Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents

被引:19
作者
Feng, Dennis
Fisher, Michael
Liang, Gui-Bai
Qian, Xiaoxia
Brown, Chris
Gurnett, Anne
Leavitt, Penny Sue
Liberator, Paul A.
Mathew, John
Misura, Andrew
Samaras, Samantha
Tamas, Tamas
Schmatz, Dennis M.
Wyvratt, Matthew
Biftu, Tesfaye
机构
[1] Merck & Co Inc, Dept Med Chem, Merck Res Labs, Rahway, NJ 07065 USA
[2] Merck & Co Inc, Human & Anim Infect Dis Res, Rahway, NJ 07065 USA
关键词
kinase; coccidiosis; parasite; imidazopyrimidine; PKG inhibitor;
D O I
10.1016/j.bmcl.2006.08.127
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Compounds 10a-10d and 10i are very potent inhibitors of Eimeria tenella cGMP-dependent protein kinase (0.081-0.32 nM) and are very efficacious antiparasitic agents in vivo when administered to chickens at 12.5-25 ppm levels in the feed. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5978 / 5981
页数:4
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