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

页码：415 / 420

页数：6

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