期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 10, 页码 4563-4577出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01863
关键词
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资金
- COE Project for Private Universities from the Ministry of Education, Culture, Sports, Science and Technology [S0801055, S1311027]
- Japan Society for the Promotion of Science (JSPS)
- National Research Council of Thailand (NRCT) Joint Research Program [12038611-000281, DIA.2/JSPS-Joint4/2555]
- JSPS [22380067, 25460157]
- Grants-in-Aid for Scientific Research [16K00397, 25460157, 26291011, 16H05840, 22380067] Funding Source: KAKEN
People throughout the world continue to be at risk for death from influenza A virus, which is always creating a new variant. Here we present a new effective and specific anti influenza viral neuraminidase (viNA) inhibitor, 9-cyclo-propylcarbonylamino-4-guanidino-Neu5Ac2en (cPro-GUN). Like zanamivir, it is highly effective against N1-N9 avian and N1-N2 human viNAs, including H274Y oseltamivir-resistant N1 viNA, due to its C-6 portion still being anchored in the active site, different from the disruption of oseltamivir's C-6 anchoring by H274Y mutation. Unlike zanamivir, no sialidase inhibitory activity has been observed for cPro-GUN against huNeu1-huNeu4 enzymes. Broad efficacy of cPro-GUN against avian and human influenza viruses in cell cultures comparable to its sialidase inhibitory activities makes cPro-GUN ideal for further development for safe therapeutic or prophylactic use against both seasonal and pandemic influenza.
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