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抗球虫剂:2,3-二芳基吲哚的合成与生物活性

Synthesis and biological activity of anticoccidial agents: 2,3-diarylindoles.

作者信息

Scribner Andrew, Moore Joseph A, Ouvry Gilles, Fisher Michael, Wyvratt Matthew, Leavitt Penny, Liberator Paul, Gurnett Anne, Brown Chris, Mathew John, Thompson Donald, Schmatz Dennis, Biftu Tesfaye

机构信息

SCYNEXIS, Inc., Discovery Chemistry, PO Box 12878, Research Triangle Park, NC 27709-2878, USA.

出版信息

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1517-21. doi: 10.1016/j.bmcl.2009.01.001. Epub 2009 Jan 9.

Abstract

Novel 2,3-diarylindoles bearing an amine substituent at the indole 5- and 6-positions 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 27.

摘要

已合成了在吲哚5-和6-位带有胺取代基的新型2,3-二芳基吲哚,并在体外和体内试验中作为抗球虫剂进行了评估。几种化合物,特别是化合物27,检测到了亚纳摩尔级的体外活性和广谱的体内效力。

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