Synthesis and SAR studies of potent imidazopyridine anticoccidial agents

Gui-Bai Liang; Xiaoxia Qian; Dennis Feng; Michael Fisher; Christine M Brown; Anne Gurnett; Penny Sue Leavitt; Paul A Liberator; Andrew S Misura; Tamas Tamas; Dennis M Schmatz; Matthew Wyvratt; Tesfaye Biftu

doi:10.1016/j.bmcl.2007.04.041

Synthesis and SAR studies of potent imidazopyridine anticoccidial agents

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3558-61. doi: 10.1016/j.bmcl.2007.04.041. Epub 2007 Apr 24.

Authors

Gui-Bai Liang¹, Xiaoxia Qian, Dennis Feng, Michael Fisher, Christine M Brown, Anne Gurnett, Penny Sue Leavitt, Paul A Liberator, Andrew S Misura, Tamas Tamas, Dennis M Schmatz, Matthew Wyvratt, Tesfaye Biftu

Affiliation

¹ Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. gui-bai_liang@merck.com <gui-bai_liang@merck.com>

PMID: 17475489
DOI: 10.1016/j.bmcl.2007.04.041

Abstract

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.

MeSH terms

Animals
Chemistry, Pharmaceutical / methods
Coccidiosis / drug therapy*
Coccidiostats / chemistry
Coccidiostats / pharmacology*
Cyclic GMP-Dependent Protein Kinases / metabolism
Drug Design
Eimeria tenella
Imidazoles / chemistry*
Models, Chemical
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / pharmacology*
Pyridines / chemistry*
Pyridines / pharmacology*
Structure-Activity Relationship

Substances

Coccidiostats
Imidazoles
Protein Kinase Inhibitors
Pyridines
Cyclic GMP-Dependent Protein Kinases