Kim O K, Ohemeng K, Barrett J F
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA.
Expert Opin Investig Drugs. 2001 Feb;10(2):199-212. doi: 10.1517/13543784.10.2.199.
The therapeutic use of DNA gyrase inhibitors, mainly quinolone antibacterials, has proven to be a tremendous success story in the treatment of bacterial infections. The rapid changes in quinolone research and development in recent years have produced several new quinolones: moxifloxacin, gatifloxacin, gemifloxacin and des-6-fluoroquinolone antibacterials. These newly developed compounds are equal or superior to existing ones in their potency, spectrum of activity, pharmacodynamics/pharmacokinetics and safety profiles. The recent discovery of non-fluoroquinolones and 2-pyridone antibacterials represents yet additional progress in the search for novel DNA gyrase inhibitors. Although these two classes of compounds are either in the discovery or early development phase, they extend the possibilities of establishing new structure-activity relationships and new chemotypes for DNA gyrase inhibition.
DNA 回旋酶抑制剂（主要是喹诺酮类抗菌药）的治疗用途已被证明在治疗细菌感染方面取得了巨大成功。近年来喹诺酮研究与开发的快速发展产生了几种新的喹诺酮类药物：莫西沙星、加替沙星、吉米沙星和去氟喹诺酮类抗菌药。这些新开发的化合物在效力、活性谱、药效学/药代动力学和安全性方面与现有化合物相当或更优。非氟喹诺酮类和 2-吡啶酮类抗菌药的最新发现代表了在寻找新型 DNA 回旋酶抑制剂方面的又一进展。尽管这两类化合物都处于发现或早期开发阶段，但它们扩展了建立新的构效关系和 DNA 回旋酶抑制新化学类型的可能性。
