Oseltamivir Analogues Bearing N-Substituted Guanidines as Potent Neuraminidase Inhibitors

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• 作者：Caitlin A. Mooney ; Stuart A. Johnson ; Peter 鈥檛 Hart ; Linda Quarles van Ufford ; Cornelis A. M. de Haan ; Ed E. Moret ; Nathaniel I. Martin
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：April 10, 2014
• 年：2014
• 卷：57
• 期：7
• 页码：3154-3160
• 全文大小：406K
• 年卷期：v.57,no.7(April 10, 2014)
• ISSN：1520-4804

文摘

A series of oseltamivir analogues bearing an N-substituted guanidine unit were prepared and evaluated as inhibitors of neuraminidases from four strains of influenza. The two most potent analogues identified contain relatively small N-guanidine substituents (N-methyl and N-hydroxyl) and display enhanced inhibition with IC₅₀ values in the low nanomolar range against neuraminidases from wild-type and oseltamivir-resistant strains. Potential advantages of including the N-hydroxyguanidine moiety in neuraminidase inhibitors are also discussed.