Inhibition of human immunodeficiency virus type (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives.

Witvrouw M; Pannecouque C; De Clercq-E; Fernandez Alvarez-E; Marco JL

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Inhibition of human immunodeficiency virus type (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives.

机译：某些功能不同的螺环丙基衍生物对人类免疫缺陷病毒类型（HIV-1）复制的抑制作用。

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摘要

Inhibition of HIV-1 replication by differently substituted spirocyclopropyl compounds has been evaluated. Compound 21 showed a moderate activity (EC50 ranging from 2.3 to 5.8 micrograms/ml) against different HIV-1 strains (IIIB, RF, NDK, and an AZT-resistant strain) in different cell lines (MT-4 and C-8166 cells), while it was cytotoxic at 77.7 micrograms/ml, resulting in a selectivity index of 34. This compound was inactive against HIV-2 (ROD) and SIV (MAC251). From "time-of-addition" experiments compound 21, like AZT, appeared to inhibit HIV-1 at the reverse transcriptase step.

机译：已经评估了不同取代的螺环丙基化合物对HIV-1复制的抑制作用。化合物21在不同的细胞系（MT-4和C-8166细胞）中对不同的HIV-1株（IIIB，RF，NDK和AZT耐药株）表现出中等活性（EC50在2.3至5.8微克/毫升之间）），但在77.7微克/毫升时具有细胞毒性，因此选择性指数为34。该化合物对HIV-2（ROD）和SIV（MAC251）无活性。从“添加时间”实验中，化合物21（如AZT）似乎在逆转录酶步骤中抑制HIV-1。

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来源
《Archiv der Pharmazie》 |1999年第5期|共4页
作者
Witvrouw M; Pannecouque C; De Clercq-E; Fernandez Alvarez-E; Marco JL;
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正文语种 eng
中图分类药学;
关键词
Anti-HIV Agents; Cyclopropanes; HIV-1; Spiro Compounds; Virus Replication; 抗HIV药; 环丙烷类; HIV-1; 螺环化合物; 病毒复制;

机译：Anti-HIV Agents;Cyclopropanes;HIV-1;Spiro Compounds;Virus Replication;抗HIV药;环丙烷类;HIV-1;螺环化合物;病毒复制;

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1. Inhibition of human immunodeficiency virus type (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives. [J] . Witvrouw M, Pannecouque C, De Clercq-E, Archiv der Pharmazie . 1999,第5期

机译：某些功能不同的螺环丙基衍生物对人类免疫缺陷病毒类型（HIV-1）复制的抑制作用。
2. Inhibition of acute-, latent-, and chronic-phase human immunodeficiency virus type 1 (HIV-1) replication by a bistriazoloacridone analog that selectively inhibits HIV-1 transcription. [J] . Turpin JA, Buckheit RW Jr, Derse D, Antimicrobial agents and chemotherapy. . 1998,第3期

机译：通过选择性抑制HIV-1转录的双三唑并rid啶酮类似物抑制急性，潜伏和慢性阶段的1型人类免疫缺陷病毒（HIV-1）复制。
3. Inhibition of human immunodeficiency virus type-1 (HIV-1) replication at a reverse transcription step by human cell factor(s) [J] . Tempaku A Biological & pharmaceutical bulletin . 2005,第5期

机译：人类细胞因子在逆转录步骤抑制人类1型免疫缺陷病毒（HIV-1）复制
4. Simultaneous extraction of human immunodeficiency virus type 1 (HIV-1) and hepatitis C virus (HCV) RNA with the M1000 apparatus does not impair the measurement of the viral load of both viruses when tested by using the LCx PCR system [C] . T. Bourlet, S. Thamm, S. Pillet, European Congress of Virology . 2004

机译：通过使用LCX PCR系统测试，同时提取人免疫缺陷病毒类型1（HIV-1）和丙型肝炎病毒（HCV）RNA，不会损害两种病毒的病毒载量的测量
5. Isolation of two highly potent and non-toxic inhibitors of human immunodeficiency virus type 1 (HIV-1) integrase and viral replication. [D] . Abd-Elazem, Ibrahim Shawky. 2002

机译：分离两种1型人类免疫缺陷病毒（HIV-1）的高效和无毒抑制剂整合酶和病毒复制。
6. Inhibition of human immunodeficiency virus (HIV-1) replication by synthetic oligo-RNA derivatives. [O] . S Shibahara, S Mukai, H Morisawa, 1989

机译：合成的寡RNA衍生物抑制人免疫缺陷病毒（HIV-1）复制。
7. Inhibition of human immunodeficiency virus (HIV-1) replication by synthetic oligo-RNA derivatives. [O] . Shibahara, S, Mukai, S, Morisawa, H, 1989

机译：合成的寡RNA衍生物抑制人免疫缺陷病毒（HIV-1）复制。

Inhibition of human immunodeficiency virus type (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives.

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