Abstract
2-(4-Fluorophenyl)-3-(4-pyridinyl)-5-substituted pyrroles were prepared and evaluated as anticoccidial agents in both in vitro and in vivo assays. Among the compounds evaluated, the dimethylamine-substituted pyrrole 19a is the most potent inhibitor of Eimeria tenella PKG (cGMP-dependent protein kinase). Further SAR studies on the side chain of the 2-pyrrolidine nitrogen did not enhance in vivo anticoccidial activity.
MeSH terms
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Animals
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Coccidiostats / chemical synthesis*
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Coccidiostats / chemistry
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Coccidiostats / pharmacology*
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Cyclic GMP-Dependent Protein Kinases / antagonists & inhibitors
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Eimeria tenella / drug effects
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Eimeria tenella / enzymology
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Structure-Activity Relationship
Substances
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Coccidiostats
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Enzyme Inhibitors
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Pyrroles
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Cyclic GMP-Dependent Protein Kinases