Oseltamivir Analogues Bearing N?Substituted Guanidines as Potent Neuraminidase Inhibitors

Caitlin A. Mooney; Stuart A. Johnson; Peter t Hart; Linda Quarles van Ufford; Cornelis A. M. de Haan; Ed E. Moret; Nathaniel I. Martin

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Oseltamivir Analogues Bearing N?Substituted Guanidines as Potent Neuraminidase Inhibitors

机译：带有N？取代胍作为有效神经氨酸酶抑制剂的Oseltamivir类似物

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A series of oseltamivir analogues bearing an Nsubstituted 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 IC_(50) 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.

机译：制备了一系列带有N取代的胍单元的奥司他韦类似物，并将其评估为来自四种流感菌株的神经氨酸酶的抑制剂。鉴定出的两个最有效的类似物含有相对较小的N-胍取代基（N-甲基和N-羟基），并在低纳摩尔范围内以IC_（50）值显示出对野生型和奥司他韦耐药菌株神经氨酸酶的抑制作用增强。还讨论了在神经氨酸酶抑制剂中包括N-羟基胍部分的潜在优势。

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《Journal of Medicinal Chemistry》 |2014年第7期|共7页
作者
Caitlin A. Mooney; Stuart A. Johnson; Peter t Hart; Linda Quarles van Ufford; Cornelis A. M. de Haan; Ed E. Moret; Nathaniel I. Martin;
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正文语种 eng
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关键词
Oseltamivir; Analogues; Bearing;

机译：奥司他韦;类似物;轴承;

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1. Oseltamivir Analogues Bearing N?Substituted Guanidines as Potent Neuraminidase Inhibitors [J] . Caitlin A. Mooney, Stuart A. Johnson, Peter t Hart, Journal of Medicinal Chemistry . 2014,第7期

机译：带有N？取代胍作为有效神经氨酸酶抑制剂的Oseltamivir类似物
2. NH 2 -acyl oseltamivir analogues as potent neuraminidase inhibitors [J] . Kuanglei Wang, Fei Yang, Lihui Wang, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2017,第期

机译：NH 2 - 奥酰·奥司他韦类似物为有效的神经氨酸酶抑制剂
3. Novel N-Substituted oseltamivir derivatives as potent influenza neuraminidase inhibitors: Design, synthesis, biological evaluation, ADME prediction and molecular docking studies [J] . Ye Jiqing, Yang Xiao, Xu Min, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2019,第期

机译：新型N-取代的奥司他虫衍生物作为有效流感神经氨酸酶抑制剂：设计，合成，生物学评估，ADME预测和分子对接研究
4. Desorption Electrospray Ionization Reactions Between Host Crown Ethers and the Influenza Neuraminidase Inhibitor Oseltamivir for the Screening of Potentially Counterfeit Tamiflu~(~R). [C] . Leonard Nyadong, Edward G. Hohenstein, Kristin Johnson, ASMS Conference on Mass Spectrometry and Allied Topics . 2008

机译：解吸电喷雾电离反应宿主醚和流感神经氨酸酶抑制剂Oseltamivir用于筛选潜在的伪造塔米......（〜r）。
5. Synthesis of new glutamate receptor probes: I. Total synthesis of dysiherbaine, a potent glutamate receptor excitotoxin; II. Design and synthesis of dysiherbaine analogues; III. Synthesis and structure-activity relationships of substituted benzothiadiazides and their role as AMPA receptor modulators. [D] . Phillips, Dean Paul. 2001

机译：新型谷氨酸受体探针的合成：I. dysiherbaine的全合成，一种有效的谷氨酸受体兴奋性毒素；二。 dysiherbaine类似物的设计和合成；三，取代的苯并噻二叠氮化物的合成及其构效关系及其作为AMPA受体调节剂的作用。
6. Synthesis and Biological Evaluation of NH2-Sulfonyl Oseltamivir Analogues as Influenza Neuraminidase Inhibitors [O] . Yaping Hu, Binfeng Chen, Zaiqiang Lei, 2019

机译：NH2-磺酰奥瑟他韦类似物作为流感神经氨酸酶抑制剂的合成及生物学评价
7. Synthesis and Biological Evaluation of NH2-Sulfonyl Oseltamivir Analogues as Influenza Neuraminidase Inhibitors [O] . Yaping Hu, Binfeng Chen, Zaiqiang Lei, 2019

机译：NH2-磺酰奥喇叭类似物与流感神经氨酸酶抑制剂的合成与生物学评价

Oseltamivir Analogues Bearing N?Substituted Guanidines as Potent Neuraminidase Inhibitors

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