Anti-HIV-1 activity of poly(mandelic acid) derivatives.

Anti-HIV-1 activity of poly(mandelic acid) derivatives.
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DOI:
10.1021/bm070221y
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发表时间:
2007-10
期刊:
影响因子:
6.2
通讯作者:
Marty Ward;Bing Yu;V. Wyatt;Jelani Griffith;Tara L. Craft;A. Neurath;N. Strick;Yun-yao Li;D. Wertz;J. Pojman;A. Lowe
Marty Ward;Bing Yu;V. Wyatt;Jelani Griffith;Tara L. Craft;A. Neurath;N. Strick;Yun-yao Li;D. Wertz;J. Pojman;A. Lowe
中科院分区:
化学2区
文献类型:
--
作者:
Marty Ward;Bing Yu;V. Wyatt;Jelani Griffith;Tara L. Craft;A. Neurath;N. Strick;Yun-yao Li;D. Wertz;J. Pojman;A. Lowe

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在强酸性、弱酸性和非酸性条件下合成了同手性和异手性聚扁桃酸(PMDA)。评价这些聚合物的水溶性部分对人免疫缺陷病毒(HIV-1)的抑制活性。聚合物通过逐步生长机制制备,得到线性聚酯。聚合物的特征在于通过CHS元素微量分析,X射线荧光(XRF),和FT-IR光谱。三种方法制备的聚合物具有不同的结构。元素微量分析和X射线荧光光谱表明,S的存在下,在这些聚合物中制备的治疗与浓硫酸,这是唯一的表现出抑制和杀病毒活性对HIV-1,介导的结合到细胞的辅助受体结合位点上的病毒包膜糖蛋白gp 120。此外,FT-IR光谱表明在H2SO 4制备的PMDA中完全不存在C=O官能团。
Homo- and heterochiral poly(mandelic acid)s (PMDAs) were synthesized under strongly acidic, mildly acidic, and nonacidic conditions. The water-soluble fractions of these polymers were evaluated with respect to their inhibitory activity against the human immunodeficiency virus (HIV-1). Polymers were prepared via a step-growth mechanism, yielding linear polyesters. The polymers were characterized by CHS elemental microanalysis, X-ray fluorescence (XRF), and FT-IR spectroscopy. Polymers prepared by the three methods have different structures. Both elemental microanalysis and XRF indicated the presence of S in those polymers prepared by treatment with concentrated H2SO4, which were the only ones exhibiting inhibitory and virucidal activity against HIV-1, mediated by their binding to cellular co-receptor binding sites on the virus envelope glycoprotein gp120. Additionally, FT-IR spectroscopy indicated the complete absence of C=O functionality in the H2SO4-prepared PMDA.