Activity of RX-04 Pyrrolocytosine Protein Synthesis Inhibitors against Multidrug-Resistant Gram-Negative Bacteria

作者：Vickers Anna; Mushtaq Shazad; Woodford Neil; Doumith Michel; Livermore David M^*

来源：Antimicrobial Agents and Chemotherapy, 2018, 62(8).

DOI：10.1128/AAC.00689-18;e00689-18

• 50S ribosomal subunit
• blasticidin
• mcr-1
• pyrrolocytosine

Pyrrolocytosines RX-04A to -D are designed to bind to the bacterial 505 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 Enterobacteriaceae, Acinetobacter baumannii, and Pseudomonas aeruginosa at 0.5 to 4 mu g/ml, with no MICs of >8 mu g/ml. MICs for multidrug-resistant (MDR) carbapenemase producers were up to 2-fold higher than those for control strains; values were highest for one Serratia isolate with porin and efflux lesions. mcr-1 did not affect MICs.

• 出版日期2018-8