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噻吩并二嗪2,2 -二氧化物无环核苷:合成与抗病毒活性。

Thienothiadiazine 2,2-dioxide acyclonucleosides: synthesis and antiviral activity.

作者信息

Martinez A, Esteban A, Castro A, Gil C, Conde S, Andrei G, Snoeck R, Balzarini J, De Clercq E

机构信息

Instituto de Quimica Medica (CSIC), Madrid, Spain.

出版信息

Antivir Chem Chemother. 2000 May;11(3):221-30. doi: 10.1177/095632020001100305.

DOI:10.1177/095632020001100305
PMID:10901293
Abstract

The synthesis of acyclonucleosides derived from thieno[3,2-c] and thieno[2,3-c][1,2,6]thiadiazine 2,2-dioxides was achieved following the silylation method. Lipase-mediated methodology was employed for deprotection of the acyclic moieties. The antiviral effects were determined against a broad spectrum of viruses, including cytomegalovirus (CMV) and varicella zoster virus (VZV). Only minor antiviral activity against VZV was observed for those acyclonucleosides carrying a benzyl group.

摘要

通过硅烷化方法实现了源自噻吩并[3,2 - c]和噻吩并[2,3 - c][1,2,6]噻二嗪2,2 - 二氧化物的无环核苷的合成。采用脂肪酶介导的方法对无环部分进行脱保护。针对包括巨细胞病毒(CMV)和水痘带状疱疹病毒(VZV)在内的多种病毒测定了抗病毒效果。对于那些带有苄基的无环核苷,仅观察到对VZV的轻微抗病毒活性。

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