Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents

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

doi:10.1016/j.bmcl.2006.08.127

Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents

Bioorg Med Chem Lett. 2006 Dec 1;16(23):5978-81. doi: 10.1016/j.bmcl.2006.08.127. Epub 2006 Sep 26.

Authors

Dennis Feng¹, Michael Fisher, Gui-Bai Liang, Xiaoxia Qian, Chris Brown, Anne Gurnett, Penny Sue Leavitt, Paul A Liberator, John Mathew, Andrew Misura, Samantha Samaras, 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. dennis_feng@merck.com <dennis_feng@merck.com>

PMID: 17000105
DOI: 10.1016/j.bmcl.2006.08.127

Abstract

Compounds 10a-10d and 10i are very potent inhibitors of Eimeria tenella cGMP-dependent protein kinase (0.081-0.32 nM) and are very efficacious antiparasitic agents in vivo when administered to chickens at 12.5-25 ppm levels in the feed.

MeSH terms

Animals
Coccidiostats / chemical synthesis*
Coccidiostats / chemistry
Coccidiostats / pharmacology*
Eimeria / drug effects
Imidazoles / chemical synthesis*
Imidazoles / chemistry
Imidazoles / pharmacology*
Molecular Structure
Pyridines / chemical synthesis*
Pyridines / chemistry*
Pyridines / pharmacology*
Structure-Activity Relationship

Substances

2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo(1,2-a)pyridine
Coccidiostats
Imidazoles
Pyridines
pyridine