Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 20, 2005, Pages 4570-4573

  Liang, Gui Bai ^a   Qian, Xiaoxia ^a   Biftu, Tesfaye ^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  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Coccidiosis; PKG inhibitor

Indexed keywords

COCCIDIOSTATIC AGENT; CYCLIC GMP DEPENDENT PROTEIN KINASE; PIPERIDINE DERIVATIVE; PYRROLE DERIVATIVE;

ANTIPROTOZOAL ACTIVITY; ARTICLE; DRUG EFFICACY; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; HYDROXYLATION; STRUCTURE ACTIVITY RELATION;

COCCIDIOSTATS; CYCLIC GMP-DEPENDENT PROTEIN KINASES; HYDROXYLATION; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 24344478781     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.06.096     Document Type: Article

References (8)

1. R.B. Williams Int. J. Parasitol. 29 1999 1209
2. A.M. Gurnett, P.A. Liberator, P.M. Dulski, S.P. Salowe, R.G.K. Donald, J.W. Anderson, J. Wiltsie, C.A. Diaz, G. Harris, B. Chang, S.J. Darkin-Rattray, B. Nare, T. Crumley, P.S. Blum, A.S. Misura, T. Tamas, M.K. Sardana, J. Yuan, T. Biftu, and D.M. Schmatz J. Biol. Chem. 277 2002 15913
3. H.I. Wiersma, S.E. Galuska, F.M. Tomley, L.D. Sibley, P.A. Liberator, and R.G.K. Donald Int. J. Parasitol. 34 2004 369
4. S. de-Laszlo, D. Visco, and L. Agarwal Bioorg. Med. Chem. Lett. 8 1998 2689
5. After treatments of infected birds with compounds at indicated level for 24 h, oocysts were counted and scores were given as such: 3 for >80% reduction in oocyst production; 2 for 50-79% reduction; and 0 for <50% reduction. Selected compounds (e.g., 5g and 5h) were tested at lower levels, such as 50 ppm. For a detailed description, please see: T. Biftu, D. Feng, M. Ponpipon, N. Girotra, G.-B. Liang, X. Qian, J. Simeone, L. Chang, A.M. Gurnett, P.A. Liberator, P.M. Dulski, P.S. Leavitt, T. Crumley, A.S. Misura, T. Murphy, S.J. Darkin-Rattray, S. Smamras, T. Tamas, J. Mathew, C. Brown, D. Thompson, D. Schmatz, M.H. Fisher, and M.J. Wyvratt Bioorg. Med. Chem. Lett. 15 2005 3296
6. 1H NMR and MS.
7. T. Cosgrove, and S.M. Shane Poultry 9 2001 10
8. L.R. McDougald P.L. Long Coccidiosis of Man and Domestic Animals 1990 Boca Raton FL 307 320