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5-烷基-2-[(芳基和烷氧基羰基甲基)硫代]-6-(1-萘甲基)嘧啶-4(3H)-酮作为S-DABO系列独特的HIV逆转录酶抑制剂。

5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.

作者信息

He Yanping, Chen Fener, Sun Guangfu, Wang Yueping, De Clercq Erik, Balzarini Jan, Pannecouque Christophe

机构信息

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

出版信息

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3173-6. doi: 10.1016/j.bmcl.2004.04.008.

Abstract

The introduction of a beta-carbonyl group to the C-2 side chain of S-DABO led to the finding of a series of novel potent anti-HIV agent. Some derivatives proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentrations. Furthermore, the novel S-DABOs differ from the classical NNRTIs in that some compounds are active against both HIV-1 and HIV-2. They might interfere with another target or at least act on RT in a different way as compared to typical NNRTIs.

摘要

在S-DABO的C-2侧链引入β-羰基基团,从而发现了一系列新型强效抗HIV药物。一些衍生物在纳摩尔浓度下对抑制HIV-1复制非常有效。此外,新型S-DABO与经典的非核苷类逆转录酶抑制剂不同,因为一些化合物对HIV-1和HIV-2均有活性。它们可能作用于另一个靶点,或者至少与典型的非核苷类逆转录酶抑制剂相比,以不同的方式作用于逆转录酶。

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