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

Fraser Cunningham,Jorge Esquivias,Raquel Fernández Menéndez,Arancha Pérez,Ana Guardia,Jaime Escribano,Cristina Rivero,Mythily Vimal,Monica Cacho,Paco de Dios-Anton,Maria Santos Martinez-Martinez,Elena Jimenez,Leticia Huertas Valentín,María José Rebollo-López,Eva Maria Lopez-Roman,Verónica Sousa-Morcuende,Joaquín Rullas,Margaret Neu,Chun-wa Chung,Robert H. Bates

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

2020

In the course of optimizing a novel indazole sulfonamide series that inhibits β-ketoacyl-ACP synthase (KasA) of Mycobacterium tuberculosis, a mutagenic aniline metabolite was identified. Further le...

Keywords:

Metabolite
Aniline
Indazole
Mycobacterium tuberculosis
Tuberculosis
Binding site
ATP synthase
Chemistry
Biochemistry

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