Synthesis and SAR studies of potent imidazopyridine anticoccidial agents.
Diaryl imidazo[1,2-a]pyridine derivatives, such as 6a and 7i, have been synthesized and found to be potent inhibitors of parasite PKG activity. The most potent compounds are the 7-isopropylaminomethyl analog 6a and 2-isopropylamino analog 7i. These compounds are also fully active in in vivo assay as anticoccidial agents at 25 ppm in feed.
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 <gui-bai_liang@merck.com>
Qian
Xiaoxia
X
Feng
Dennis
D
Fisher
Michael
M
Brown
Christine M
CM
Gurnett
Anne
A
Leavitt
Penny Sue
PS
Liberator
Paul A
PA
Misura
Andrew S
AS
Tamas
Tamas
T
Schmatz
Dennis M
DM
Wyvratt
Matthew
M
Biftu
Tesfaye
T
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003048:Coccidiosis / Q000188:drug therapy*; D003049:Coccidiostats / Q000737:chemistry / Q000494:pharmacology*; D017869:Cyclic GMP-Dependent Protein Kinases / Q000378:metabolism; D015195:Drug Design; D016786:Eimeria tenella; D007093:Imidazoles / Q000737:chemistry*; D008956:Models, Chemical; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D003049:Coccidiostats; D007093:Imidazoles; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D017869:Cyclic GMP-Dependent Protein Kinases