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. It exhibits 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].

老鼠在接受PF-04753299 (皮下剂量；载体：40% β环糊精溶于水) 的处理后0.5小时和4小时，遭受了铜绿假单胞菌UC12120株的腹腔挑战，这是一株对青霉素有抗性、对喹诺酮敏感的临床分离株（1a最低抑菌浓度MIC = 0.25 μg/mL）。在感染后24小时，动物被处死，随后测定脾脏的细菌负荷。与未经处理的动物相比，减少50%细菌负荷所需的化合物剂量（ED50）被确定为35 mg/kg[2]。