Synthesis and biological activity of new 6-benzylisocytosine derivatives: non-nucleoside HIV-1 reverse transcriptase inhibitors

被引：5
作者：
Valuev-Elliston, V. T. [1 ]
Ivanov, A. V. [1 ]
Orlinson, B. S. [2 ]
Gerasimov, E. N. [2 ]
Brunilina, L. L. [2 ]
Kochetkov, S. N. [1 ]
Novakov, I. A. [2 ]
Navrotskii, M. B. [2 ]
机构：
[1] Russian Acad Sci, VA Engelhardt Mol Biol Inst, Moscow, Russia
[2] Volgograd State Tech Univ, Volgograd, Russia
来源：
PHARMACEUTICAL CHEMISTRY JOURNAL | 2012年 / 46卷 / 07期
关键词：
6-benzylisocytosine derivatives; HIV-1 reverse transcriptase inhibitors; ANTI-HIV-1; ACTIVITY; POTENT; AGENTS; FAMILY;
D O I：
10.1007/s11094-012-0808-y
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
New 6-benzylisocytosine derivatives were synthesized by aminolysis of 6-benzyl-2-(methylsulfanyl)pyrimidin-4(3H)-ones with aliphatic aromatic and cage-structured amines. Some of the synthesized compounds appeared to be effective HIV-1 reverse transcriptase inhibitors. Among these, 6-(2,6-difluorobenzyl)-5-methyl-2-[(2-phenylethyl)amino]pyrimidin-4(3H)-one showed the most pronounced inhibitory properties, being nine times more effective than the reference anti-HIV drug nevirapine.
引用
收藏
页码：397 / 401
页数：5
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