Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.

Wai JS; Kim B; Fisher TE; Zhuang L; Embrey MW; Williams PD; Staas DD; Culberson C; Lyle TA; Vacca JP; Hazuda DJ; Felock PJ; Schleif WA; Gabryelski LJ; Jin L; Chen IW; Ellis JD; Mallai R; Young SD

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Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.

机译：二羟基吡啶并吡嗪-1,6-二酮HIV-1整合酶抑制剂。

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A series of potent novel dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 6 is active against replication of HIV with a CIC(95) of 0.31 microM and exhibits no shift in potency in the presence of 50% normal human serum. It displays a good pharmacokinetic profile when dosed in rats and no covalent binding with microsomal proteins in both in vitro and in vivo models.

机译：鉴定出一系列有效的新型二羟基吡啶并吡嗪-1,6-二酮HIV-1整合酶抑制剂。这些化合物抑制了HIV-1整合酶的链转移过程和细胞中的病毒复制。化合物6具有0.31 microM的CIC（95）具有抗HIV复制的活性，并且在50％正常人血清中，其效力没有变化。当在大鼠中给药时，它显示出良好的药代动力学特征，并且在体外和体内模型中均不与微粒体蛋白共价结合。

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《Bioorganic and Medicinal Chemistry Letters》 |2007年第20期|共5页
作者
Wai JS; Kim B; Fisher TE; Zhuang L; Embrey MW; Williams PD; Staas DD; Culberson C; Lyle TA; Vacca JP; Hazuda DJ; Felock PJ; Schleif WA; Gabryelski LJ; Jin L; Chen IW; Ellis JD; Mallai R; Young SD;
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正文语种 eng
中图分类药学;生物化学;
关键词
Integrase; HIV-1; inhibitors; replication; in vivo; 整合酶;

机译：Integrase;HIV-1;inhibitors;replication;in vivo;整合酶;

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专利

1. Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors. [J] . Wai JS, Kim B, Fisher TE, Bioorganic and Medicinal Chemistry Letters . 2007,第20期

机译：二羟基吡啶并吡嗪-1,6-二酮HIV-1整合酶抑制剂。
2. Specific HIV-1 integrase polymorphisms change their prevalence in untreated versus antiretroviral-treated HIV-1-infected patients, all naive to integrase inhibitors. [J] . Ceccherini Silberstein F, Malet I, Fabeni L, The Journal of Antimicrobial Chemotherapy . 2010,第11期

机译：特定的HIV-1整合酶多态性改变了未经治疗与抗逆转录病毒治疗的HIV-1感染患者的患病率，所有患者均未使用整合酶抑制剂。
3. The use of a new in vitro reaction substrate reproducing both U3 and U5 regions of the HIV-1 3'-ends increases the correlation between the in vitro and in vivo effects of the HIV-1 integrase inhibitors. [J] . Tramontano E, Onidi L, Esposito F, Biochemical Pharmacology . 2004,第9期

机译：使用可复制HIV-1 3'-末端的U3和U5区域的新的体外反应底物，可提高HIV-1整合酶抑制剂的体外和体内作用之间的相关性。
4. Comparative study of Differential Evolutionary-Binary Particle Swarm Optimization (DE-BPSO) algorithm as a feature selection technique with different linear regression models for analysis of HIV-1 Integrase Inhibition features of Aryl β-Diketo Acids [C] . Falguni Thakor, Ahmad Reza Hadaegh, Xiaoyu Zhang International Conference on Bioinformatics and Computational Biology . 2017

机译：差分进化二元粒子群优化（DE-BPSO）算法作为具有不同线性回归模型的特征选择技术的对比研究分析芳基β-Diketo酸的HIV-1整合酶抑制特征
5. Design and synthesis of HIV-1 integrase inhibitors. [D] . Scarry, Sarah Chajkowski. 2012

机译：HIV-1整合酶抑制剂的设计和合成。
6. HIV-1 Group O Integrase Displays Lower Enzymatic Efficiency and Higher Susceptibility to Raltegravir than HIV-1 Group M Subtype B Integrase [O] . Agnès Depatureaux, Peter K. Quashie, Thibault Mesplède, 2014

机译：与HIV-1组M亚型B整合酶相比HIV-1组O整合酶显示更低的酶效率和对Raltegravir的敏感性更高
7. Molecular modeling study on the allosteric inhibition mechanism of HIV-1 integrase by LEDGF/p75 binding site inhibitors. [O] . Weiwei Xue, Huanxiang Liu, Xiaojun Yao 2014

机译：用LEDGF / p75结合位点抑制剂研究HIV-1整合酶的变构抑制机制的分子模拟研究。

Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.

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