Bioprospecting for antituberculosis leads from microbial metabolites

Microbial metabolites have been an important source of tuberculosis (TB) therapeutics, but the last truly novel drug that was approved for the treatment of TB was discovered 40 years ago. In light of the growing threat of multi-drug resistance, recent advances have been made to accelerate the discovery rate of novel TB drugs including diversifying strategies for environmental strains, and high-throughput screening assays. This review will discuss the approaches used in biodiversity- and taxonomy-guided microbial natural product library construction, specific cell-based and target-based high-throughput screening assays and early-stage dereplication processes by liquid chromatography-mass spectrometry (LC-MS). New antituberculosis natural products that have been recently discovered are highlighted.