Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents.
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.
Liang
Gui-Bai
GB
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
Qian
Xiaoxia
X
Biftu
Tesfaye
T
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
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
D003049:Coccidiostats; D011758:Pyrroles; D017869:Cyclic GMP-Dependent Protein Kinases