新型水溶性双功能化[60]富勒烯衍生物的合成及其抗HIV特性
Synthesis and anti-HIV properties of new water-soluble bis-functionalized[60]fullerene derivatives.
作者信息
Bosi Susanna, Da Ros Tatiana, Spalluto Giampiero, Balzarini Jan, Prato Maurizio
机构信息
Dipartimento di Scienze Farmaceutiche, Università di Trieste, Piazzale Europa 1, I-34127 Trieste, Italy.
出版信息
Bioorg Med Chem Lett. 2003 Dec 15;13(24):4437-40. doi: 10.1016/j.bmcl.2003.09.016.
A new series of bis-functionalized fullerene C(60) derivatives bearing two or more solubilizing chains have been evaluated for their activity against HIV-1 and HIV-2 strains. Some of the compounds show activity against HIV-1 type in the low micromolar range. The effect of the positions of the addends on the C(60) nucleus has been investigated, indicating that only trans-2 isomers possess promising activity. The presence of a quaternary pyrrolidinium nitrogen is essential to increase solubility.
已对一系列带有两个或更多增溶链的双官能化富勒烯C(60)衍生物针对HIV-1和HIV-2毒株的活性进行了评估。一些化合物在低微摩尔范围内显示出对HIV-1型的活性。已研究了加成物在C(60)核上的位置的影响，表明只有反式-2异构体具有有前景的活性。季铵化吡咯烷氮的存在对于增加溶解度至关重要。
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