Microwave-Assisted Combinatorial Synthesis of 2-Alkyl-2-(N-Arylsulfonylindol-3-yl)-3-N-Acyl-5-Aryl-1,3,4-Oxadiazolines as Anti-HIV-1 Agents

被引：1

作者：

Che, Zhi-Ping ^{[1
]}

Huang, Ning ^{[2
,3
]}

Yu, Xiang ^{[1
]}

Yang, Liu-Meng ^{[2
,3
]}

Ran, Jun-Qiang ^{[1
]}

Zhi, Xiaoyan ^{[1
]}

Xu, Hui ^{[1
]}

Zheng, Yong-Tang ^{[2
,3
]}

机构：

[1] Northwest A&F Univ, Lab Pharmaceut Design & Synth, Coll Sci, Yangling 712100, Peoples R China

[2] Chinese Acad Sci, Key Lab Anim Models & Human Dis Mechanisms, Kunming 650223, Peoples R China

[3] Chinese Acad Sci, Kunming Inst Zool, Kunming 650223, Yunnan Province, Peoples R China

来源：

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING | 2013年 / 16卷 / 05期

基金：

中国国家自然科学基金;

关键词：

1,3,4-Oxadiazoline; microwave heating; human immunodeficiency virus-1; inhibitor; SOLVENT-FREE; INDOLES; ANALOGS;

D O I：

暂无

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

A library of new 2-alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines was efficiently synthesized from hydrazones and anhydrides under microwave irradiation and solvent-free conditions. Compared with the traditional procedure (100 equiv. of anhydride and 1.5-4 h of reaction time), the present methodology has the advantages of short reaction time (10-20 min), and avoiding excess of anhydride (only 1.5 equiv.). Moreover, two compounds exhibited the promising anti-HIV-1 activity when evaluated for their inhibitory activity against HIV-1 replication in acutely infected C8166 cells.

引用

页码：400 / 407

页数：8

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