Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.

Zhao XZ; Maddali K; Metifiot M; Smith SJ; Vu BC; Marchand C; Hughes SH; Pommier Y; Burke TR Jr

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Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.

机译：开发含有HIV-1整合酶抑制剂的三环羟基-1H-吡咯并吡啶-三酮。

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New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the introduction of a nitrogen into the aryl ring and the addition of a fused third ring to our previously described inhibitors. The resulting analogues showed low micromolar inhibitory potency in in vitro HIV-1 integrase assays, with good selectivity for strand transfer relative to 3'-processing.

机译：制备了新的三环HIV-1整合酶（IN）抑制剂，该抑制剂将双环嘧啶酮的结构特征与最近公开的4,5-二羟基-1H-异吲哚-1,3（2H）-二酮结合在一起。这种结合导致将氮引入芳基环并向我们先前描述的抑制剂中加入稠合的第三环。所得类似物在体外HIV-1整合酶测定中显示出低的微摩尔抑制力，相对于3'加工，对链转移具有良好的选择性。

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《Bioorganic and Medicinal Chemistry Letters》 |2011年第10期|共5页
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Zhao XZ; Maddali K; Metifiot M; Smith SJ; Vu BC; Marchand C; Hughes SH; Pommier Y; Burke TR Jr;
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1. Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors. [J] . Zhao XZ, Maddali K, Metifiot M, Bioorganic and Medicinal Chemistry Letters . 2011,第10期

机译：开发含有HIV-1整合酶抑制剂的三环羟基-1H-吡咯并吡啶-三酮。
2. Effect of substitution on novel tricyclic HIV-1 integrase inhibitors. [J] . Fardis M, Jin H, Jabri S, Bioorganic and Medicinal Chemistry Letters . 2006,第15期

机译：取代对新型三环HIV-1整合酶抑制剂的影响。
3. Subtype diversity associated with the development of HIV-1 resistance to integrase inhibitors. [J] . Brenner BG, Lowe M, Moisi D, Journal of Medical Virology . 2011,第5期

机译：亚型多样性与HIV-1对整合酶抑制剂的抗性发展有关。
4. Improving the Feature Selection for the Development of Linear Model for Discovery of HIV-1 Integrase Inhibitors [C] . Matineh Kashani Moghaddam, Richard Adrian Galvan, Ahmad Reza Hadaegh International Conference on Advances in Big Data Analytics . 2015

机译：改进HIV-1整合酶抑制剂发现线性模型的特征选择
5. An organic chemistry approach toward the synthesis of valuable biological compounds: Synthetic progress toward the Palmerolide A subunits, expeditious enyne coupling via alkynes, and development of the next generation of HIV-1 integrase inhibitors. [D] . Hadi, Victor. 2010

机译：合成有价值的生物化合物的有机化学方法：合成Palmerolide A亚基的合成进展，通过炔烃快速进行的炔烃偶联以及下一代HIV-1整合酶抑制剂的开发。
6. Development of Tricyclic Hydroxy-1H-pyrrolopyridine-trione Containing HIV-1 Integrase Inhibitors [O] . Xue Zhi Zhao, Kasthuraiah Maddali, Mathieu Metifiot, -1

机译：含有HIV-1整合酶抑制剂三环羟基-1H-吡咯烷吡啶-Trione的研制
7. Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors [O] . Xue Zhi Zhao, Kasthuraiah Maddali, Mathieu Metifiot, 2011

机译：含有HIV-1整合酶抑制剂三环羟基-1H-吡咯烷吡啶-Trione的研制

Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.

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