Syntheses of mycobactin analogs as potent and selective inhibitors of Mycobacterium tuberculosis |
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Authors: | Raúl E Juárez-Hernández Scott G Franzblau Marvin J Miller |
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Affiliation: | Department of Chemistry and Biochemistry, University of Notre Dame, 251 Nieuwland Science Hall, Notre Dame, IN 46556, USA. mmiller1@nd.edu. |
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Abstract: | Three analogs of mycobactin T, the siderophore secreted by Mycobacterium tuberculosis (Mtb) were synthesized and screened for their antibiotic activity against Mtb H(37)Rv and a broad panel of Gram-positive and Gram-negative bacteria. The synthetic mycobactins were potent (MIC(90) 0.02-0.88 μM in 7H12 media) and selective Mtb inhibitors, with no inhibitory activity observed against any other of the microorganisms tested. The maleimide-containing analog 40 represents a versatile platform for the development of mycobactin-drug conjugates, as well as other applications. |
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