Novel N-3 substituted TSAO-T derivatives: Synthesis and anti-HIV-evaluation
Novel N-3 substituted TSAO-T derivatives: Synthesis and anti-HIV-evaluation
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DOI：
10.1080/15257770801943990
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发表时间：
2008-01-01
影响因子：
1.3
通讯作者：
San-Felix, Ana
中科院分区：
文献类型：
--
作者：
Bonache, Maria-Cruz;Quesada, Emesto;San-Felix, Ana
制备了具有N-3烷基化基团或光亲和标记的新型抗hiv -1衍生物TSAO-T，并对其抗hiv活性进行了评价。所有这些化合物都显示出明显的抗HIV-1活性并抑制HIV-1 RT；然而，我们无法检测到抑制剂和酶之间稳定的共价键。此外，还制备了具有醇官能团通过顺式或反式双键连接到N-3位的化合物。这些化合物有助于研究连接体的构象限制如何影响N-3取代基与HIV-1 RT酶之间的相互作用。
Novel derivatives of the anti-HIV-1 agent, TSAO-T, bearing at the N-3 position alkylating groups or photoaffinity labels were prepared and evaluated for their anti-HIV activity. All of these compounds demonstrated pronounced anti-HIV-1 activity and inhibited HIV-1 RT; however, we were unable to detect stable covalent linkages between inhibitor and enzyme. In addition, compounds with an alcohol functional group connected to the N-3 position through a cis or trans double bond have been prepared. These compounds have been useful to study how the conformational restriction of the linker affects in the interaction between the N-3 substituent and the HIV-1 RT enzyme.