6-Azathymine is a competitive antagonist of the growth of Streptococcus faecalis (8043) and several other strains of microorganisms. Studies of the mechanism of action of 6-Azathymine reveal that S. faecalis can convert the analog to the corresponding deoxyriboside, azathymidine.

The administration of 6-Azathymine to the mouse leads to the urinary elimination not only of free Azathymine, but also of various metabolites of it. Following the administration of 6-Azathymine-5- ¹⁴ C to mice, radioactivity is found in all tissues investigated, not only in the form of free Azathymine, but also as metabolic derivatives.