CAS: 1352062-19-1; (1S,2S,3R,4R)-3-((S)-1-Acetamido-2-Ethylbutyl)-4-Amino-2-Hydroxyl Cyclopentane-1-Carboxylic Acid Hydrochloride

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229615-05-8 1624261-89-7 2758048-80-3

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(-)-methyl (1S,2S,3R,4R)-3-[(1S)-1-(acetylamino)-2-ethylbutyl]-4-[(tert-butoxycarbonyl)amino]-2-hydroxycyclopentanecarboxylate

📜(-)-Methyl (1S,2S,3R,4R)-3-[(1S)-1-(Acetylamino)-2-Ethylbutyl]-4-[(Tert-Butoxycarbonyl)Amino]-2-Hydroxycyclopentanecarboxylate置于盐酸,水体系中,用 乙醚 用作溶剂,化学反应 24.0H,以100%的收率获得帕拉米韦杂质
参考文献:The De-Guanidinylated Derivative Of Peramivir Remains A Potent Inhibitor Of Influenza Neuraminidase
标题:The De-Guanidinylated Derivative Of Peramivir Remains A Potent Inhibitor Of Influenza Neuraminidase
摘要:The Guanidine Function In The Potent Neuraminidase Inhibitor Peramivir Was Included Early On In The Drug Design Process,And Examination Of X-Ray Structural Data For The Enzyme-Inhibitor Complex Would Seem To Indicate That The Guanidine Plays A Critical Role In Promoting Binding. However,This Functional Group May Also Contribute To The Poor Oral Availability Of The Drug. Given That The Relative Stereochemistry On The Guanidine-Bearing Carbon In Peramivir Is Opposite To That In Zanamivir (A Related Neuraminidase Inhibitor,For Which The Guanidine Function Is Known To Contribute Substantially To The Potency),We Sought To Determine The Importance Of The Guanidine Group To Peramivir'S Overall Potency. Here We Report That The De-Guanidinylated Analogue Of Peramivir Is Only Ca. 1-Order Of Magnitude Less Potent Than Peramivir Itself In Two In Vitro Inhibition Assays. This Suggests That Next-Generation Inhibitors Designed To Improve On Peramivir'S Properties Might Profitably Dispense With The Guanidine Function. (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2011.09.076