N-Alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 6, 2008, Pages 2019-2022

  Liang, Gui Bai ^a   Qian, Xiaoxia ^a   Feng, Dennis ^a   Fisher, Michael ^a   Crumley, Tami ^a   Darkin Rattray, Sandra J ^a   Dulski, Paula M ^a   Gurnett, Anne ^a   Leavitt, Penny Sue ^a   Liberator, Paul A ^a   Misura, Andrew S ^a   Samaras, Samantha ^a   Tamas, Tamas ^a   Schmatz, Dennis M ^a   Wyvratt, Matthew ^a   Biftu, Tesfaye ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Coccidiosis; PKG; PKG inhibitor

Indexed keywords

ALKYL GROUP; AMINE; AZETIDINE DERIVATIVE; COCCIDIOSTATIC AGENT; CYCLIC GMP DEPENDENT PROTEIN KINASE; CYCLIC GMP DEPENDENT PROTEIN KINASE INHIBITOR; HETEROCYCLIC COMPOUND; HYDROXYPROLINE; MORPHOLINE DERIVATIVE; PIPERIDINE DERIVATIVE; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; PYRROLE DERIVATIVE;

ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; EIMERIA; ENZYME INHIBITION; INHIBITION KINETICS; NONHUMAN;

ANIMALS; CHICKENS; COCCIDIOSIS; COCCIDIOSTATS; CYCLIC GMP-DEPENDENT PROTEIN KINASES; EIMERIA; FEMALE; MOLECULAR STRUCTURE; OOCYSTS; PROTEIN KINASE INHIBITORS; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 40749109331     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.01.104     Document Type: Article

References (11)

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10. 1H NMR and MS.
11. Three-day-old chicks are randomly placed on medicated or control diets for the duration of the experiment. Following 24 h premedication, in each replicate one bird is infected with Eimeria acervulina, the other bird is infected with E. tenella. The E. acervulina portion of the experiment is terminated on Day 5, the E. tenella on Day 6 post infection. Treatments which provide at least 80% reduction in oocyst production are rated (3), those with 50-79% are rated (2), and those with <50% are rated (0). For a detailed description, please see Ref. 1.