Article
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
Journal of medicinal chemistry - 26 Jul 2018
Zhang Jian, Poongavanam Vasanthanathan, Kang Dongwei, Bertagnin Chiara, Lu Huamei, Kong Xiujie, Ju Han, Lu Xueyi, Gao Ping, Tian Ye, Jia Haiyong, Desta Samuel, Ding Xiao, Sun Lin, Fang Zengjun, Huang Boshi, Liang Xuewu, Jia Ruifang, Ma Xiuli, Xu Wenfang, Murugan Natarajan Arul, Loregian Arianna, Huang Bing, Zhan Peng, Liu Xinyong
Abstract excerpt
On the basis of our earlier discovery of N1-selective inhibitors, the 150-cavity of influenza virus neuraminidases (NAs) could be further exploited to yield more potent oseltamivir derivatives. Among the synthesized compounds, 15b and 15c were exceptionally active against both group-1 and -2 NAs. Especially for 09N1, N2, N6, and N9 subtypes, they showed 6.80-12.47 and 1.20-3.94 times greater activity than...
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