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2-(4-硝基苯氧基)乙醇置于三溴化磷体系中,用 氯仿 用作溶剂,化学反应生成1-(2-溴乙氧基)-4-硝基苯
参考文献:探索乙二醇连接的呋喃妥因衍生物抗利什曼原虫:合成和体外活性
标题:探索乙二醇连接的呋喃妥因衍生物抗利什曼原虫:合成和体外活性
摘要:利什曼病是一种被忽视的热带疾病,由利什曼原虫引起.据估计,每年有超过 3.5 亿人面临感染风险.目前临床上使用的治疗方法价格昂贵,有毒副作用,并且面临寄生虫耐药性.因此,迫切需要新的药物.为了寻求新的,安全的和具有成本效益的药物,合成了一系列新型呋喃妥因乙二醇衍生物,并测试了化合物对杜氏利什曼原虫和大利什曼原虫的体外抗利什曼原虫功效菌株.芳基化乙二醇衍生物被发现是最有效的,其亚微摩尔活性比母体化合物呋喃妥因高 294 倍.类似物2J和2K对l. Major Ir-173 和抗锑l. Donovani 9515 菌株具有亚微摩尔 Ic 50值的最佳抗前鞭毛体活性.
Doi:10.1002/ardp.202200529

专利信息

专利号:US-2011015119-A1
优先权日:2009-06-24
标题:Novel semi-synthetic glycopeptides as antibacterial agents
发明人：CHU DANIEL; YE TAO; WANG BING
权利人:LEAD THERAPEUTICS INC
摘要:Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.