Exploring the SAR of the β-Ketoacyl-ACP Synthase Inhibitor GSK3011724A and Optimization around a Genotoxic Metabolite

Author:

Cunningham Fraser1,Esquivias Jorge1,Fernández-Menéndez Raquel1,Pérez Arancha1,Guardia Ana1,Escribano Jaime1,Rivero Cristina1,Vimal Mythily2,Cacho Mónica1ORCID,de Dios-Antón Paco1,Martínez-Martínez María Santos1,Jiménez Elena1,Huertas Valentín Leticia1,Rebollo-López María José1,López-Román Eva María1,Sousa-Morcuende Verónica1,Rullas Joaquín1,Neu Margaret2,Chung Chun-wa2,Bates Robert H.1ORCID

Affiliation:

1. Global Health R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, 28760 Madrid, Spain

2. GlaxoSmithKline, Gunnels Wood Road, Stevenage SG1 2NY, U.K.

Funder

TB Alliance

Publisher

American Chemical Society (ACS)

Subject

Infectious Diseases

Reference29 articles.

1. Tuberculosis: A disease without boundaries

2. WHO. (2015) Global Tuberculosis Report 2015. http://apps.who.int/iris/bitstream/10665/191102/1/9789241565059_eng.pdf (accessed June 12, 2019).

3. WHO. (2019) Global Tuberculosis Report 2019. https://apps.who.int/iris/bitstream/handle/10665/329368/9789241565714-eng.pdf?ua=1 (accessed January 31, 2020).

4. Identification of KasA as the cellular target of an anti-tubercular scaffold

5. Synergistic Lethality of a Binary Inhibitor of Mycobacterium tuberculosis KasA

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