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

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

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 16 , Issue 5 , 2013

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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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Article Details

VOLUME: 16
ISSUE: 5
Year: 2013
Page: [400 - 407]
Pages: 8
DOI: 10.2174/1386207311316050005
Price: $58

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