N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents

Gui-Bai Liang; Xiaoxia Qian; Dennis Feng; Michael Fisher; Tami Crumley; Sandra J Darkin-Rattray; Paula M Dulski; Anne Gurnett; Penny Sue Leavitt; Paul A Liberator; Andrew S Misura; Samantha Samaras; Tamas Tamas; Dennis M Schmatz; Matthew Wyvratt; Tesfaye Biftu

doi:10.1016/j.bmcl.2008.01.104

N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2019-22. doi: 10.1016/j.bmcl.2008.01.104. Epub 2008 Feb 2.

Authors

Gui-Bai Liang¹, Xiaoxia Qian, Dennis Feng, Michael Fisher, Tami Crumley, Sandra J Darkin-Rattray, Paula M Dulski, Anne Gurnett, Penny Sue Leavitt, Paul A Liberator, Andrew S 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. gui-bai_liang@merck.com

PMID: 18276140
DOI: 10.1016/j.bmcl.2008.01.104

Abstract

Diaryl-(4-piperidinyl)-pyrrole derivatives bearing cyclic amine substituents have been synthesized and evaluated as anticoccidial agents. Improvements in potency of Et-PKG inhibition, such as azetidine derivative 3a, and broad spectrum anticoccidial activities in feed, such as morpholine derivative 8c, have been achieved.

MeSH terms

Animals
Chickens
Coccidiosis / drug therapy*
Coccidiostats / chemical synthesis
Coccidiostats / pharmacology*
Cyclic GMP-Dependent Protein Kinases / antagonists & inhibitors
Eimeria / drug effects*
Eimeria / enzymology
Female
Molecular Structure
Oocysts / drug effects
Oocysts / physiology
Protein Kinase Inhibitors / pharmacology
Pyrroles / chemical synthesis
Pyrroles / chemistry
Pyrroles / pharmacology*
Structure-Activity Relationship

Substances

Coccidiostats
Protein Kinase Inhibitors
Pyrroles
Cyclic GMP-Dependent Protein Kinases