α-噻吩氧基-羟乙酰胺衍生物的合成及其抗HIV活性
Synthesis and anti-HIV activity of alpha-thiophenoxy-hydroxyethylamide derivatives.
作者信息
Medou M, Priem G, Rocheblave L, Pepe G, Meyer M, Chermann J C, Kraus J L
机构信息
Laboratoire de Chimie Biomoléculaire, Faculté des Sciences de Luminy, Case 901, 163 avenue de Luminy, 13288 cedex 9, Marseille, France.
出版信息
Eur J Med Chem. 1999 Jul-Aug;34(7-8):625-38. doi: 10.1016/s0223-5234(00)80031-8.
A series of new anti-HIV derivatives containing a novel alpha-thiophenoxyhydroxyethylamide core have been synthesized, using S-phenylbenzenethiosulfonate as the thiosulfenylating reagent. Some of the new synthesized compounds (1a, 1c, 1g, 1i, 1j and 1l) inhibited HIV replication in cell culture assays (syncytia formation) with effective concentrations (EC(50)) ranging from 0.1-1 microM. Incorporation of thiophenoxy substitution within various pseudomimetic peptide backbones provided a series of highly potent HIV inhibitors.
使用苯硫代磺酸苯酯作为硫代亚磺酰化试剂，合成了一系列含有新型α-噻吩氧基羟乙酰胺核心的新型抗HIV衍生物。一些新合成的化合物（1a、1c、1g、1i、1j和1l）在细胞培养试验（多核体形成）中抑制HIV复制，有效浓度（EC(50)）范围为0.1 - 1微摩尔。在各种拟肽主链中引入噻吩氧基取代基，得到了一系列高效的HIV抑制剂。
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