Synthesis and Anti-HIV Activity of Some [Nucleoside Reverse Transcriptase Inhibitor]-C5′-Linker-[Integrase Inhibitor] Heterodimers as Inhibitors of HIV Replication
Synthesis and Anti-HIV Activity of Some [Nucleoside Reverse Transcriptase Inhibitor]-C5′-Linker-[Integrase Inhibitor] Heterodimers as Inhibitors of HIV Replication
复制标题
一些[核苷逆转录酶抑制剂]-C5′-Linker-[整合酶抑制剂]异二聚体作为HIV复制抑制剂的合成和抗HIV活性
DOI：
10.1080/14756360412331280554
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发表时间：
2004
影响因子：
5.6
通讯作者：
A. Aubertin
中科院分区：
文献类型：
--
作者：
E. Sugeac;C. Fossey;D. Ladurée;S. Schmidt;G. Laumond;A. Aubertin
根据其预期的抑制HIV复制的能力进行选择，设计并合成了一系列含有核苷逆转录酶抑制剂（NRTI）和整合酶抑制剂（INI）的异二聚体，所述异二聚体通过接头结合。对于NRTI，选择d4 U、d2 U和d4 T。对于INI，选择4-[1-（4-氟苄基）-1H-吡咯-2-基]-2，4-二氧代丁酸（6）和4-（3，5-二苄氧基苯基）-2，4-二氧代丁酸（9）（属于β-二酮酸类）。使用氨基酸（甘氨酸或β-丙氨酸）作为可切割接头进行两种不同抑制剂（NRTI和INI）的缀合。
Selected for their expected ability to inhibit HIV replication, a series of eight heterodimers containing a Nucleoside Reverse Transcriptase Inhibitor (NRTI) and an Integrase Inhibitor (INI), bound by a linker, were designed and synthesized. For the NRTIs, d4U, d2U and d4T were chosen. For the INIs, 4-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxobutyric acid (6) and 4-(3,5-dibenzyloxyphenyl)-2,4-dioxobutyric acid (9) (belonging to the β-diketo acids class) were chosen. The conjugation of the two different inhibitors (NRTI and INI) was performed using an amino acid (glycine or β-alanine) as a cleavable linker.
影响因子：
7.3
作者：
MANSURI, MM;STARRETT, JE;MARTIN, JC
通讯作者：
MARTIN, JC