214759-22-5Relevant articles and documents
Design and synthesis of heteroaromatic-based benzenesulfonamide derivatives as potent inhibitors of H5N1 influenza A virus
Yu, Yongshi,Tazeem,Xu, Zhichao,Du, Liaoqi,Jin, Mengyu,Dong, Chune,Zhou, Hai-Bing,Wu, Shuwen
, p. 89 - 100 (2019/01/30)
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.
COMPOUNDS FOR USE IN PREVENTION AND TREATMENT OF NEURODEGENERATIVE DISEASES AND PAIN
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Paragraph 0040; 0061, (2020/09/17)
Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N6-[(3-halothien-2-yl)methyl]adenosine, N6-[(4-halothien-2-yl)methyl]adenosine, and N6-[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N6-[(2-bromothien-3-yl)methyl]adenosine, N6-[(4-bromothien-3-yl)methyl]adenosine, N6-[(5-bromothien-3-yl)methyl]adenosine N6-[(2-chlorothien-3-yl)methyl]adenosine, N6-[(4-chlorothien-3-yl)methyl]adenosine, and N6-[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.
COMPOUNDS FOR USE IN PREVENTION AND TREATMENT OF NEURODEGENERATIVE DISEASES AND PAIN
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Paragraph 0040; 0061, (2019/01/06)
Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting ofN 6 -[(3-halothien-2-yl)methyl]adenosine,N 6 -[(4-halothien-2-yl)methyl]adenosine, andN 6 -[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting ofN 6 -[(2-bromothien-3-yl)methyl]adenosine,N 6 -[(4-bromothien-3-yl)methyl]adenosine,N 6 -[(5-bromothien-3-yl)methyl]adenosineN 6 -[(2-chlorothien-3-yl)methyl]adenosine,N 6 -[(4-chlorothien-3-yl)methyl]adenosine, andN 6 -[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.