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Dihydro-2H-thiopyran-3(4H)-one-1,1-dioxide – a versatile building block for the synthesis of new thiopyran-based heterocyclic systems†
New Journal of Chemistry ( IF 3.3 ) Pub Date : 2017-12-18 00:00:00 , DOI: 10.1039/c7nj03846a
Vitalii A. Palchykov 1, 2, 3, 4 , Roman M. Chabanenko 1, 2, 3, 4 , Valeriy V. Konshin 5, 6, 7, 8 , Victor V. Dotsenko 5, 6, 7, 8, 9 , Sergey G. Krivokolysko 5, 6, 7, 8 , Elena A. Chigorina 8, 10, 11 , Yuriy I. Horak 1, 4, 12, 13 , Roman Z. Lytvyn 1, 4, 12, 13 , Andriy A. Vakhula 1, 4, 12, 13 , Mykola D. Obushak 1, 4, 12, 13 , Alexander V. Mazepa 4, 14, 15, 16
Affiliation  

Three series of new cyclic sulfones have been prepared by a one-pot multi-component reaction (MCR) starting from the readily available dihydro-2H-thiopyran-3(4H)-one-1,1-dioxide. The in silico screening of the synthesized compounds revealed their high anti-inflammatory, antiarthritic, antiasthmatic and antiallergic potential coupled with the strong probability levels of cystinyl aminopeptidase inhibition. The key structures were confirmed by 2D NMR techniques.

中文翻译:

Dihydro-2 H -thiopyran-3(4 H)-one-1,1-dioxide-合成新的基于噻喃基的杂环系统的通用构件

从容易获得的二氢-2 H-硫代吡喃-3(4 H)-one-1,1-二氧化物开始,通过一锅多组分反应(MCR)制备了三个系列的新型环状砜。的在计算机芯片筛选合成的化合物显示它们的高的抗炎,抗关节炎,抗哮喘和抗过敏潜在加上氨肽酶胱抑制的强概率水平。关键结构通过2D NMR技术确认。
更新日期:2017-12-18
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