General Review Article

氟喹诺酮的当前趋势和未来方向

卷 26, 期 17, 2019

页: [3132 - 3149] 页: 18

弟呕挨: 10.2174/0929867325666180214122944

价格: $65

摘要

氟喹诺酮类是一种有趣的合成类抗微生物剂,具有广谱和强效活性。 自从喹诺酮的原型萘啶酮酸的发现以来,已经对喹诺酮核进行了几种结构修饰以改善效力,活性谱,并了解它们的结构活性关系(SAR)。 据报道,C-7取代基对活性有重大影响。 因此,发现C-7或其N-4-哌嗪基部分的取代影响效力,生物利用度和物理化学性质。 此外,它可以增加对哺乳动物拓扑异构酶的亲和力,这可能将喹诺酮类药物从抗菌药物转变为抗癌药物。 此外,真核细胞和原核细胞中DNA拓扑异构酶的存在使它们成为抗菌和抗癌治疗中化学治疗干预的优良靶标。 基于该概念,已经合成了几种氟喹诺酮衍生物并且生物学评价为抗细菌剂,抗结核剂,抗增殖剂,抗病毒剂和抗真菌剂。 本综述旨在关注氟喹诺酮类药物的治疗前景,并更新其非典型应用,如抗结核和抗癌活性。

关键词: 氟喹诺酮类,环丙沙星,抗菌,抗结核,抗增殖,SAR,抗生素趋势。

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