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

Zhi-Ping      Che; Ning      Huang; Xiang      Yu; Liu-Meng      Yang; Jun-Qiang      Ran; Xiaoyan      Zhi; Hui      Xu; Yong-Tang      Zheng

doi:10.2174/1386207311316050005

Abstract

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.

Keywords: 1, 3, 4-Oxadiazoline, microwave heating, human immunodeficiency virus-1, inhibitor.

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Combinatorial Chemistry & High Throughput Screening

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

Volume: 16 Issue: 5

Author(s): Zhi-Ping Che, Ning Huang, Xiang Yu, Liu-Meng Yang, Jun-Qiang Ran, Xiaoyan Zhi, Hui Xu and Yong-Tang Zheng

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Keywords: 1, 3, 4-Oxadiazoline, microwave heating, human immunodeficiency virus-1, inhibitor.

Abstract: 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.

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Che Zhi-Ping, Huang Ning, Yu Xiang, Yang Liu-Meng, Ran Jun-Qiang, Zhi Xiaoyan, Xu Hui and Zheng Yong-Tang, Microwave-Assisted Combinatorial Synthesis of 2-Alkyl-2-(NArylsulfonylindol- 3-yl)-3-N-Acyl-5-Aryl-1,3,4-Oxadiazolines as Anti-HIV- 1 Agents, Combinatorial Chemistry & High Throughput Screening 2013; 16 (5) . https://dx.doi.org/10.2174/1386207311316050005