新型酮内酯衍生物RU 64004（HMR 3004）对呼吸道病原体的抗菌活性
Antibacterial activity of RU 64004 (HMR 3004), a novel ketolide derivative active against respiratory pathogens.
作者信息
Agouridas C, Bonnefoy A, Chantot J F
机构信息
Disease Group Antiinfectives, Hoechst Marion Roussel, Romainville, France.
出版信息
Antimicrob Agents Chemother. 1997 Oct;41(10):2149-58. doi: 10.1128/AAC.41.10.2149.
Abstract
The antibacterial activity of RU 64004, a new ketolide, was evaluated against more than 600 bacterial strains and was compared with those of various macrolides and pristinamycin. RU 64004 had good activity against multiresistant pneumococci, whether they were erythromycin A resistant or not, including penicillin-resistant strains. RU 64004 inhibited 90% of pneumococci resistant to erythromycin A and penicillin G at 0.6 and 0.15 microg/ml, respectively. Unlike macrolides, RU 64004 did not induce the phenotype of resistance to macrolides-lincosamides-streptogramin B. Its good antibacterial activity against multiresistant pneumococci ran in parallel with its well-balanced activity against all bacteria involved in respiratory infections (e.g., Haemophilus influenzae, Moraxella catarrhalis, Streptococcus pyogenes). In contrast to all comparators (14- and 16-membered-ring macrolides and pristinamycin), RU 64004 displayed high therapeutic activity in animals infected with all major strains, irrespective of the phenotypes of the strains. The results suggest that RU 64004 has potential for use in the treatment of infections caused by respiratory pathogens including multiresistant pneumococci.
摘要
新型酮内酯类药物RU 64004的抗菌活性针对600多种细菌菌株进行了评估，并与各种大环内酯类药物和 pristinamycin进行了比较。RU 64004对多重耐药肺炎球菌具有良好的活性，无论它们是否对红霉素A耐药，包括耐青霉素菌株。RU 64004分别在0.6和0.15微克/毫升的浓度下抑制了90%对红霉素A和青霉素G耐药的肺炎球菌。与大环内酯类药物不同，RU 64004不会诱导对大环内酯类-林可酰胺类-链阳菌素B的耐药表型。它对多重耐药肺炎球菌的良好抗菌活性与其对呼吸道感染中涉及的所有细菌（如流感嗜血杆菌、卡他莫拉菌、化脓性链球菌）的平衡活性并行。与所有对照药物（14元和16元环大环内酯类药物和pristinamycin）相比，无论菌株的表型如何，RU 64004在感染所有主要菌株的动物中均表现出高治疗活性。结果表明，RU 64004有潜力用于治疗由包括多重耐药肺炎球菌在内的呼吸道病原体引起的感染。
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