For six decades, natural products have taken a central role in the discovery of new antimicrobial agents. The structural diversity of these compounds and its ability for interacting specifically with biological target molecules has laid an ideal foundation in the development of new drugs. The importance of fungus in TB treatment can be observed in several aminoglycosides isolated from different Streptomyces species, which are used as second line drug. Due to the fundamental importance of fungi in the past and present of TB treatment, several research groups isolated and evaluated a number of compounds from different fungal species against Mycobacterium tuberculosis, which will be described in this chapter.
Keywords: Tuberculosis; Mycobacterium tuberculosis; natural products; fungus; semi-synthesis; synthesis; analogues; treatment; multi-drug-resistant tuberculosis (MDR TB); extensive-drug-resistant tuberculosis (XDR TB); target; mechanism of action; biological evaluation; drug development.