Structure-activity relationship study on anti-HIV 6-desfluoroquinolones

Tabarrini O; Massari S; Daelemans D; Stevens M; Manfroni G; Sabatini S; Balzarini J; Cecchetti V; Pannecouque C; Fravolini A

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Structure-activity relationship study on anti-HIV 6-desfluoroquinolones

机译：抗HIV 6-去氟喹诺酮类药物的构效关系研究

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the basis Of Our recent findings that 6-aminoquinolones inhibit the HIV Tat-mediated transactivation, have designed a broad series of derivatives identifying novel potent agents such as the 6-desfluoroquinolones 24 (HM12) and 27 (HM13), which showed pronounced anti-HIV activity in acutely, chronically, latently HIV-1 infected cell Cultures. We demonstrate here that highly potent molecules can be obtained optimizing the substituent in the various positions of the quinolone nucleus.

机译：根据我们最近的发现，即6-氨基喹诺酮类药物抑制HIV Tat介导的反式激活，我们设计了一系列衍生物，这些衍生物可鉴定出新型有效药物，例如6-去氟喹诺酮类药物24（HM12）和27（HM13），它们显示出明显的抗在急性，慢性，潜在HIV-1感染的细胞培养物中的HIV活性。我们在这里证明，可以获得高效分子，优化喹诺酮核的各个位置上的取代基。

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《Journal of Medicinal Chemistry》 |2008年第17期|共5页
作者
Tabarrini O; Massari S; Daelemans D; Stevens M; Manfroni G; Sabatini S; Balzarini J; Cecchetti V; Pannecouque C; Fravolini A;
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正文语种 eng
中图分类药学;
关键词
INTEGRASE INHIBITORS; GENE-EXPRESSION; DERIVATIVES; 6-AMINOQUINOLONES; REPLICATION;

机译：整合酶抑制剂;基因表达;衍生物;6-氨基喹诺酮;复制;

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1. Structure-activity relationship study on anti-HIV 6-desfluoroquinolones [J] . Tabarrini O, Massari S, Daelemans D, Journal of Medicinal Chemistry . 2008,第17期

机译：抗HIV 6-去氟喹诺酮类药物的构效关系研究
2. Design, Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies of 2,3-Diaryl-1,3-thiazolidin-4-ones as Potent Anti-HIV Agents [J] . Maria L. Barreca, Jan Balzarini, Alba Chimirri, Journal of Medicinal Chemistry . 2002,第24期

机译：2,3-二芳基-1,3-噻唑烷酮-4-酮作为有效的抗HIV药物的设计，合成，结构活性关系和分子模型研究
3. Quantitative structure-activity relationship studies of diarylpyrimidine derivatives as anti-HIV drugs using new three-dimensional structure descriptors [J] . Jianbo Tong, Li Zhong, Xiang Zhao, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2014,第4期

机译：使用新的三维结构描述符对二芳基嘧啶衍生物作为抗HIV药物进行定量构效关系研究
4. Quantitative structure-activity relationship studies on 1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents [C] . Ke-xian Chen, Hai-ying Xie, Zu-guang Li, 第四届国际分子模拟与信息技术应用学术会议（The 4th International Conference of Molecular Simulations and Applied Informatics Technologies）论文集 . 2008

机译：1-芳基-四氢异喹啉类似物作为抗HIV活性剂的定量构效关系研究
5. Synthesis and Structure-Activity Relationship Studies of Cyclotriaza Compounds as CD4 Down-Modulators and Anti-HIV Agents. [D] . Chawla, Reena. 2014

机译：Cyclotriaza化合物作为CD4下调剂和抗HIV剂的合成及构效关系研究。
6. Anti-AIDS agents 79. Design synthesis molecular modeling and structure-activity relationships of novel dicamphanoyl-2′2′-dimethyldihydropyranochromone (DCP) analogs as potent anti-HIV agents [O] . Ting Zhou, Qian Shi, Chin-Ho Chen, -1

机译：抗助剂剂79.新型二曼酰基-22-DimethylDihydropyranochromone（DCP）类似物的设计合成分子建模和结构 - 活性关系作为有效的抗HIV药剂
7. Structure-activity relationship study of pyrimido1,2-c1,3benzothiazin-6-imine derivatives for potent anti-HIV agents. [O] . Mizuhara Tsukasa, Oishi Shinya, Ohno Hiroaki, 2012

机译：嘧啶1,2-c 1,3苯并噻嗪-6-亚胺衍生物作为抗HIV有效剂的构效关系研究。

Structure-activity relationship study on anti-HIV 6-desfluoroquinolones

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