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 and High Throughput Screening(2013)

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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. © 2013 Bentham Science Publishers.
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关键词
1,3,4-oxadiazoline,human immunodeficiency virus-1,inhibitor,microwave heating
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