Synthesis and biological activity of anticoccidial agents:: 5,6-diarylimidazo[2,1-b][1,3]thiazoles

被引:43
作者
Scribner, Andrew [1 ]
Meitz, Susan [1 ]
Fisher, Michael [2 ]
Wyvratt, Matthew [2 ]
Leavitt, Penny [3 ]
Liberator, Paul [3 ]
Gurnett, Anne [3 ]
Brown, Chris [3 ]
Mathew, John [3 ]
Thompson, Donald [3 ]
Schmatz, Dennis [3 ]
Biftu, Tesfaye [2 ]
机构
[1] SCYNEXIS Inc, Discovery Chem, Res Triangle Pk, NC 27709 USA
[2] Merck & Co Inc, Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[3] Merck & Co Inc, Merck Res Labs, Dept Human & Anim Infect Dis Res, Rahway, NJ 07065 USA
关键词
anticoccidial; antiprotozoan; protein kinase G; PKG inhibitor; imidazothiazole;
D O I
10.1016/j.bmcl.2008.08.063
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel 5,6-diarylimidazo[2,1-b][1,3]thiazoles bearing an amine substituent at the imidazothiazole 2-position have been synthesized and evaluated as anticoccidial agents in both in vitro and in vivo assays. Both subnanomolar in vitro activity and broad spectrum in vivo potency were detected for several compounds, particularly compound 10. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5263 / 5267
页数:5
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