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三环阿昔洛韦的6-杂芳基衍生物和9-{[顺式-1',2'-双(羟甲基)环丙-1'-基]甲基}鸟嘌呤类似物的合成及抗水痘带状疱疹病毒活性

Synthesis and anti-VZV activity of 6-heteroaryl derivatives of tricyclic acyclovir and 9-{[cis-1',2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl}guanine analogues.

作者信息

Ostrowski Tomasz, Golankiewicz Bozenna, De Clercq Erik, Andrei Graciela, Snoeck Robert

机构信息

Institute of Bioorganic Chemistry, Polish Academy of Sciences, Poznan, Poland.

出版信息

Eur J Med Chem. 2009 Aug;44(8):3313-7. doi: 10.1016/j.ejmech.2009.03.005. Epub 2009 Mar 21.

DOI:10.1016/j.ejmech.2009.03.005
PMID:19339082
Abstract

A series of tricyclic analogues of acyclovir and 9-{[cis-1',2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl}guanine substituted in the 6 position with thien-2-yl, 5-bromothien-2-yl or furan-2-yl group were synthesized. The new compounds 5a-f were evaluated for their activity in vitro against varicella-zoster virus (VZV) and cytomegalovirus (CMV). The marked anti-VZV activities of 5a-f remained comparable to those of their previously described 6-phenyl-substituted counterparts.

摘要

合成了一系列阿昔洛韦的三环类似物以及6位被噻吩-2-基、5-溴噻吩-2-基或呋喃-2-基取代的9-{[顺式-1',2'-双(羟甲基)环丙-1'-基]甲基}鸟嘌呤。对新化合物5a - f进行了体外抗水痘带状疱疹病毒(VZV)和巨细胞病毒(CMV)活性评估。5a - f显著的抗VZV活性与之前描述的6-苯基取代类似物相当。

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