Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents

Gui-Bai Liang; Xiaoxia Qian; Tesfaye Biftu; 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

doi:10.1016/j.bmcl.2005.06.096

Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4570-3. doi: 10.1016/j.bmcl.2005.06.096.

Authors

Gui-Bai Liang¹, Xiaoxia Qian, Tesfaye Biftu, 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

Affiliation

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

PMID: 16087336
DOI: 10.1016/j.bmcl.2005.06.096

Abstract

Diaryl-(4-piperidinyl)-pyrrole derivatives bearing hydroxylated N-alkyl substituents have been synthesized and evaluated as anticoccidial agents. High potency in Et-PKG inhibition and broad-spectrum anticoccidial activities have been observed on compounds, such as 4b and 5h, which are fully efficacious in vivo at 50 ppm in feed.

MeSH terms

Coccidiostats / chemistry*
Coccidiostats / pharmacology*
Cyclic GMP-Dependent Protein Kinases / antagonists & inhibitors
Hydroxylation
Pyrroles / chemistry*
Pyrroles / pharmacology*
Structure-Activity Relationship

Substances

Coccidiostats
Pyrroles
Cyclic GMP-Dependent Protein Kinases