the optimization of...

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Detalles Bibliográficos
Autores principales: Yeung, Bryan K. S., Zou, Bin, Rottmann, Matthias, Lakshminarayana, Suresh B., Ang, Shi Hua, Leong, Seh Yong, Tan, Jocelyn, Wong, Josephine, Keller-Maerki, Sonja, Fischli, Christoph, Goh, Anne, Schmitt, Esther K., Krastel, Philipp, Francotte, Eric, Kuhen, Kelli, Plouffe, David, Henson, Kerstin, Wagner, Trixie, Winzeler, Elizabeth A., Petersen, Frank, Brun, Reto, Dartois, Veronique, Diagana, Thierry T., Keller, Thomas H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2010
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6996867/
https://www.ncbi.nlm.nih.gov/pubmed/20568778
http://dx.doi.org/10.1021/jm100410f