RX-04 吡咯烷酮胞嘧啶蛋白合成抑制剂对多重耐药革兰氏阴性菌的活性。
Activity of RX-04 Pyrrolocytosine Protein Synthesis Inhibitors against Multidrug-Resistant Gram-Negative Bacteria.
机构信息
Antimicrobial Resistance and Healthcare Associated Infections (AMRHAI) Reference Unit, National Infection Service, Public Health England, London, United Kingdom.
Antimicrobial Resistance and Healthcare Associated Infections (AMRHAI) Reference Unit, National Infection Service, Public Health England, London, United Kingdom
出版信息
Antimicrob Agents Chemother. 2018 Jul 27;62(8). doi: 10.1128/AAC.00689-18. Print 2018 Aug.
Abstract
Pyrrolocytosines RX-04A to -D are designed to bind to the bacterial 50S ribosomal subunit differently from currently used antibiotics. The four analogs had broad anti-Gram-negative activity: RX-04A-the most active analog-inhibited 94.7% of clinical , , and at 0.5 to 4 μg/ml, with no MICs of >8 μg/ml. MICs for multidrug-resistant (MDR) carbapenemase producers were up to 2-fold higher than those for control strains; values were highest for one isolate with porin and efflux lesions. did not affect MICs.
摘要
吡咯并环胞嘧啶 RX-04A 至 -D 的设计目的是与目前使用的抗生素不同，与细菌的 50S 核糖体亚基结合。这四种类似物具有广泛的抗革兰氏阴性活性：RX-04A——最活跃的类似物——在 0.5 至 4μg/ml 时抑制了 94.7%的临床、和分离株，MIC 没有大于 8μg/ml 的。对多药耐药（MDR）碳青霉烯酶产生菌的 MIC 比对照株高 2 倍；对一种具有孔蛋白和外排缺陷的分离株的数值最高。不影响 MIC。
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