Journal of Medicinal Chemistry · 2005 · 235 citations · 20 references
Life SciencesMedicinal ChemistryMicrobiologyAntimicrobial PharmacologyEnzymologyMicrobial MetabolismAntibacterial AgentsAntibacterial PharmacologyAntibacterial ResistanceAntibiotic ResistanceEnzyme InhibitionTuberculosis PharmacotherapyMycobacterium Tuberculosis InfectionMycobacterium Tuberculosis PathogenesisNucleoside AnalogsSiderophore BiosynthesisTuberculosis Drug Development
A rationally designed nucleoside inhibitor of Mycobacterium tuberculosis growth (MIC(99) = 0.19 microM) that disrupts siderophore biosynthesis was identified. The activity is due to inhibition of the adenylate-forming enzyme MbtA which is involved in biosynthesis of the mycobactins.
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