Tuberculosis (TB) is a highly contagious and potentially life-threatening
infectious disease caused by the bacterium Mycobacterium tuberculosis (MTB).
Despite significant progress in medical science, TB remains a global health concern,
affecting millions of people worldwide. Efforts to combat this disease have led to the
development of various treatment regimens, and research in TB drug discovery
continues to be a crucial area of study. Identifying the new drug targets is essential in
the fight against MDR TB, TDR TB, and XDR TB. Owing to the current situation, the
key aspect of modern drug discovery is based on the concept of structural information
along with functional activity relationships to combat tuberculosis disease. The
structure-activity relationship (SAR) involves understanding the relationship between a
compound's chemical structure and its biological activity. The line of treatment of
MTB addresses multiple targets, such as various ribosomal targets, including the exit
tunnel of the 50S subunit of ribosome, DNA gyrase (GyrB), Inosine-5’-monophosphate
dehydrogenase (IMPD), Adenosine kinases (AK), Chorismate mutase (CM), and many
other targets as well. This chapter provides a complete insight into the existing
medications versus newly developed drug molecules based on SAR, their protein
targets, modes of action, and mechanisms of resistance. By comprehending the intricate
relationship between the chemical structure of drugs and their biological activity, it is
possible to develop more effective therapies to combat this deadly disease.
Keywords: Drugs, Mycobacterium tuberculosis, Protein targets, Resistance mechanism, Structural activity relationship.
