900514-76-3Relevant academic research and scientific papers
The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold
Sandoval, Elena,Lafuente-Monasterio, María José,Almela, María J.,Casta?eda, Pablo,Jiménez Díaz, María Belén,Martínez-Martínez, María S.,Vidal, Jaume,Angulo-Barturen, í?igo,Bamborough, Paul,Burrows, Jeremy,Cammack, Nicholas,Chaparro, María J.,Coterón, José M.,De Cozar, Cristina,Crespo, Benigno,Díaz, Beatriz,Drewes, Gerard,Fernández, Esther,Ferrer-Bazaga, Santiago,Fraile, María Teresa,Gamo, Francisco J.,Ghidelli-Disse, Sonja,Gómez, Rubén,Haselden, John,Huss, Sophie,León, María Luisa,De Mercado, Jaime,MacDonald, Simon J. F.,Martín Hernando, José Ignacio,Prats, Sara,Puente, Margarita,Rodríguez, Anne,De La Rosa, Juan C.,Rueda, Lourdes,Selenski, Carolyn,Willis, Paul,Wilson, David M.,Witty, Michael,Calderón, Félix
, p. 6880 - 6896 (2017/09/07)
Since the appearance of resistance to the current front-line antimalarial treatments, ACTs (artemisinin combination therapies), the discovery of novel chemical entities to treat the disease is recognized as a major global health priority. From the GSK antimalarial set, we identified an aminoxadiazole with an antiparasitic profile comparable with artemisinin (1), with no cross-resistance in a resistant strains panel and a potential new mode of action. A medicinal chemistry program allowed delivery of compounds such as 19 with high solubility in aqueous media, an acceptable toxicological profile, and oral efficacy. Further evaluation of the lead compounds showed that in vivo genotoxic degradants might be generated. The compounds generated during this medicinal chemistry program and others from the GSK collection were used to build a pharmacophore model which could be used in the virtual screening of compound collections and potentially identify new chemotypes that could deliver the same antiparasitic profile.
MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-?B ACTIVITY AND USE THEREOF
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A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the
