Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria

[Image: see text] A series of 5-aryl-2-amino-imidazothiadiazole (ITD) derivatives were identified by a phenotype-based high-throughput screening using a blood stage Plasmodium falciparum (Pf) growth inhibition assay. A lead optimization program focused on improving antiplasmodium potency, selectivit...

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Detalles Bibliográficos
Autores principales: Taft, Benjamin R., Yokokawa, Fumiaki, Kirrane, Tom, Mata, Anne-Catherine, Huang, Richard, Blaquiere, Nicole, Waldron, Grace, Zou, Bin, Simon, Oliver, Vankadara, Subramanyam, Chan, Wai Ling, Ding, Mei, Sim, Sandra, Straimer, Judith, Guiguemde, Armand, Lakshminarayana, Suresh B., Jain, Jay Prakash, Bodenreider, Christophe, Thompson, Christopher, Lanshoeft, Christian, Shu, Wei, Fang, Eric, Qumber, Jafri, Chan, Katherine, Pei, Luying, Chen, Yen-Liang, Schulz, Hanna, Lim, Jessie, Abas, Siti Nurdiana, Ang, Xiaoman, Liu, Yugang, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Gamo, Francisco Javier, Crespo-Fernandez, Benigno, Rosenthal, Philip J., Cooper, Roland A., Tumwebaze, Patrick, Aguiar, Anna Caroline Campos, Campo, Brice, Campbell, Simon, Wagner, Jürgen, Diagana, Thierry T., Sarko, Christopher
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9278664/
https://www.ncbi.nlm.nih.gov/pubmed/35229610
http://dx.doi.org/10.1021/acs.jmedchem.1c01995

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