title: N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents.
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.
authors.affiliation: Merck Research Laboratories, Department of Medicinal Chemistry, 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: 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
authors.forename: Tesfaye
authors.initials: T
authors.lastname: Biftu
mesh_terms: D000818:Animals; D002645:Chickens; D003048:Coccidiosis / Q000188:drug therapy*; D003049:Coccidiostats / Q000138:chemical synthesis / Q000494:pharmacology*; D017869:Cyclic GMP-Dependent Protein Kinases / Q000037:antagonists & inhibitors; D004539:Eimeria / Q000187:drug effects* / Q000201:enzymology; D005260:Female; D015394:Molecular Structure; D033661:Oocysts / Q000187:drug effects / Q000502:physiology; D047428:Protein Kinase Inhibitors / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D003049:Coccidiostats; D047428:Protein Kinase Inhibitors; D011758:Pyrroles; D017869:Cyclic GMP-Dependent Protein Kinases