In Vitro: Antibacterial agent 138 (compound 7a) inhibits DNA gyrase and topoisomerase IV from S. aureus (IC50=1.22 nM and 8.0 nM, repsectivley), E. coli (IC50=<10 nM and 44 nM, repsectivley), A. baumannii (IC50=2.42 nM and 119.7 nM, repsectivley), and P. aeruginosa (IC50=<10 nM and 27.5 nM, repsectivley) with low nanomolar ranges. Antibacterial agent 138 (up to 100 μM) shows no cytotoxicity on a breast cancer MCF-7 cell line and a liver cancer HepG2 cell.
In Vivo: Antibacterial agent 138 (compound 7a) (25 and 50 mg/kg; iv; single dose) shows bactericidal activity in neutropenic mouse thigh infection model.