Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis.

ABSTRACT: A new class of Cyclophostin and Cyclipostins (CyC) analogs have been investigated against Mycobacterium tuberculosis H37Rv (M. tb) grown either in broth medium or inside macrophages. Our compounds displayed a diversity of action by acting either on extracellular M. tb bacterial growth only, or both intracellularly on infected macrophages as well as extracellularly on bacterial growth with very low toxicity towards host macrophages. Among the eight potential CyCs identified, CyC ₁₇ exhibited the best extracellular antitubercular activity (MIC₅₀ = 500 nM). This compound was selected and further used in a competitive labelling/enrichment assay against the activity-based probe Desthiobiotin-FP in order to identify its putative target(s). This approach, combined with mass

SUBMITTER: Nguyen PC 

PROVIDER: S-EPMC5603573 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature