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Molecules 2018, 23(11), 2936; https://doi.org/10.3390/molecules23112936

Microwave-Assisted Expeditious Synthesis of 2-Alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines Catalyzed by HgCl2 under Solvent-Free Conditions as Potential Anti-HIV-1 Agents

Laboratory of Pharmaceutical Design & Synthesis, Department of Plant Protection, College of Forestry, Henan University of Science and Technology, Luoyang 471003, China
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Academic Editor: John Spencer
Received: 30 September 2018 / Revised: 3 November 2018 / Accepted: 9 November 2018 / Published: 10 November 2018
(This article belongs to the Special Issue Microwave-mediated Chemistry)
Full-Text   |   PDF [2122 KB, uploaded 10 November 2018]   |  

Abstract

A series of 2-alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines were expeditious prepared under microwave-assisted, catalyzed by HgCl2 and solvent-free conditions. This method has the advantage of low catalyst loading and recovering catalyst, ease reaction and repaid reaction times, easy separation products and excellent yields, and more conducive to the large-scale synthesis products. Furthermore, compounds 3s, 3y, 3a′, 3b′, 3f′, 3i′, 3q′, and 3r′ exhibited more potent anti-HIV-1 activity with EC50 values of 3.35, 6.12, 3.63, 9.54, 1.79, 0.51, 3.00, and 4.01 μg/mL, and TI values of 32.66, >32.68, 31.22, 13.94, 24.27, 39.59, 26.01, and 24.51, respectively. Especially compound 3i′ displayed the highest anti-HIV-1 activity with TI values of 39.59. View Full-Text
Keywords: 1,3,4-oxadiazolines; microwave irradiation; HgCl2 catalyst; anti-HIV-1 activity 1,3,4-oxadiazolines; microwave irradiation; HgCl2 catalyst; anti-HIV-1 activity
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Che, Z.; Tian, Y.; Liu, S.; Jiang, J.; Hu, M.; Chen, G. Microwave-Assisted Expeditious Synthesis of 2-Alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines Catalyzed by HgCl2 under Solvent-Free Conditions as Potential Anti-HIV-1 Agents. Molecules 2018, 23, 2936.

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