Tuberculosis (TB) is the biggest global killer in history. One of the main objectives for fighting TB is to find a shorter treatment and also to target multidrug-resistant (MDR) and extensively drug-resistant XDR strains. Nowadays, finding and developing new compounds that are active against tuberculosis constitutes a main objective for the Diseases of the Developing World (DDW) center of GlaxoSmithKline (GSK) at Tres Cantos. At our site, both target- and cell-based screens have been approached to identify new anti-TB compounds. Mtb phenotypic HTS represents the main source of new chemical entities, although the major challenge resides in their successful optimization and the elucidation of their mechanism of action (MoA).
In this work, we will present a new hit (GSK1) from a whole cell phenotypic screen and also Medicinal Chemistry efforts in the Hit Optimization program to overcome the risks associated with the Lead.
Acknowledgments
We would like to thank Wellcome Trust for the financial support.
Conflicts of Interest
The authors declare no conflict of interest.
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