产品描述:
AN3365 is an inhibitor of leucyl-tRNA synthetase (LeuRS; IC50 = 0.31 µM for the E. coli enzyme).{34086} It is active against a variety of Gram-negative and Gram-positive bacteria, including E. coli, E. faecalis, S. epidermidis, S. pneumoniae, and S. pyogenes (MICs = 4, 8, 2, 2, and 2 µg/ml, respectively), as well as a panel of multidrug-resistant (MDR) clinical isolates of the Gram-negative bacteria A. baumannii, Enterobacteriaceae, and P. aeruginosa (MICs = 0.5-4, 0.5-2, and 1-4 µg/ml, respectively). AN3365 inhibits protein, RNA, DNA, and fatty acid synthesis in E. coli (IC50s = 8.3, 105, 366, and 396 µg/ml, respectively). It reduces the number of colony forming units (CFUs) in neutropenic mouse thigh models of E. coli or P. aeruginosa infection when administered at a dose of 30 mg/kg.