Anticoccidial derivatives of 6-azauracil. 5. Potentiation by benzophenone side chains.
Attachment of p-benzophenone side chains at N1 was found to be one of the most effective modifications for enhancing the potency of 6-azauracil against a broad spectrum of coccidia in chickens. Compound 20 was about 1000-fold more potent than 6-azauracil. Structure-activity relationships paralleled those found in a previously reported series of related analogues containing diphenyl sulfide and sulfone side chains. Drug metabolism studies showed the ketones to be reduced rapidly to carbinols, which are the prevalent species in vivo.
D000818:Animals; D001577:Benzophenones / Q000138:chemical synthesis / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D002645:Chickens; D003049:Coccidiostats / Q000097:blood / Q000138:chemical synthesis*; D004539:Eimeria / Q000187:drug effects; D006207:Half-Life; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D001577:Benzophenones; D003049:Coccidiostats; D014498:Uracil; C100248:azauracil