thiacetazone

Thiacetazone (also known as thioacetazone) is a small molecule antitubercular agent belonging to the thiosemicarbazone class. It is a prodrug that requires activation by the mycobacterial monooxygenase EthA. Once activated, it targets the HadABC dehydratase complex, specifically inhibiting the cyclopropanation and dehydration steps in the biosynthesis of mycolic acids, which are critical components of the *Mycobacterium tuberculosis* cell wall. Historically, it was used in combination with isoniazid to treat tuberculosis, particularly in resource-limited settings due to its low cost. However, its use has been largely discontinued in many regions due to severe side effects, including Stevens-Johnson syndrome and toxic epidermal necrolysis, which occur at a higher frequency in HIV-infected individuals. Innovative Pharmaceuticals markets a generic version of this drug, although there is some ambiguity as the brand name Acetazone is also frequently associated with acetazolamide.

Brand names

Acetazone

Other names

thioacetazoneamithiozone4-acetamidobenzaldehyde thiosemicarbazone