Pazufloxacin (mesylate)

Pazufloxacin is a broad-spectrum synthetic fluoroquinolone antibiotic. It is active against Gram-negative and Gram-positive bacteria, including clinical isolates of E. coli, K. pneumoniae, methicillin-susceptible and -resistant S. aureus, and methicillin-susceptible and -resistant S. epidermidis (MIC90s = 0.05, 0.1, 0.39, 12.5, 0.39, and 6.25 µg/ml, respectively). It inhibits E. coli, P. aeruginosa, and S. aureus DNA gyrase (IC50s = 0.88, 1.9, and 10.2 µg/ml, respectively) and S. aureus topoisomerase IV (IC50 = 24.2 µg/ml) in cell-free assays. In vivo, pazufloxacin is active against systemic E. coli, K. pneumoniae, and methicillin-resistant S. aureus infections in mice (ED50s = 0.15, 5.5, and 4.5 mg/kg, respectively).Formal Name: 10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid monomethanesulfonate. CAS Number: 163680-77-1. Synonyms: Pazufloxacin methanesulfonate, T-3762. Molecular Formula: C16H15FN2O4 . CH3SO3H. Formula Weight: 414.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 239, 318 nm. SMILES: OC(C(C1=O)=CN2[C@@H](C)COC3=C2C1=CC(F)=C3C4(N)CC4)=O.CS(=O)(O)=O. InChi Code: InChI=1S/C16H15FN2O4.CH4O3S/c1-7-6-23-14-11(16(18)2-3-16)10(17)4-8-12(14)19(7)5-9(13(8)20)15(21)22,1-5(2,3)4/h4-5,7H,2-3,6,18H2,1H3,(H,21,22),1H3,(H,2,3,4)/t7-,/m0./s1. InChi Key: UDHGFPATQWQARM-FJXQXJEOSA-N.