CAS: 55752-58-4; (2,3-Dimethylphenyl)Thiourea

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📜2,3-二甲基苯胺置于水,Sodium Hydroxide体系中,用 乙醇 作为反应溶剂,化学反应生成 2,3-二甲基苯基硫脲
参考文献:Structure-activity Relationships Of 2-Aminothiazoles Effective Against Mycobacterium Tuberculosis
标题:Structure-activity Relationships Of 2-Aminothiazoles Effective Against Mycobacterium Tuberculosis
摘要:A Series Of 2-Aminothiazoles Was Synthesized Based On A Hts Scaffold From A Whole-Cell Screen Against Mycobacterium Tuberculosis (Mtb). The Sar Shows The Central Thiazole Moiety And The 2-Pyridyl Moiety At C-4 Of The Thiazole Are Intolerant To Modification. However,The N-2 Position Of The Aminothiazole Exhibits High Flexibility And We Successfully Improved The Antitubercular Activity Of The Initial Hit By More Than 128-Fold Through Introduction Of Substituted Benzoyl Groups At This Position. N-(3-Chlorobenzoyl)-4-(2-Pyridinyl)-1,3-Thiazol-2-Amine (55) Emerged As One Of The Most Promising Analogues With A Mic Of 0.024 Mu M Or 0.008 Mu G/ml In 7H9 Media And Therapeutic Index Of Nearly Similar To 300. However,55 Is Rapidly Metabolized By Human Liver Microsomes (T(1/2) = 28 Min) With Metabolism occurring At The Invariant Aminothiazole Moiety And Mtb Develops Spontaneous Low-Level Resistance With A Frequency Of Similar To 10 (5). (C) 2013 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2013.08.048