Nowadays, tuberculosis (TB) is an important global public health problem, being responsible
for millions of TB-related deaths worldwide. Due to the increased number of cases and resistance of
Mycobacterium tuberculosis to all drugs used for the treatment of this disease, we desperately need new
drugs and strategies that could reduce treatment time with fewer side effects, reduced cost and highly
active drugs against resistant strains and latent disease. Considering that, 4H-1,3-benzothiazin-4-one is a
promising class of antimycobacterial agents in special against TB-resistant strains being the aim of this
review the discussion of different aspects of this chemical class such as synthesis, mechanism of action,
medicinal chemistry and combination with other drugs.