The Medicinal Chemistry of Tuberculosis Chemotherapy

The development of effective chemotherapy for the treatment of tuberculosis (TB) began in the 1940s and has been reinvigorated recently due to concern regarding the emergence of highly drug-resistant TB strains. This chapter explores the medicinal chemistry efforts that gave rise to current frontline and second-line drugs in global use today and attempts to comprehensively summarize ongoing discovery and lead optimization programs being conducted in both the private and the public sector. TB has a large number of disease-specific considerations and constraints that introduce significant complexity in drug discovery efforts. Conceptually, the disease encompasses all the drug discovery challenges of both infectious diseases and oncology, and integrating these considerations into programs that often demand collaboration between industry and academia is both challenging and rewarding.