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

Anna Vickers, Shazad Mushtaq, Neil Woodford, Michel Doumith, David M. Livermore
2018 Antimicrobial Agents and Chemotherapy  
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 Enterobacteriaceae, Acinetobacter baumannii, and Pseudomonas aeruginosa 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
more » ... t for one Serratia isolate with porin and efflux lesions. mcr-1 did not affect MICs.
doi:10.1128/aac.00689-18 pmid:29914946 fatcat:krrhkbbjhffnhhufqu57m2amue