79601-27-7Relevant articles and documents
N-(1H-IMIDAZOL-2-YL)BENZAMIDE COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AS ACTIVE INGREDIENT
-
Page/Page column 41, (2021/04/10)
N-(1H-imidazol-2-yl)benzamide compound of formula (I), or a pharmaceutically acceptable salt, a prodrug, a solvate, or a stereoisomer thereof which is a novel compound exhibiting excellent inhibitory activity against IRAK-4, can be used without side effects for efficient prevention and treatment of diseases mediated by IRAK-4 receptors, particularly autoimmune diseases or lymphomas.
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.
Benzoheterocyclic derivatives
-
Page column 91, (2010/01/21)
A benzoheterocyclic derivative of the following formula [1]: and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist, vasopressin agonist or oxytocin antagonist.
