Abstract:
: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.
journal_name
Antimicrob Agents Chemotherjournal_title
Antimicrobial agents and chemotherapyauthors
Blanco D,Perez-Herran E,Cacho M,Ballell L,Castro J,González Del Río R,Lavandera JL,Remuiñán MJ,Richards C,Rullas J,Vázquez-Muñiz MJ,Woldu E,Zapatero-González MC,Angulo-Barturen I,Mendoza A,Barros Ddoi
10.1128/AAC.03913-14subject
Has Abstractpub_date
2015-04-01 00:00:00pages
1868-75issue
4eissn
0066-4804issn
1098-6596pii
AAC.03913-14journal_volume
59pub_type
杂志文章abstract::The report describes the establishment and characterization of a mouse xenograft transplantation model for the study of papillomavirus infection of bovine skin. Calf scrotal skin was inoculated with bovine papillomavirus type 2 before grafting it to the dorsum of severe combined immunodeficient mice. The grafted skin ...
journal_title:Antimicrobial agents and chemotherapy
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journal_title:Antimicrobial agents and chemotherapy
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journal_title:Antimicrobial agents and chemotherapy
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