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Bacterial resistance development has become a very serious clinical problem for many classes of antibiotics. The 3-aryl-2-oxazolidinones are a relatively new class of synthetic antibacterial agents, having a new mechanism of action which involves very early inhibition of bacterial protein synthesis. We have prepared two potent, synthetic oxazolidinones, U-100592 and U-100766, which are currently in clinical development for the treatment of serious multidrug-resistant Gram-positive bacterial infections caused by strains of staphylococci, streptococci,and enterococci. The in vitro and in vivo (po and iv) activities of U-100592 and U-100766 against representative strains are similar to those of vancomycin. U-100592 and U-100766 demonstrate potent in vitro activity against Mycobacterium tuberculosis. A novel and practical asymmetric synthesis of (5S)-(acetamidomethyl)-2-oxazolidinones has been developed and is employed for the synthesis of U-100592 and U-100766. This involves the reaction of N-lithioarylcarbamates with (R)-glycidyl butyrate, resulting in excellent yields and high enantiomeric purity of the intermediate (R)-5-(hydroxymethyl)-2-oxazolidinones. |
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zap65535(金币+0,VIP+0):质量不合格 12-25 01:14
| 对许多抗菌学来讲，抗菌药品的开发是很重要的临床问题。The 3-aryl-2-oxazolidinones 是相对较新种类的合成抗菌剂，它的新作用机理包括在早期阻止病菌蛋白质的合成 .我们准备了2种有效的人工合成剂oxazolidinones, U-100592 和 U-100766，它们是现今临床发展上针对由葡萄糖菌、链球菌和肠球菌引起的严重的多重耐药性革兰氏(染色)阳性细菌感染的治疗药品。The in vitro and in vivo (po and iv) activities of U-100592 and U-100766 against representative strains are similar to those of vancomycin. 在对抗典型的疾病类型中，U-100592 和U-100766 在试管中和有机体内的活跃性和万古霉素相似 |
3楼2009-12-18 23:24:39