Sarafloxacin hydrochloride exhibits potent in vitro antibacterial activity against a wide range of bacteria, including Staphylococcus aureus, Staphylococcus epidermis, Streptococcus faecium, Streptococcus pyogenes, Escherichia coli, Enterobacter aerogenes, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Acinetobacter, with minimal inhibitory concentrations (MIC) ranging from 0.02 to 1.56 µg/mL. The compound also demonstrates significant in vivo antibacterial efficacy against systemic infections by Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa in mice, with effective dose (ED50) values ranging from 0.6 to 21.4 mg/kg when administered subcutaneously or orally.
Additionally, Sarafloxacin hydrochloride shows inhibition against various enzyme and receptor targets, including Lamin A splicing, HSD17B4, JMJD2E, ALDH1A1, HPGD, and the vitamin D receptor (VDR), with potencies ranging from 2238.7 nM to 100000.0 nM. It also acts as a delayed death inhibitor of the malarial parasite plastid and inhibits human tyrosyl-DNA phosphodiesterase 1 (TDP1) under varying conditions, with potencies between 14581.0 nM and 23715.0 nM.
Furthermore, Sarafloxacin hydrochloride exhibits antiviral properties, including inhibition of SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells at 10 µM concentration after 48 hours, as well as protease inhibition against the SARS-CoV-2 3CL-Pro protease, although these activities show variable inhibition percentages. The compound also demonstrates the ability to inhibit sodium fluorescein uptake in OATP1B1- and OATP1B3-transfected CHO cells with inhibition rates of 109.55% and 115.57%, respectively, at an equimolar concentration of 10 µM..
Note: Summary generated by AI. Data source: ChEMBL 