title: Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents.
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.
authors.affiliation: 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
authors.forename: Gui-Bai
authors.initials: GB
authors.lastname: Liang
authors.forename: Xiaoxia
authors.initials: X
authors.lastname: Qian
authors.forename: Tesfaye
authors.initials: T
authors.lastname: Biftu
authors.forename: Dennis
authors.initials: D
authors.lastname: Feng
authors.forename: Michael
authors.initials: M
authors.lastname: Fisher
authors.forename: Tami
authors.initials: T
authors.lastname: Crumley
authors.forename: Sandra J
authors.initials: SJ
authors.lastname: Darkin-Rattray
authors.forename: Paula M
authors.initials: PM
authors.lastname: Dulski
authors.forename: Anne
authors.initials: A
authors.lastname: Gurnett
authors.forename: Penny Sue
authors.initials: PS
authors.lastname: Leavitt
authors.forename: Paul A
authors.initials: PA
authors.lastname: Liberator
authors.forename: Andrew S
authors.initials: AS
authors.lastname: Misura
authors.forename: Samantha
authors.initials: S
authors.lastname: Samaras
authors.forename: Tamas
authors.initials: T
authors.lastname: Tamas
authors.forename: Dennis M
authors.initials: DM
authors.lastname: Schmatz
authors.forename: Matthew
authors.initials: M
authors.lastname: Wyvratt
mesh_terms: D003049:Coccidiostats / Q000737:chemistry* / Q000494:pharmacology*; D017869:Cyclic GMP-Dependent Protein Kinases / Q000037:antagonists & inhibitors; D006900:Hydroxylation; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D003049:Coccidiostats; D011758:Pyrroles; D017869:Cyclic GMP-Dependent Protein Kinases