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Comparative in vitro activities of new 14-, 15-, and 16-membered macrolides.

机译:比较新的14、15和16元大环内酯类药物的体外活性。

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摘要

The in vitro activities of several 14-, 15- and 16-membered macrolides were compared with that of erythromycin. In general, 14-membered macrolides such as erythromycin, clarithromycin, and flurithromycin were more active against streptococci and Bordetella pertussis than was the 15-membered macrolide azithromycin, which was more active than 16-membered macrolides such as miocamycin and rokitamycin. Clarithromycin was the most active compound against Streptococcus pyogenes, pneumococci, Listeria monocytogenes, and Corynebacterium species. Legionella pneumophila was most susceptible to miocamycin, clarithromycin, and rokitamycin. Branhamella catarrhalis, Neisseria gonorrhoeae, and Haemophilus influenzae were most susceptible to azithromycin. Azithromycin and dirithromycin were the most active compounds against Campylobacter jejuni. MICs of 16-membered macrolides for strains expressing inducible-type resistance to erythromycin were less than or equal to 1 microgram/ml, whereas none of the compounds had activity against strains expressing constitutive-type resistance. The MICs of roxithromycin, miocamycin, rokitamycin, and josamycin increased in the presence of human serum, whereas MICs of the other compounds either were unchanged or decreased.
机译:将几种14、15和16元大环内酯类药物的体外活性与红霉素进行了比较。总的来说,与15元大环内酯类阿奇霉素相比,红霉素,克拉霉素和百日咳杆菌等14元大环内酯类药物对链球菌和百日咳博德特氏菌的活性更高,后者比米卡霉素和罗奇霉素等16元大环内酯类药物更具活性。克拉霉素是针对化脓性链球菌,肺炎球菌,单核细胞增生性李斯特菌和棒状杆菌属物种最具活性的化合物。嗜肺军团菌对米卡霉素,克拉霉素和罗他霉素最敏感。卡他氏杆菌,淋病奈瑟氏球菌和流感嗜血杆菌对阿奇霉素最敏感。阿奇霉素和地红霉素是针对空肠弯曲菌最活跃的化合物。表达红霉素诱导型抗性的菌株的16元大环内酯类化合物的MIC小于或等于1微克/毫升,而这些化合物均没有抗表达本构型抗性的菌株的活性。在存在人血清的情况下,罗红霉素,米卡霉素,罗他霉素和若沙霉素的MICs增加,而其他化合物的MICs不变或降低。

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