结构修饰性四环素类抗生素研究进展

Research Progress in the Tetracyclines Modification

四环素类抗生素是发现于20世纪40年代的一类广谱抗生素,50年代开始应用于幼儿和孕妇以外的临床。同时,在相当长的时期内四环素还是重要的促进动物生长的添加剂,目前仍然有少量的四环素还应用于人类临床。四环素耐药病原体的相继发现,严重影响了四环素的治疗效果,因而,四环素结构的适当修饰可改善其性能,是探索开发新药的有效途径之一。文章综述了四环素类抗生素药物的主要化学性质、抗菌作用及耐药机制和结构修饰的最新进展,并简要列举了增强抗菌活性的四环素结构修饰物和结构修饰后所获得的临床治疗目的的相关性等。

Tetracyclines belong to a family of structurally related compounds that includes tetracycline,doxycycline, chlortetracycline, sancycline and methacyclineand are widely used antibiotics.Since their discovery in 1943, this class of antibiotics has found use in the chnical treatment of a wide variety of infectious microorganisms. Tetracyclines are widely used as broad spectrum antibiotics for their high activity against nearly all gram-positive and gram-negative bacteria. The importance of these derivatives in？antibiotic resistance？has recently been overshadowed by increasing resistance curtailing their current clinical use. Tetracycline modification can improve the therapeutic？effect, it is one of the effective ways to explore a new drugs. In this paper, the research progress in the tetracycline modification was reviewed in the chemical properties, antibacterial effect, mechanisms and new developments of structural modifications.