Abstract

Preliminary study of three new sulfonamides as intestinal chemotherapeutic agents is reported : 2-sulfanilamido-5-carbamylthiazole, 2-(N⁴-succinamylsulfanilamido)-thiazole, and 2-(N⁴-succinylsulfanilamido)- 1 , 3, 4-thiadiazole.

The presence of the carbamyl group in the 5-position of sulfathiazole greatly reduces absorption from the gastro-intestinal tract and activity in vitro. However, marked anti-coli action was demonstrated in mice and dogs. Sulfacarbamylthiazole is relatively stable and activity is apparently due to the drug per se.

Replacement of the carboxy group of succinylsulfathiazole with the carbamyl group yields a compound considerably more labile than the parent drug. While absorption was slight following oral administration of succinamylsulfathiazole to mice and dogs, the drug showed but little anti-coli activity in vivo.

Substitution of the succinyl radical in the N⁴-position of sulfathiadiazole resuits in a compound highly active in the intestinal tract of both mice and dogs and only slightly absorbed into the blood. The anti-coli activity of succinylsulfathiadiazole was found to be much greater than that of sulfathalidine in mice and about equal to the latter drug in dogs. Data seem to establish succinylsulfathiadiazole as a potentially useful drug for trial in therapy of enteric infections.