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Details

Stereochemistry ABSOLUTE
Molecular Formula C16H15FN2O4
Molecular Weight 318.2997
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PAZUFLOXACIN

SMILES

C[C@H]1COC2=C(C(F)=CC3=C2N1C=C(C(O)=O)C3=O)C4(N)CC4

InChI

InChIKey=XAGMUUZPGZWTRP-ZETCQYMHSA-N
InChI=1S/C16H15FN2O4/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/h4-5,7H,2-3,6,18H2,1H3,(H,21,22)/t7-/m0/s1

HIDE SMILES / InChI

Molecular Formula C16H15FN2O4
Molecular Weight 318.2997
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including, http://www.mt-pharma.co.jp/e/release/nr/mpc/2002/pdf/e020902.pdf

Pazufloxacin is a fused tricyclic quinolone derivative that has a broad spectrum of anti-bacterial activity. Pazufloxacin inhibits bot DNA gyrase and topoisomerase IV and has shown in vitro activity against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella, Enterobacter, Hafnia, Citrobacter, Proteus, Providencia, Serratia, Shigella, Salmonella, Aeromonas and Yersinia. The drug is used for the treatment of infectious diseases such as abdominal infections, genital infections, urinary tract infections, respiratory tract infections, etc.

Originator

Curator's Comment: The development was carried out jointly with Mitsubishi Pharma.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
PASIL

Approved Use

Unknown

Launch Date

1.03083842E12
Curative
PASIL

Approved Use

Unknown

Launch Date

1.03083842E12
Curative
PASIL

Approved Use

Unknown

Launch Date

1.03083842E12
Curative
PASIL

Approved Use

Unknown

Launch Date

1.03083842E12
Curative
PASIL

Approved Use

Unknown

Launch Date

1.03083842E12
PubMed

PubMed

TitleDatePubMed
[Drug interactions between nonsteroidal anti-inflammatory drug and pazufloxacin mesilate, a new quinolone antibacterial agent for intravenous use: convulsions in mice after intravenous or intracerebroventricular administration].
2002 Jun
Patents

Sample Use Guides

The usually recommended dose of Pazufloxacin Injections in most infections is 500 mg twice a day administered as an I.V. infusion over 30-60 minutes. Depending on age, symptoms and severity of infection, the dose of the drug may be reduced to 300 mg twice a day.
Route of Administration: Intravenous
Pazufloxacin has good antibacterial activity against variety of clinical isolates. The MICs at which 90% of the isolates were inhibited (MIC90s) of pazufloxacin were 0.2 to 0.39 ug/ml for Staphylococcus aureus and Staphylococcus epidermidis, including methicillin-resistant strains.5 Pazufloxacin has similar or 2-fold greater activity than other quinolones, against the following Enterobacteriaceae (MIC90 ≤ 0.25 ug/ml): Escherichia coli, Klebsiella, Enterobacter, Hafnia, Citrobacter, Proteus, Providencia, Serratia, Shigella, Salmonella, Aeromonas and Yersinia. Against P. aeruginosa, pazufloxacin shows more potent activity than tosufloxacin, norfloxacin and ofloxacin. Against clinical isolates of methicillin-resistant Staphylococcus aureus and P. aeruginosa, pazufloxacin has an MIC90 of 0.39 ug/ml and an MIC90 of 0.78 ug/ml respectively. MIC90 for clinical isolates of H. influenzae is ≤ 0.013 ug/l.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:43:57 UTC 2023
Edited
by admin
on Fri Dec 15 15:43:57 UTC 2023
Record UNII
4CZ1R38NDI
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PAZUFLOXACIN
INN   JAN   MI   WHO-DD  
INN  
Official Name English
T-3761
Code English
Pazufloxacin [WHO-DD]
Common Name English
(-)-(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
Systematic Name English
PAZUFLOXACIN [JAN]
Common Name English
PAZUFLOXACIN [MI]
Common Name English
pazufloxacin [INN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C795
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
WHO-ATC J01MA18
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
WHO-VATC QJ01MA18
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
Code System Code Type Description
NCI_THESAURUS
C66331
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
DRUG BANK
DB11774
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
SMS_ID
100000083003
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
MESH
C078052
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
EVMPD
SUB09641MIG
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
MERCK INDEX
m8431
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY Merck Index
CAS
127045-41-4
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
DRUG CENTRAL
2070
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
INN
7247
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
FDA UNII
4CZ1R38NDI
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
ChEMBL
CHEMBL240163
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
PUBCHEM
65957
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
EPA CompTox
DTXSID5046697
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
WIKIPEDIA
PAZUFLOXACIN
Created by admin on Fri Dec 15 15:43:57 UTC 2023 , Edited by admin on Fri Dec 15 15:43:57 UTC 2023
PRIMARY
Related Record Type Details
RACEMATE -> ENANTIOMER
SALT/SOLVATE -> PARENT
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ACTIVE MOIETY