CAS: 1322062-57-6; Moxifloxacin Decarboxy Analog

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moxifloxacin

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    📜莫西沙星置于sodium Cyanide体系中,用 二甲基亚砜 用作溶剂,化学反应 17.0H,以99%的收率获得莫西沙星去羧基类似物
    参考文献:Synthesis And Evaluation Of 1-Cyclopropyl-2-Thioalkyl-8-Methoxy Fluoroquinolones
    标题:Synthesis And Evaluation Of 1-Cyclopropyl-2-Thioalkyl-8-Methoxy Fluoroquinolones
    摘要:Novel Fluoroquinolone Derivatives Substituted With A 2-Thioalkyl Moiety,With And Without A Concomitant 3-Carboxylate Group,Were Synthesized To Evaluate The Effect Of C-2 Thioalkyl Substituents On Gyrase Binding And Inhibition. The Presence Of A 2-Thioalkyl Group Universally Decreased Activity As Compared To Parent Fluoroquinolones. However,With Derivatives Of Moxifloxacin The Presence Of Either A 2-Thioalkyl Group Or A 3-Carboxylate Moiety Increased Activity Over The 2,3-Unsubstituted Derivative. Energy Minimization Of Structures Provides An Explanation For Relative Activities Of Fluoroquinolones Having A C-2 Thio Moiety. (C) 2011 Elsevier Ltd. All Rights Reserved.
    Doi:10.1016/j.Bmcl.2011.05.112

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    参考文献:10.1016/j.bmcl.2011.05.112
    摘要:Marks KR, Malik M, Mustaev A, Hiasa H, Drlica K, Kerns RJ. Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones. Bioorganic & Medicinal Chemistry Letters. 2011 Aug;21(15):4585–8. doi: 10.1016/j.bmcl.2011.05.112.
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