SYNTHESIS AND BIOLOGICAL ACTIVITY OF NEW 6-BENZYLISOCYTOSINE DERIVATIVES: NON-NUCLEOSIDE HIV-1 REVERSE TRANSCRIPTASE INHIBITORS

V. T. Valuev-Elliston; A. V. Ivanov; B. S. Orlinson; E. N. Gerasimov; L. L. Brunilina; S. N. Kochetkov; I. A. Novakov; M. B. Navrotskii

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SYNTHESIS AND BIOLOGICAL ACTIVITY OF NEW 6-BENZYLISOCYTOSINE DERIVATIVES: NON-NUCLEOSIDE HIV-1 REVERSE TRANSCRIPTASE INHIBITORS

机译：新型6-苄基胞嘧啶衍生物的合成及生物活性：非核苷HIV-1逆转录酶抑制剂

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New 6-benzylisocytosine derivatives were synthesized by aminolysis of 6-benzyl-2-(methylsulfanyl)pyrimi-din-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.

机译：通过将6-苄基-2-（甲基硫烷基）嘧啶-din-4（3H）-与脂肪族芳香族和笼型结构的胺进行氨解反应，合成了新的6-苄基异胞嘧啶衍生物。一些合成的化合物似乎是有效的HIV-1逆转录酶抑制剂。其中，6-（2,6-二氟苄基）-5-甲基-2-[（（2-苯乙基）氨基]嘧啶-4（3H）-one表现出最明显的抑制特性，比参考文献有效九倍。抗艾滋病毒药物奈韦拉平。

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来源
《Pharmaceutical Chemistry Journal》 |2012年第7期|共5页
作者
V. T. Valuev-Elliston; A. V. Ivanov; B. S. Orlinson; E. N. Gerasimov; L. L. Brunilina; S. N. Kochetkov; I. A. Novakov; M. B. Navrotskii;
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正文语种 eng
中图分类药学;
关键词
6-benzylisocytosine derivatives; HIV-1 reverse transcriptase inhibitors;

机译：6-苄基异胞嘧啶衍生物;HIV-1逆转录酶抑制剂;

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1. SYNTHESIS AND BIOLOGICAL ACTIVITY OF NEW 6-BENZYLISOCYTOSINE DERIVATIVES: NON-NUCLEOSIDE HIV-1 REVERSE TRANSCRIPTASE INHIBITORS [J] . V. T. Valuev-Elliston, A. V. Ivanov, B. S. Orlinson, Pharmaceutical Chemistry Journal . 2012,第7期

机译：新型6-苄基胞嘧啶衍生物的合成及生物活性：非核苷HIV-1逆转录酶抑制剂
2. Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors [J] . Viira Birgit, Selyutina Anastasia, Garcia-Sosa Alfonso T., Bioorganic and medicinal chemistry . 2016,第11期

机译：设计，发现，建模，合成和生物学评估新型和小型，低毒性的s-三嗪衍生物作为HIV-1非核苷逆转录酶抑制剂
3. Synthesis and Biological Evaluation of 2-Thioxopyrimidin-4(1H)-one Derivatives as Potential Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors [J] . Bing Yan, Mohamed A. Al-Omar, Nagy M. Khalifa International Journal of Molecular Sciences . 2014,第11期

机译：作为潜在的非核苷HIV-1逆转录酶抑制剂的2-硫代嘧啶丁-4（1H）-一衍生物的合成和生物学评价
4. Diarylaniline Derivatives as a Distinct Class of HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors [C] . Bingjie Qin, Shibo Jiang, Kuo-Hsiung Lee, ICMSI;International conference of molecular simulations and applied informatics technologies . 2010

机译：二芳基苯胺衍生物作为HIV-1非核苷逆转录酶抑制剂的一类。
5. A. Studies towards the formation of asymmetric quaternary centres via radical allylation. B. Applications of chiral hydrazide organocatalysts to Diels-Alder, hydride reduction, and alpha-chlorination reactions. C. Studies directed towards the synthesis of potential HIV-1 reverse transcriptase inhibitors: 9-Alkylaryl TIBO derivatives. [D] . Aumand, Livia M. 2005

机译：A.关于通过自由基烯丙基化形成不对称四元中心的研究。 B.手性酰肼有机催化剂在Diels-Alder，氢化物还原和α-氯化反应中的应用。 C.针对潜在的HIV-1逆转录酶抑制剂的合成的研究：9-烷基芳基TIBO衍生物。
6. Synthesis and Biological Evaluation of 2-Thioxopyrimidin-4(1H)-one Derivatives as Potential Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors [O] . Nagy M. Khalifa, Mohamed A. Al-Omar 2014

机译：作为潜在的非核苷HIV-1逆转录酶抑制剂的2-硫代嘧啶丁-4（1H）-一衍生物的合成与生物学评价
7. Synthesis and Biological Evaluation of 2-Thioxopyrimidin-4(1H)-one Derivatives as Potential Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors [O] . Nagy M. Khalifa, Mohamed A. Al-Omar 2014

机译：2-噻吩并嘧啶-4（1H） - 酮衍生物作为潜在的非核苷类HIV-1逆转录酶抑制剂的合成和生物学评价

SYNTHESIS AND BIOLOGICAL ACTIVITY OF NEW 6-BENZYLISOCYTOSINE DERIVATIVES: NON-NUCLEOSIDE HIV-1 REVERSE TRANSCRIPTASE INHIBITORS

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