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. Author manuscript; available in PMC: 2017 Jun 17.
Published in final edited form as: ACS Chem Biol. 2016 Apr 7;11(6):1639–1646. doi: 10.1021/acschembio.6b00110

Figure 1.

Figure 1

(a) Schematic representation of the winnowing of ~123 000 small organic molecules to 18 showing inhibition of both Eis enzymatic activity and growth of Mtb K204 in the presence of KAN. (b) Structures of the 41 Eis inhibitors (with an isothiazole S,S-dioxide heterocyclic scaffold) for which IC50 against pure Eis enzyme and MIC values against strains H37Rv and K204 of Mtb have been determined. Note: Compounds highlighted in turquoise are those for which MIC values of KAN against Mtb K204 were found to be <2.5–5 µg/mL. Compounds highlighted in gray are those for which MIC values of KAN against Mtb K204 were found to be >5–10 µg/mL. Compounds highlighted in fuchsia are those for which the X-ray structure in complex with EisC204A and CoA has been determined.