Article
Peramivir analogues bearing hydrophilic side chains exhibit higher activities against H275Y mutant than wild-type influenza virus.
Organic & biomolecular chemistry - 29 Nov 2017
Chiu Din-Chi, Lin Tzu-Chen, Huang Wen-I, Cheng Ting-Jen, Tsai Keng-Chang, Fang Jim-Min
Abstract excerpt
Peramivir is an effective anti-influenza drug in the clinical treatment of influenza, but its efficacy toward the H275Y mutant is reduced. The previously reported cocrystal structures of inhibitors in the mutant neuraminidase (NA) suggest that the hydrophobic side chain should be at the origin of reduced binding affinity. In contrast, zanamivir having a hydrophilic glycerol side chain still possesses high...
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