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

• Published in: Journal of medicinal chemistry Vol. 23; no. 10; pp. 1083 - 1087
• Main Authors: Miller, Max W, Mylari, Banavara L, Howes, Harold L, Figdor, Sanford K, Lynch, Martin J, Lynch, John E, Koch, Richard C
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 01-10-1980
• Subjects: 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
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/jm00184a005

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.