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Pazufloxacin

Pazufloxacin structure

Pazufloxacin 

structure
  • CAS No:

    127045-41-4

  • Formula:

    C16H15FN2O4

  • Chemical Name:

    Pazufloxacin

  • Synonyms:

    7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid,10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-,(3S)-;7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid,10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-,(S)-;(3S)-10-(1-Aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid;T 3761;(-)-(3S)-10-(1-Aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid;Pazufloxacin

  • Categories:

    Active Pharmaceutical Ingredients  >  Synthetic Anti-infective Drugs

Description

Pazufloxacin is a fluoroquinolone with a 1-aminocyclopropyl substituent at C10 position. The presence of aminoacyl group at C-10 is a unique feature of the molecule imparting potent broad spectrum activity against gram-positive and gram-negative bacteria. This activity is based on the inhibition of bacterial DNA gyrase.


LSM-5745 is a member of quinolines.|Pazufloxacin is under investigation in clinical trial NCT02592096 (Pazufloxacin Mesilate Ear Drops Clinical Trial Protocol).

Pazufloxacin Basic Attributes

318.3

318.30

1806241-263-5

4CZ1R38NDI

DTXSID5046697

J - Antiinfectives for systemic use

Characteristics

92.9

0.09

like white to light yellow crystalline

1.56

269-271.5 °C

531.5±50.0 °C(Predicted)

275.2±30.1 °C

1.692

2-8°C

4E-12mmHg at 25°C

LD50 i.v. in male mice: >500 mg/kg (Todo)

D25 -88.0° (c = 0.5 in 0.05N aq NaOH)

Safety Information

NONH for all modes of transport

3

20/21/22-34-11

36/37-45-36/37/39-26-16

UU8815300

Xn,C,F

P280

H302-H312-H332

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P312, P304+P340, P312, P322, P330, P363, and P501|Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II. (See all compounds classified as Topoisomerase II Inhibitors.)|Drugs used in the treatment of tuberculosis. They are divided into two main classes: "first-line" agents, those with the greatest efficacy and acceptable degrees of toxicity used successfully in the great majority of cases; and "second-line" drugs used in drug-resistant cases or those in which some other patient-related condition has compromised the effectiveness of primary therapy. (See all compounds classified as Antitubercular Agents.)

10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido(1,2,3-d,e)(1,4)benzoxazinecarboxylic acid

Pazufloxacin Use and Manufacturing

antibactierial

Computed Properties

Molecular Weight:318.30
XLogP3:-0.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:2
Exact Mass:318.10158513
Monoisotopic Mass:318.10158513
Topological Polar Surface Area:92.9
Heavy Atom Count:23
Complexity:603
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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