Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro
Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro
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作为 HIV-1 抑制剂的新型 2-(N-芳基磺酰基吲哚-3-基)-3-芳基-1,3-噻唑烷-4-酮的体外合成
DOI：
10.2174/157018012799859936
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发表时间：
2012-05
影响因子：
1
通讯作者：
Xu, Hui
中科院分区：
文献类型：
--
作者：
Yang, Rui-Ge;Yang, Liu-Meng;Ke, Ya-Zhen;Huang, Ning;Zhang, Rui;Zheng, Yong-Tang;Xu, Hui
合成了21个2-(N-arylsulfonylindol-3-yl)-3-aryl-1，3-thiazolidin-4-ones(4a-u)，并对其进行了体外评价。其中，化合物4N和4P具有较强的抗HIV-1活性，其EC50值分别为3.48和8.61mU g/mL，TI值分别为34.08和23.22。结果表明，对于一系列2-(N-arylsulfonyl-6-methylindol-3-yl)-3-aryl-1，3-thiazolidin-4-one衍生物，引入R-2作为4-氯，引入R-3作为H或3-Cl可以得到更有前途和更有效的化合物。
Twenty-one 2-(N-arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones (4a-u) were synthesized and evaluated as HIV-1 inhibitors in vitro. Among all compounds, compounds 4n and 4p displayed the potent anti-HIV-1 activities with EC50 values of 3.48 and 8.61 mu g/mL, and TI values of 34.08 and g 23.22, respectively. It demonstrated that, to a series of 2-(N-arylsulfonyl-6-methylindol-3-yl)-3-aryl-1,3-thiazolidin-4-one derivatives, introduction of R-2 as 4-Cl and R-3 as H or 3-Cl could afford the more promising and potent compounds.