Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6- phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces parasite growth in vitro

A high throughput screen of the NIH’s MLSMR collection of ~340,000 compounds was undertaken to identify compounds that inhibit Plasmodium falciparum glucose-6-phosphate dehydrogenase (PfG6PD). PfG6PD is essential for proliferating and propagating P. falciparum and differs structurally and mechanisti...

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Autori principali: Preuss, Janina, Maloney, Patrick, Peddibhotla, Satyamaheshwar, Hedrick, Michael P., Hershberger, Paul, Gosalia, Palak, Milewski, Monika, Li, Yujie Linda, Sugarman, Eliot, Hood, Becky, Suyama, Eigo, Nguyen, Kevin, Vasile, Stefan, Sergienko, Eduard, Mangravita-Novo, Arianna, Vicchiarelli, Michael, McAnally, Danielle, Smith, Layton H., Roth, Gregory P., Diwan, Jena, Chung, Thomas D.Y., Jortzik, Esther, Rahlfs, Stefan, Becker, Katja, Pinkerton, Anthony B., Bode, Lars
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2012
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC3530835/
https://ncbi.nlm.nih.gov/pubmed/22813531
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300833h
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