Black Michael T, Coleman Kenneth
Novexel SA, Parc Biocitech, 102 Avenue Gaston Roussel, Romainville, France.
Curr Opin Investig Drugs. 2009 Aug;10(8):804-10.
Inhibitors of the GyrA and ParC subunits of the bacterial type IIA topoisomerases DNA gyrase and topoisomerase IV, respectively, belong to classes of antibiotics that are among the most successful of the past 50 years, both in a therapeutic and a commercial sense. The initial promise of progressive modification of an antibiotic scaffold to extend the antibacterial spectrum and to modulate pharmacokinetic/pharmacodynamic parameters of existing antibiotics in an advantageous manner has been tempered by the frequent concomitant appearance of serious toxicity. The merits of the most prominent novel antibiotics that have reached, or are expected to reach the clinical phase of drug development are summarized in this review.
细菌IIA型拓扑异构酶DNA促旋酶和拓扑异构酶IV的GyrA和ParC亚基抑制剂，分别属于过去50年中最成功的抗生素类别，在治疗和商业意义上都是如此。通过对抗生素骨架进行逐步修饰以扩展抗菌谱并以有利方式调节现有抗生素的药代动力学/药效学参数，这一最初的前景因严重毒性的频繁出现而受到影响。本文综述了已进入或预计将进入药物开发临床阶段的最突出新型抗生素的优点。
