Hardy D J, Hanson C W, Hensey D M, Beyer J M, Fernandes P B
Anti-infective Research Department, Abbott Laboratories, Abbott Park, Illinois 60064.
J Antimicrob Chemother. 1988 Nov;22(5):631-6. doi: 10.1093/jac/22.5.631.
The in-vitro activities of several 14-, 15- and 16-membered macrolides and fluoroquinolones against Campylobacter pylori were determined. In general, 14-membered macrolides, such as clarithromycin and flurithromycin, were more active than the 15-membered macrolide, azithromycin, which was more active than 16-membered macrolides, such as miocamycin and rokitamycin. Fluoroquinolones, except ciprofloxacin and A-61827, were less active than macrolides. Clarithromycin was the most active of the new compounds against C. pylori and was as active as ampicillin. MICs of all compounds at pH 5.5 were increased when compared to MICs determined at pH 7.3. All compounds had MBCs which were the same as or within one two-fold dilution of their MICs. Frequencies of spontaneous resistance development by C. pylori NCTC 11637 at four and eight times the MIC of the compounds were low and ranged from less than 1 x 10(-9) to 1 x 10(-7).
测定了几种14元、15元和16元大环内酯类抗生素及氟喹诺酮类药物对幽门螺杆菌的体外活性。一般来说,14元大环内酯类抗生素,如克拉霉素和氟红霉素,比15元大环内酯类抗生素阿奇霉素活性更强,而阿奇霉素又比16元大环内酯类抗生素,如米卡霉素和罗他霉素活性更强。除环丙沙星和A-61827外,氟喹诺酮类药物的活性比大环内酯类抗生素低。克拉霉素是新型化合物中对幽门螺杆菌活性最强的,其活性与氨苄西林相当。与在pH 7.3条件下测定的最低抑菌浓度(MIC)相比,所有化合物在pH 5.5时的MIC均升高。所有化合物的最低杀菌浓度(MBC)与MIC相同或在其MIC的两倍稀释范围内。幽门螺杆菌NCTC 11637在化合物MIC的4倍和8倍浓度下自发产生耐药性的频率较低,范围从小于1×10^(-9)到1×10^(-7)。