Aryl Sulfonamides as a New Antitubercular Series: Discovery, Optimization and Target Identification †
GlaxoSmithKline GSK, 28760 Tres Cantos, Spain
†
Presented at the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain, 8 September 2017.
Proceedings 2017, 1(6), 649; https://doi.org/10.3390/proceedings1060649
Published: 19 October 2017
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
Tuberculosis (TB) remains a major global health problem. An estimated one-third of the world's population is infected with Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis. In 2015, 1.8 million people died from the disease. The development of new anti-TB therapeutics is urgently needed due to the emergence of multi-drug resistant strains (MDR and XDR-TB) as well as the co-infection with other pathogens (e.g., VIH).
World Health Organization (http://www.who.int/tb/publications/global_report/en/).
A Whole Cell HTS with GSK´s two million compound collection using Mycobacterium bovis BCG as a surrogate of Mycobacterium tuberculosis and subsequent confirmation of the obtained hits in Mtb was performed. As a result, several families with interesting antitubercular features were identified. An aryl sulfonamide series presenting a particularly promising profile was prioritized for optimization.
Details of the phenotypic screen, the initial Hit profile, preliminary SAR, Medicinal Chemistry activities and identification of the biological target will be presented.
Acknowledgments
We would like to thank the GATB for providing financial support.
Conflicts of Interest
The authors declare no conflict of interest.
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MDPI and ACS Style
García, A.P. Aryl Sulfonamides as a New Antitubercular Series: Discovery, Optimization and Target Identification. Proceedings 2017, 1, 649. https://doi.org/10.3390/proceedings1060649
AMA Style
García AP. Aryl Sulfonamides as a New Antitubercular Series: Discovery, Optimization and Target Identification. Proceedings. 2017; 1(6):649. https://doi.org/10.3390/proceedings1060649
Chicago/Turabian StyleGarcía, Arancha Pérez. 2017. "Aryl Sulfonamides as a New Antitubercular Series: Discovery, Optimization and Target Identification" Proceedings 1, no. 6: 649. https://doi.org/10.3390/proceedings1060649
