- Design and synthesis of heteroaromatic-based benzenesulfonamide derivatives as potent inhibitors of H5N1 influenza A virus
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Influenza A virus is an enveloped negative single-stranded RNA virus that causes febrile respiratory infection and represents a clinically challenging threat to human health and even lives worldwide. Even more alarming is the emergence of highly pathogenic avian influenza (HPAI) strains such as H5N1, which possess much higher mortality rate (60%) than seasonal influenza strains in human infection. In this study, a novel series of heteroaromatic-based benzenesulfonamide derivatives were identified as M2 proton channel inhibitors. A systematic investigation of the structure-activity relationships and a molecular docking study demonstrated that the sulfonamide moiety and 2,5-dimethyl-substituted thiophene as the core structure played significant roles in the anti-influenza activity. Among the derivatives, compound 11k exhibited excellent antiviral activity against H5N1 virus with an EC50 value of 0.47 μM and selectivity index of 119.9, which are comparable to those of the reference drug amantadine.
- Yu, Yongshi,Tazeem,Xu, Zhichao,Du, Liaoqi,Jin, Mengyu,Dong, Chune,Zhou, Hai-Bing,Wu, Shuwen
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- Benzene sulfonamide compound and application of compound in preparing anti-influenza A virus drug
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The invention discloses a benzene sulfonamide compound and an application of the compound in preparing an anti-influenza A virus drug and belongs to the technical field of pharmaceuticals. A structural formula of the benzene sulfonamide compound is shown as formula (I) as shown in the specification, and the benzene sulfonamide compound is prepared by preparing a corresponding furoyl chloride compound, a thiophenecarbonyl chloride compound and a benzothiophene formyl chloride compound from a furoic acid compound, a thiophenic acid compound or a thionaphthencarboxylic acid compound under the backflow conditions of thionyl chloride and methylbenzene, further performing amination reaction to form a corresponding furoylamide compound, a thiophenecarboxamide compound and a benzothiophene formamide compound, reducing to a corresponding furylmethylamine compound, a thienylmethylamine compound and a benzothiophene methylamine compound under the condition of lithium aluminium hydride, and performing sulfonylation reaction under the conditions of taking triethylamine as an acid-binding agent and dichloromethane as a solvent. The benzene sulfonamide compound can effectively inhibit activity ofan influenza A virus, is low in cytotoxicity and can be used for preparing the anti-influenza A virus drug.
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Paragraph 0027; 0030; 0031
(2018/07/06)
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- Design, synthesis, and evaluation of potential inhibitors of brassinin glucosyltransferase, a phytoalexin detoxifying enzyme from Sclerotinia sclerotiorum
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Sclerotinia sclerotiorum is a fungal pathogen, which causes stem rot in crucifer crops and in several other plant families resulting in enormous yield losses all over the world. Brassinin is a phytoalexin produced by crucifer plants as part of a general d
- Pedras, M. Soledade C.,Hossain, Mohammad
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p. 5981 - 5996
(2008/03/27)
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