REVIEW Protionamide (also known as prothionamide) is used in the treatment of tuberculosis and leprosy. Protionamide mode of action involves bioactivation via flavin monoxygenase, which then form covalent adducts with nicotinamide adenine dinucleotide (NAD) with protinamide, and that these adducts are tight-binding inhibitors of M. tuberculosis and M. leprae enoyl CoA reductase InhA, the ultimate target of these. The crystal structures of the inhibited M. leprae and M. tuberculosis InhA complexes provide the molecular details of target-drug interactions. The purified ETH-NAD and PTH-NAD adducts both showed nanomolar Kis against M. tuberculosis and M. leprae InhA.
Wang F, Langley R, Gulten G, Dover LG, Besra GS, Jacobs WR Jr, Sacchettini JC. Mechanism of thioamide drug action against tuberculosis and leprosy. J Exp Med. 2007 Jan 22;204(1):73-8. Epub 2007 Jan 16.
Fajardo TT, Guinto RS, Cellona RV, Abalos RM, Dela Cruz EC, Gelber RH. A clinical trial of ethionamide and prothionamide for treatment of lepromatous leprosy. Am J Trop Med Hyg. 2006 Mar;74(3):457-61.