
pmid: 16464591
Compounds 10a (IC50 110 pM) and 21 (IC50 40 pM) are the most potent inhibitors of Eimeria tenella cGMP-dependent protein kinase activity reported to date and are efficacious in the in vivo antiparasitic assay when administered to chickens at 12.5 and 6.25 ppm levels in the feed. However, both compounds are positive in the Ames microbial mutagenesis assay which precludes them from further development as antiprotozoal agents in the absence of negative lifetime rodent carcinogenicity studies.
Male, Molecular Structure, Coccidiosis, Mutagenicity Tests, Pyridines, Antiprotozoal Agents, Imidazoles, Oocysts, Stereoisomerism, Animal Feed, Rats, Rats, Sprague-Dawley, Structure-Activity Relationship, Parasitic Sensitivity Tests, Cyclic GMP-Dependent Protein Kinases, Animals, Enzyme Inhibitors, Chickens, Eimeria tenella
Male, Molecular Structure, Coccidiosis, Mutagenicity Tests, Pyridines, Antiprotozoal Agents, Imidazoles, Oocysts, Stereoisomerism, Animal Feed, Rats, Rats, Sprague-Dawley, Structure-Activity Relationship, Parasitic Sensitivity Tests, Cyclic GMP-Dependent Protein Kinases, Animals, Enzyme Inhibitors, Chickens, Eimeria tenella
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