Article
Inhibiting mycobacterial tryptophan synthase by targeting the inter-subunit interface.
Scientific reports - 25 Aug 2017
Abrahams Katherine A, Cox Jonathan A G, Fütterer Klaus, Rullas Joaquín, Ortega-Muro Fátima, Loman Nicholas J, Moynihan Patrick J, Pérez-Herrán Esther, Jiménez Elena, Esquivias Jorge, Barros David, Ballell Lluís, Alemparte Carlos, Besra Gurdyal S
Abstract excerpt
Drug discovery efforts against the pathogen Mycobacterium tuberculosis (Mtb) have been advanced through phenotypic screens of extensive compound libraries. Such a screen revealed sulfolane 1 and indoline-5-sulfonamides 2 and 3 as potent inhibitors of mycobacterial growth. Optimization in the sulfolane series led to compound 4, which has proven activity in an in vivo murine model of Mtb infection. Here we identify...
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