Synthesis and SAR Studies of diarylpyrrole anticoccidial agents

The dimethylamine-substituted pyrrole 19a is the most potent inhibitor of Eimeria tenella PKG (cGMP-dependent protein kinase among the diaryl pyrroles evaluated as anticoccidial agents. 2-(4-Fluorophenyl)-3-(4-pyridinyl)-5-substituted pyrroles were prepared and evaluated as anticoccidial agents in b...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (10), p.2817-2821
Main Authors: Qian, Xiaoxia, Liang, Gui-Bai, Feng, Dennis, Fisher, Michael, Crumley, Tami, Rattray, Sandra, Dulski, Paula M., Gurnett, Anne, Leavitt, Penny Sue, Liberator, Paul A., Misura, Andrew S., Samaras, Samantha, Tamas, Tamas, Schmatz, Dennis M., Wyvratt, Matthew, Biftu, Tesfaye
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Anticoccidial
Antiparasitic agents
Biological and medical sciences
Coccidiostats - chemical synthesis
Coccidiostats - chemistry
Coccidiostats - pharmacology
Cyclic GMP-Dependent Protein Kinases - antagonists & inhibitors
Eimeria tenella
Eimeria tenella - drug effects
Eimeria tenella - enzymology
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Medical sciences
Pharmacology. Drug treatments
Pyrroles - chemical synthesis
Pyrroles - chemistry
Pyrroles - pharmacology
Structure-Activity Relationship
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Summary:The dimethylamine-substituted pyrrole 19a is the most potent inhibitor of Eimeria tenella PKG (cGMP-dependent protein kinase among the diaryl pyrroles evaluated as anticoccidial agents. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.01.041