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Eur J Med Chem. 2018 Sep 27;159:206-216. doi: 10.1016/j.ejmech.2018.09.065. [Epub ahead of print]
Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors.
Yu Y1, Tang Q2, Xu Z1, Li S2, Jin M1, Zhao Z2, Dong C1, Wu S3, Zhou HB4.
Author information
Abstract
H5N1 virus, one subtype of highly pathogenic influenza A virus in human infection, has recently received attention due to its unpredictable and high mortality. In this study, a series of arylsulfonamide derivatives were identified as improved H5N1 inhibitors for the influenza treatment by systematic structure-activity relationship investigation. Among them, the most potent H5N1 inhibitor 3h exhibited excellent antiviral activity against H5N1 virus with EC50 value of 0.006 μM and selectivity index 33543.3. Moreover, the molecular docking of 3h with M2 proton channel protein provides practical way for understanding the inhibition of H5N1 with this kind of compounds.
KEYWORDS:
Arylsulfonamide inhibitors; H5N1 virus; High mortality; Structure-activity relationship
PMID: 30292897 DOI: 10.1016/j.ejmech.2018.09.065
Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitors.
Yu Y1, Tang Q2, Xu Z1, Li S2, Jin M1, Zhao Z2, Dong C1, Wu S3, Zhou HB4.
Author information
Abstract
H5N1 virus, one subtype of highly pathogenic influenza A virus in human infection, has recently received attention due to its unpredictable and high mortality. In this study, a series of arylsulfonamide derivatives were identified as improved H5N1 inhibitors for the influenza treatment by systematic structure-activity relationship investigation. Among them, the most potent H5N1 inhibitor 3h exhibited excellent antiviral activity against H5N1 virus with EC50 value of 0.006 μM and selectivity index 33543.3. Moreover, the molecular docking of 3h with M2 proton channel protein provides practical way for understanding the inhibition of H5N1 with this kind of compounds.
KEYWORDS:
Arylsulfonamide inhibitors; H5N1 virus; High mortality; Structure-activity relationship
PMID: 30292897 DOI: 10.1016/j.ejmech.2018.09.065