title: Synthesis and biological activity of imidazopyridine anticoccidial agents: part I.
abstract: Coccidiosis is the major cause of morbidity and mortality in the poultry industry. Protozoan parasites of the genus Eimeria invade the intestinal lining of the avian host causing tissue pathology, poor weight gain, and in some cases mortality. Resistance to current anticoccidials has prompted the search for new therapeutic agents with potent in vitro and in vivo activity against Eimeria. Antiparasitic activity is due to inhibition of a parasite specific cGMP-dependent protein kinase (PKG). In this study, we present the synthesis and biological activity of imidazo[1,2-a]pyridine anticoccidial agents. From this series, several compounds showed subnanomolar in vitro activity and commercial levels of in vivo activity. However, the potential genotoxicity of these compounds precludes them from further development.
authors: SCYNEXIS, Inc., Discovery Chemistry, P.O. Box 12878, Research Triangle Park, NC 27709-2878, United States. andrew.scribner@scynexis.com
authors: Andrew
authors: A
authors: Scribner
authors: Richard
authors: R
authors: Dennis
authors: Jean
authors: J
authors: Hong
authors: Shuliang
authors: S
authors: Lee
authors: Donald
authors: D
authors: McIntyre
authors: David
authors: D
authors: Perrey
authors: Dennis
authors: D
authors: Feng
authors: Michael
authors: M
authors: Fisher
authors: Matthew
authors: M
authors: Wyvratt
authors: Penny
authors: P
authors: Leavitt
authors: Paul
authors: P
authors: Liberator
authors: Anne
authors: A
authors: Gurnett
authors: Chris
authors: C
authors: Brown
authors: John
authors: J
authors: Mathew
authors: Donald
authors: D
authors: Thompson
authors: Dennis
authors: D
authors: Schmatz
authors: Tesfaye
authors: T
authors: Biftu
mesh_terms: D000818:Animals; D001682:Biological Availability; D003049:Coccidiostats / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017869:Cyclic GMP-Dependent Protein Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D004539:Eimeria / Q000187:drug effects* / Q000502:physiology; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D003049:Coccidiostats; D007093:Imidazoles; D011725:Pyridines; D017869:Cyclic GMP-Dependent Protein Kinases