Abstract
Several analogs of 2,3-diaryl pyrroles were synthesized and evaluated as inhibitors of Eimeria tenella cGMP-dependent protein kinase and in in vivo anticoccidial assays. A 4-fluorophenyl group enhances both in vitro and in vivo activities. The most potent analogs are the 5-(N-methyl, N-ethyl, and N-methylazetidine methyl) piperidyl derivatives 12, 23, and 34. These compounds have a broad spectrum of activity. Based on the in vivo efficacy and cost of synthesis, the N-ethyl analog 23 was chosen as a novel anticoccidial agent for a field trial.
MeSH terms
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Animals
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Biological Availability
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Chickens
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Coccidiosis / drug therapy
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Coccidiostats / chemical synthesis*
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Coccidiostats / pharmacokinetics
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Coccidiostats / pharmacology
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Cyclic GMP-Dependent Protein Kinases / antagonists & inhibitors*
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Eimeria
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Half-Life
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Inhibitory Concentration 50
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Protozoan Proteins / antagonists & inhibitors*
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacokinetics
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Pyrroles / pharmacology
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Structure-Activity Relationship
Substances
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Coccidiostats
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Protozoan Proteins
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Pyrroles
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Cyclic GMP-Dependent Protein Kinases