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对疱疹病毒具有强效活性的吡唑并吡啶:C5取代基对抗病毒活性的影响。

Pyrazolopyridines with potent activity against herpesviruses: effects of C5 substituents on antiviral activity.

作者信息

Gudmundsson Kristjan S, Johns Brian A, Allen Scott H

机构信息

Department of Medicinal Chemistry, Infectious Diseases Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.

出版信息

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1157-61. doi: 10.1016/j.bmcl.2007.11.120. Epub 2007 Dec 4.

Abstract

Synthesis of a series of 5-substituted as well as 5,7-disubstituted 3-[2-(cyclopentylamino)-4-pyrimidinyl]-2-phenylpyrazolo[1,5-a]pyridin-7-amines with potent activity against herpes simplex viruses is described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity are highlighted. Several compounds with in vitro antiviral activity similar to or better than acyclovir are described.

摘要

描述了一系列具有抗单纯疱疹病毒活性的5-取代以及5,7-二取代的3-[2-(环戊基氨基)-4-嘧啶基]-2-苯基吡唑并[1,5-a]吡啶-7-胺的合成。概述了允许改变取代模式的合成方法,并突出了抗病毒活性的相应变化。还描述了几种体外抗病毒活性与阿昔洛韦相似或优于阿昔洛韦的化合物。

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