OBJECTIVE: Our aim was to identify natural products with anti-tubercular activity. RESULTS: A set of ~ 500 purified natural product compounds was screened for inhibition against the human pathogen Mycobacterium tuberculosis. A series of cyclic hexapeptides with anti-tubercular activity was identified. Five analogs from a set of sixteen closely related compounds were active, with minimum inhibitory concentrations ranging from 2.3 to 8.9 μM. Eleven structural analogs had no significant activity (MIC > 20 μM) demonstrating structure activity relationship. Sequencing of resistant mutant isolates failed to identify changes accounting for the resistance phenotype.
- Anti-tubercularAntibacterialAntibiotic ResistanceMycobacteriaNatural ProductAntitubercular AgentsBiological ProductsHumansMicrobial Sensitivity TestsMycobacterium TuberculosisOligopeptidesStructure-Activity Relationship