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Chemical Structure| 115964-29-9 Chemical Structure| 115964-29-9

Structure of Tosufloxacin Tosylate
CAS No.: 115964-29-9

Chemical Structure| 115964-29-9

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Tosufloxacin tosylate is an antibacterial agent that inhibits bacterial DNA gyrase inhibitor.

Synonyms: A-61827 tosylate; Tosufloxacin (tosylate)

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Product Details of Tosufloxacin Tosylate

CAS No. :115964-29-9
Formula : C26H23F3N4O6S
M.W : 576.54
SMILES Code : O=C(C1=CN(C2=CC=C(F)C=C2F)C3=C(C=C(F)C(N4CC(N)CC4)=N3)C1=O)O.O=S(C5=CC=C(C)C=C5)(O)=O
Synonyms :
A-61827 tosylate; Tosufloxacin (tosylate)
MDL No. :MFCD01711971
InChI Key :CSSQVOKOWWIUCX-UHFFFAOYSA-N
Pubchem ID :93858

Safety of Tosufloxacin Tosylate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Tosufloxacin Tosylate

DNA

Isoform Comparison

Biological Activity

Description
Tosufloxacin (A-61827) tosylate is an orally active fluoroquinolone antibiotic known for its broad spectrum of antibacterial efficacy against both gram-positive and gram-negative bacteria[1].[2].

In Vitro:

Cell Line
Concentration Treated Time Description References
Escherichia coli KEIO mutant library 10 µM 18 hours Screen for mutants tolerant to Tosufloxacin, identified 18 mutants that failed to form tolerant persisters Front Cell Infect Microbiol. 2020 Sep 30;10:581986
H. influenzae <0.016 mg/L (MIC50), 0.032 mg/L (MIC90) 18-20 hours Evaluate the in vitro activity of Tosufloxacin against H. influenzae, showing MIC50 and MIC90 of <0.016 and 0.032 mg/liter, respectively. Antimicrob Agents Chemother. 1990 Nov;34(11):2223-7
S. aureus 0.063 mg/L (MIC50), 0.063 mg/L (MIC90) 18-20 hours Evaluate the in vitro activity of Tosufloxacin against S. aureus, showing MIC50 and MIC90 of 0.063 mg/liter. Antimicrob Agents Chemother. 1990 Nov;34(11):2223-7
P. cepacia 4.0 mg/L (MIC50), 8.0 mg/L (MIC90) 18-20 hours Evaluate the in vitro activity of Tosufloxacin against P. cepacia, showing MIC50 and MIC90 of 4.0 and 8.0 mg/liter, respectively. Antimicrob Agents Chemother. 1990 Nov;34(11):2223-7
E. coli <0.016 mg/L (MIC50), 0.016 mg/L (MIC90) 18-20 hours Evaluate the in vitro activity of Tosufloxacin against E. coli, showing MIC50 and MIC90 of <0.016 and 0.016 mg/liter, respectively. Antimicrob Agents Chemother. 1990 Nov;34(11):2223-7
P. aeruginosa (resistant strains) 4.0 mg/L (MIC50), >16.0 mg/L (MIC90) 18-20 hours Evaluate the in vitro activity of Tosufloxacin against resistant P. aeruginosa, showing MIC50 and MIC90 of 4.0 and >16.0 mg/liter, respectively. Antimicrob Agents Chemother. 1990 Nov;34(11):2223-7
P. aeruginosa (standard strains) 0.5 mg/L (MIC50), 2.0 mg/L (MIC90) 18-20 hours Evaluate the in vitro activity of Tosufloxacin against standard P. aeruginosa, showing MIC50 and MIC90 of 0.5 and 2.0 mg/liter, respectively. Antimicrob Agents Chemother. 1990 Nov;34(11):2223-7
Escherichia coli TG1 5 mg/L (80×MIC) 24 hours To evaluate the bactericidal effect of tosufloxacin on E. coli TG1 biofilms, results showed that tosufloxacin effectively reduced the survival rate of E. coli TG1 under non-starved conditions, and its efficacy decreased under starved conditions but was still superior to other fluoroquinolones. Antimicrob Agents Chemother. 2019 May 24;63(6):e00069-19
Neisseria gonorrhoeae ≤0.002-0.008 μg/ml 24 hours To test the in vitro activity of Tosufloxacin against 31 strains of N. gonorrhoeae (including 15 spectinomycin-resistant and 16 penicillinase-producing strains), results showed MIC90 of 0.008 μg/ml. Antimicrob Agents Chemother. 1990 Jun;34(6):971-3
Escherichia coli BW25113 10 µM 3 days Compare persistence between wild-type and mutants, surA and lpcA mutants had no surviving cells after 3 days Front Cell Infect Microbiol. 2020 Sep 30;10:581986
McCoy cells 0.06-0.5 μg/ml 48 hours To test the in vitro activity of Tosufloxacin against 15 clinical isolates of C. trachomatis, results showed MIC90 of 0.25 μg/ml and MBC90 of 0.25 μg/ml. Antimicrob Agents Chemother. 1990 Jun;34(6):971-3

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Swiss Webster mice LPS-induced lethal shock model Oral 100 mg/kg Administered at 47, 17, and 1 h before LPS injection To investigate the protective effect of tosufloxacin against LPS-induced death in mice, results showed 50% survival (P=0.002). Antimicrob Agents Chemother. 2000 Nov;44(11):3169-73

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.67mL

1.73mL

0.87mL

17.34mL

3.47mL

1.73mL

References

 

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