PF-04753299 is a potent and selective inhibitor of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC), demonstrating bactericidal effects against gonococcal isolates and exhibiting inhibitory activity against E. coli, P. aeruginosa, and K. pneumoniae, with minimum inhibitory concentration (MIC) 90 values of 2 μg/ml, 4 μg/ml, and 16 μg/ml, respectively. This compound is utilized in researching gram-negative bacterial infections [1].

Rats were subjected to intraperitoneal challenge with Pseudomonas aeruginosa strain UC12120, a penicillin-resistant, quinolone-susceptible clinical isolate (1a Minimum Inhibitory Concentration MIC = 0.25 μg/mL), at 0.5 hr and 4 hr post-treatment with PF-04753299 (Subcutaneous Dose; Vehicle: 40% β-cyclodextrin dissolved in water). At 24 h post-infection, animals were necropsied and the bacterial load on the spleen was subsequently determined. The dose of compound required to reduce the bacterial load by 50% (ED50) was determined to be 35 mg/kg compared to untreated animals [2].