Identification of antibacterial and antiviral activities of novel fused 1,2,4-triazine esters

被引：58

作者：

Sztanke, Krzysztof

Pasternak, Kazimierz

Rajtar, Barbara

Sztanke, Malgorzata

Majek, Magdalena

Polz-Dacewicz, Malgorzata

机构：

[1] Prof Feliks Skubiszewski Med Univ, Dept Med Chem, PL-20081 Lublin, Poland

[2] Prof Feliks Skubiszewski Med Univ, Dept Virol, PL-20093 Lublin, Poland

[3] Prof Feliks Skubiszewski Med Univ, Dept Virol, PL-20093 Lublin, Poland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 16期

关键词：

fused 1,2,4-triazine esters; antibacterial activity; cytotoxicity; GMK cells; HEK-293; cells; antiviral activity; human adenovirus type-5; human enterovirus echo-9; in vitro study;

D O I：

10.1016/j.bmc.2007.05.048

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The in vitro biological activities of novel derivatives of methyl and ethyl 2-(4-oxo-8-aryl-2H-3,4,6,7-tetrahydroimidazo[2,1-c][1,2,4]triazin-3-yl)acetates (3a, 3d-j) have been evaluated and are reported. The final heterobicycles (3a-j) were obtained from monocyclic 1-aryl-2-hydrazonoimidazolidines (2a-f) by addition and cyclization reaction with fumaric acid esters. In particular, compounds 3d and 3e were found to exhibit comparable antibacterial potencies in vitro as that of ampicillin. Heterobicycles of the 3e, 3g and 3j type were screened for their antiviral activities against the selected viruses' DNA (human adenovirus type 5-Ad-5) and RNA (human enterovirus-Echo-9). Simultaneously, their cytotoxicities towards HEK-293 and GMK cells were established. In particular, heterobicycle 3j, completely non-toxic for GM K cells, was found to exhibit virucidal properties against Echo-9 virus justifying its further investigation as the potential antiviral agent. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5480 / 5486

页数：7

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