Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

Wang YP; Chen FE; De-Clercq EBalzarini JPannecouque C

首页> 外文期刊>Bioorganic and medicinal chemistry >Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

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Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

机译：Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

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摘要

A novel series of 2-arylcarbonylmethylthio-6-arylmethylpyrimidin-4(3H)-ones have been synthesized and evaluated for in vitro anti-HIV activities in MT-4 cells. Most of these new compounds showed moderate to potent activities against wild-type HIV-1 with an EC(50) range from 8.97 microM to 0.010 microM. Among them, the 6-(3,5-dimethylbenzyl) analogue 5p was identified as the most promising compound (EC(50)=0.010 microM, SI>31,800) associated with moderate activity against the HIV-1 double mutant RT strain K103N+Y181C. The structure-activity relationships of these new congeners were further discussed.

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《Bioorganic and medicinal chemistry》 |2008年第7期|3887-3894|共8页
作者
Wang YP; Chen FE; De-Clercq EBalzarini JPannecouque C;
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作者单位

Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.;

ost.saga-med.ac.jp;

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正文语种英语
中图分类药学;生物化学;
关键词
Alkylation; Cell Line; HIV-1; Humans; Methylation; Molecular Structure; Nucleosides; 烷化作用; 细胞系; 甲基化; 分子结构; 核苷类; 嘧啶类; 逆转录酶抑制剂; 构效关系;

Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

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