Anticoccidial derivatives of 6-azauracil. 3. Synthesis, high activity, and short plasma half-life of 1-phenyl-6-azauracils containing sulfonamide substituents

J Med Chem. 1980 Oct;23(10):1083-7. doi: 10.1021/jm00184a005.

Abstract

A series of 1-phenyl-6-azauracils containing sulfonamide substituents was prepared. In contrast to previous 1-phenyl-6-azauracils, some of these sulfonamides combine high activity against Eimeria tenella infections in chickens with a very rapid rate of clearance from plasma. Most active was 1-[3'-chloro-5'-methyl-4'-(morpholinylsulfonyl)phenyl]-6-azauracil, with a minimum effective concentration in feed of about 10 ppm.

MeSH terms

  • Animals
  • Chickens
  • Coccidiosis / drug therapy
  • Coccidiostats / chemical synthesis*
  • Half-Life
  • Male
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Uracil / analogs & derivatives*
  • Uracil / blood
  • Uracil / chemical synthesis
  • Uracil / pharmacology

Substances

  • Coccidiostats
  • Sulfonamides
  • Uracil
  • azauracil