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Antianaerobic activity of the ketolide RU 64004 compared to activities of four macrolides five beta-lactams clindamycin and metronidazole.

机译:与四个大环内酯类五个β-内酰胺类克林霉素和甲硝唑的活性相比酮内酯RU 64004的抗厌氧活性。

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摘要

Agar dilution methodology (with added Oxyrase in the case of the macrolide group to allow incubation without added CO2) was used to compare the activity of RU 64004, a new ketolide, with the activities of erythromycin, azithromycin, clarithromycin, roxithromycin, clindamycin, amoxicillin with and without clavulanate, piperacillin with and without tazobactam, metronidazole, and imipenem against 379 anaerobes. Overall, RU 64004 yielded an MIC at which 50% of the isolates are inhibited (MIC50) of 1.0 microg/ml and an MIC90 of 16.0 microg/ml. In comparison, MIC50s and MIC90s of erythromycin, azithromycin, clarithromycin, and roxithromycin were 2.0 to 8.0 and >64.0 microg/ml, respectively. MICs of macrolides, including RU 64004, were higher for Bacteroides ovatus, Fusobacterium varium, Fusobacterium mortiferum, and Clostridium difficile than for the other species. RU 64004 was more active against gram-positive rods and cocci, Prevotella and Porphyromonas spp., and fusobacteria other than F. mortiferum and F. varium than against the Bacteroides fragilis group. Overall MIC50s and MIC90s (in micrograms per milliliter), respectively, of other compounds were as follows: clindamycin, 1.0 and 16.0; amoxicillin, 4.0 and 64.0; amoxicillin-clavulanate, 0.5 and 4.0; piperacillin, 8.0 and >64.0; piperacillin-tazobactam, 1.0 and 16.0; metronidazole, 1.0 and 4.0; and imipenem, 0.25 and 1.0.
机译:琼脂稀释法(在大环内酯类的情况下添加了氧化酶,使其在不添加CO2的情况下进行孵育)用于比较新的酮内酯RU 64004的活性与红霉素,阿奇霉素,克拉霉素,罗红霉素,克林霉素,阿莫西林的活性含或不含克拉维酸盐,含或不含他唑巴坦,甲硝唑和亚胺培南的哌拉西林,可对抗379种厌氧菌。总体而言,RU 64004产生的MIC为1.0 microg / ml,抑制了50%的分离株(MIC50),MIC90为16.0 microg / ml。相比之下,红霉素,阿奇霉素,克拉霉素和罗红霉素的MIC50和MIC90分别为2.0至8.0和> 64.0 microg / ml。包括RU 64004在内的大环内酯类化合物的MIC高于其他物种,其中包括卵形拟杆菌,varsobacter varium,Fusobacter mortiferum和Clostridium difficile。 RU 64004对革兰氏阳性球菌和球菌,普氏杆菌和卟啉单胞菌以及除镰孢镰刀菌和var。varium以外的梭菌的活性比对脆弱拟杆菌的活性更高。其他化合物的总MIC50和MIC90(分别以微克/毫升计)如下:克林霉素1.0和16.0;克林霉素1.0和16.0。阿莫西林4.0和64.0;阿莫西林-克拉维酸0.5和4.0;哌拉西林8.0和> 64.0;哌拉西林-他唑巴坦1.0和16.0;甲硝唑1.0和4.0;亚胺培南分别为0.25和1.0。

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