Synthesis and SAR studies of potent imidazopyridine anticoccidial agents

Diaryl imidazo[1,2- a]pyridine derivatives bearing N-alkyl amino substituents have been synthesized and evaluated as highly potent Et-PKG inhibitor and efficacious anticoccidial agents. Diaryl imidazo[1,2- a]pyridine derivatives, such as 6a and 7i, have been synthesized and found to be potent inhibi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-07, Vol.17 (13), p.3558-3561
Main Authors: Liang, Gui-Bai, Qian, Xiaoxia, Feng, Dennis, Fisher, Michael, Brown, Christine M., Gurnett, Anne, Leavitt, Penny Sue, Liberator, Paul A., Misura, Andrew S., Tamas, Tamas, Schmatz, Dennis M., Wyvratt, Matthew, Biftu, Tesfaye
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Biological and medical sciences
Chemistry, Pharmaceutical - methods
Coccidiosis
Coccidiosis - drug therapy
Coccidiostats - chemistry
Coccidiostats - pharmacology
Cyclic GMP-Dependent Protein Kinases - metabolism
Drug Design
Eimeria tenella
Et-PKG
Imidazoles - chemistry
Imidazopyridine
Medical sciences
Models, Chemical
Pharmacology. Drug treatments
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
Pyridines - chemistry
Pyridines - pharmacology
Structure-Activity Relationship
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Summary:Diaryl imidazo[1,2- a]pyridine derivatives bearing N-alkyl amino substituents have been synthesized and evaluated as highly potent Et-PKG inhibitor and efficacious anticoccidial agents. Diaryl imidazo[1,2- a]pyridine derivatives, such as 6a and 7i, have been synthesized and found to be potent inhibitors of parasite PKG activity. The most potent compounds are the 7-isopropylaminomethyl analog 6a and 2-isopropylamino analog 7i. These compounds are also fully active in in vivo assay as anticoccidial agents at 25 ppm in feed.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.041