Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro

被引：2
|
作者：
Yang, Rui-Ge [1 ]
Yang, Liu-Meng [2 ,3 ]
Ke, Ya-Zhen [1 ]
Huang, Ning [2 ,3 ,4 ]
Zhang, Rui [1 ]
Zheng, Yong-Tang [2 ,3 ]
Xu, Hui [1 ]
机构：
[1] NW A&F Univ, Lab Pharmaceut Design & Synth, Coll Sci, Yangling 712100, Peoples R China
[2] Chinese Acad Sci, Kunming Inst Zool, Kunming 650223, Yunnan, Peoples R China
[3] Chinese Acad Sci, Key Lab Anim Models & Human Dis Mech, Kunming 650223, Yunnan, Peoples R China
[4] Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2012年 / 9卷 / 04期
基金：
中国国家自然科学基金;
关键词：
2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones; Acquired immunodeficiency syndrome; Human immunodeficiency virus-1; AIDS; REVERSE-TRANSCRIPTASE; DERIVATIVES; DISCOVERY; AGENTS; THIAZOLIDIN-4-ONES; 4-THIAZOLIDINONES; ANALOGS;
D O I：
10.2174/157018012799859936
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 > 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.
引用
收藏
页码：415 / 420
页数：6
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