959615-84-0Relevant articles and documents
Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs
Blanco, Delia,Perez-Herran, Esther,Cacho, Mónica,Ballell, Lluís,Castro, Julia,Del Río, Rubén González,Lavandera, José Luis,Remui?án, Modesto J.,Richards, Cindy,Rullas, Joaquin,Vázquez-Mu?iz, María Jesús,Woldu, Ermias,Zapatero-González, María Cleofé,Angulo-Barturen, I?igo,Mendoza, Alfonso,Barros, David
, p. 1868 - 1875 (2015/06/08)
One way to speed up the TB drug discovery process is to search for antitubercular activity among compound series that already possess some of the key properties needed in anti-infective drug discovery, such as whole-cell activity and oral absorption. Here, we present MGIs, a new series of Mycobacterium tuberculosis gyrase inhibitors, which stem from the long-term efforts GSK has dedicated to the discovery and development of novel bacterial topoisomerase inhibitors (NBTIs). The compounds identified were found to be devoid of fluoroquinolone (FQ) cross-resistance and seem to operate through a mechanism similar to that of the previously described NBTI GSK antibacterial drug candidate. The remarkable in vitro and in vivo antitubercular profiles showed by the hits has prompted us to further advance the MGI project to full lead optimization.
Compounds
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Page/Page column 17, (2009/08/14)
Compounds of Formula (I), compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
