Furneri P M, Nicoletti G
Institute of Microbiology, University of Catania, Italy.
J Chemother. 1991 Jan;3 Suppl 1:24-7.
Macrolides belong to a large family of drugs called macrocyclic antibiotics, that can be divided into four groups: macrolactamas or ansamycins, polyene macrolides, macrolide-like compounds and macrolide antibiotics. Macrolide antibiotics comprise a large group of drugs, which are very much alike, characterized by large lactonic cycle with 12, 14, 15 or 16 atoms, to which are bound sugar and/or aminosugar. Although there are very large structural differences, macrolides represent a homogeneous group of drugs for which both a spectrum and a mode of action are similar. Macrolide antibiotics bind to the large subunit of prokaryotic ribosomes and perturb protein synthesis. The antimicrobial activity of macrolides is broad spectrum, being exhibited against gram-positive and gram-negative bacteria, including actinomyces and mycobacteria, as well as against treponemes, mycoplasmas, chlamydiae, rickettsias and also against some protozoa. Depending on the drug concentrations, bacterial species and phase of growth, macrolides may be bacteriostatic or bactericidal. Macrolides show high tissue/serum rations and greater concentrations of antibiotics are though to be achieved at the presumed site of infection. Such findings are in agreement with the apparent volumes of distribution for all the macrolide drugs, which are generally large. The worldwide resurgence of interest in macrolide antibiotics has yielded several semisynthetic derivatives of 14- and 16-membered macrolides which have progressed to clinical trials.
大环内酯类药物属于一大类被称为大环抗生素的药物，可分为四组：大环内酯胺类或安莎霉素类、多烯大环内酯类、大环内酯样化合物和大环内酯类抗生素。大环内酯类抗生素包含一大类药物，它们非常相似，其特征是具有12、14、15或16个原子的大内酯环，与糖和/或氨基糖相连。尽管存在很大的结构差异，但大环内酯类药物代表了一组药物，其抗菌谱和作用方式相似。大环内酯类抗生素与原核生物核糖体的大亚基结合并干扰蛋白质合成。大环内酯类药物的抗菌活性具有广谱性，对革兰氏阳性菌和革兰氏阴性菌（包括放线菌和分枝杆菌）以及对密螺旋体、支原体、衣原体、立克次氏体以及一些原生动物均有抗菌活性。根据药物浓度、细菌种类和生长阶段，大环内酯类药物可能具有抑菌或杀菌作用。大环内酯类药物显示出高组织/血清比率，并且据认为在假定的感染部位可达到更高的抗生素浓度。这些发现与所有大环内酯类药物的表观分布容积一致，其通常较大。全球对大环内酯类抗生素的兴趣再度兴起，已产生了几种14元和16元大环内酯类的半合成衍生物，这些衍生物已进入临床试验阶段。
