2-Mercaptopyridine N-oxide (pyrithione, PTOH) along with several transition metal ions forms coordination compounds displaying notable biological activities.

Trimethoprim is a synthetic antibiotic that inhibits dihydrofolate reductase (DHFR) which is necessary for the synthesis of purines, amino acids, and thymidylic acid, with prominent selectivity for bacterial DHFR over mammalian DHFR (IC50s = 5 and 30,000 nM, respectively). Trimethoprim is used mainly in the prophylaxis and treatment of urinary tract infections.

Isonicotinic acid hydrazide is an antibacterial agent used primarily as a tuberculostatic by blocking the action of fatty acid synthase by interacting with KatG.

Ethionamide is a second-line antitubercular agent which can inhibit mycolic acid synthesis.

Prothionamide is the second line of drug used in leprosy and in tuberculosis and it is highly effective against Mycobacterium tuberculosis.

Zinc pyrithione是一种具有抗真菌和抗细菌活性的药物，可以通过阻断质子泵（Proton pump）破坏膜转运。