N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents.
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.
Liang
Gui-Bai
GB
Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. gui-bai_liang@merck.com
Qian
Xiaoxia
X
Feng
Dennis
D
Fisher
Michael
M
Crumley
Tami
T
Darkin-Rattray
Sandra J
SJ
Dulski
Paula M
PM
Gurnett
Anne
A
Leavitt
Penny Sue
PS
Liberator
Paul A
PA
Misura
Andrew S
AS
Samaras
Samantha
S
Tamas
Tamas
T
Schmatz
Dennis M
DM
Wyvratt
Matthew
M
Biftu
Tesfaye
T
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
D003049:Coccidiostats; D047428:Protein Kinase Inhibitors; D011758:Pyrroles; D017869:Cyclic GMP-Dependent Protein Kinases