Repositioning Candidate Details
| Candidate ID: | R0448 |
| Source ID: | DB01208 |
| Source Type: | approved; investigational; withdrawn |
| Compound Type: | small molecule |
| Compound Name: | Sparfloxacin |
| Synonyms: | cis-5-Amino-1-cyclopropyl-7-(3,5-dimethyl-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid; Sparfloxacin |
| Molecular Formula: | C19H22F2N4O3 |
| SMILES: | C[C@H]1CN(C[C@@H](C)N1)C1=C(F)C(N)=C2C(=O)C(=CN(C3CC3)C2=C1F)C(O)=O |
| Structure: |
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| DrugBank Description: | Sparfloxacin is a fluoroquinolone antibiotic indicated for bacterial infections. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription. |
| CAS Number: | 110871-86-8 |
| Molecular Weight: | 392.3998 |
| DrugBank Indication: | For the treatment of adults with the following infections caused by susceptible strains microorganisms: community-acquired pneumonia (caused by <i>Chlamydia pneumoniae</i>, <i>Haemophilus influenzae</i>, <i>Haemophilus parainfluenzae</i>, <i>Moraxella catarrhalis</i>, <i>Mycoplasma pneumoniae</i>, or <i>Streptococcus pneumoniae</i>) and acute bacterial exacerbations of chronic bronchitis (caused by <i>Chlamydia pneumoniae</i>, <i>Enterobacter cloacae</i>, <i>Haemophilus influenzae</i>, <i>Haemophilus parainfluenzae</i>, <i>Klebsiella pneumoniae</i>, <i>Moraxella catarrhalis</i>, <i>Staphylococcus aureus</i>, or <i>Streptococcus pneumoniae</i>). |
| DrugBank Pharmacology: | Sparfloxacin is a synthetic fluoroquinolone broad-spectrum antimicrobial agent in the same class as ofloxacin and norfloxacin. Sparfloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription. Quinolones differ in chemical structure and mode of action from (beta)-lactam antibiotics. Quinolones may, therefore, be active against bacteria resistant to (beta)-lactam antibiotics. Although cross-resistance has been observed between sparfloxacin and other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to sparfloxacin. In vitro tests show that the combination of sparfloxacin and rifampin is antagonistic against Staphylococcus aureus. |
| DrugBank MoA: | The bactericidal action of sparfloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination. |
| Targets: | DNA topoisomerase 4 subunit A inhibitor; DNA gyrase subunit A inhibitor; DNA topoisomerase 2-alpha inhibitor |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I01 | 552 | Pneumonia | A lung disease that involves lung parenchyma or alveolar inflammation and abnormal alveolar filling with fluid (consolidation and exudation). It results from a variety of causes including infection with bacteria, viruses, fungi or parasites, and chemical or physical injury to the lungs. It is accompanied by fever, chills, cough, and difficulty in breathing. http://en.wikipedia.org/wiki/Pneumonia | disease of anatomical entity/respiratory system disease/ lower respiratory tract disease/lung disease | Details |