Page last updated: 2024-11-06

premafloxacin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Premafloxacin is a synthetic fluoroquinolone antibiotic that exhibits potent antibacterial activity against a broad spectrum of Gram-positive and Gram-negative bacteria. It acts by inhibiting bacterial DNA gyrase and topoisomerase IV, essential enzymes involved in DNA replication and repair. Premafloxacin's high bioavailability and excellent tissue penetration make it a promising candidate for treating various infections, including respiratory, urinary tract, and skin infections. Its potent activity against resistant strains of bacteria, like methicillin-resistant Staphylococcus aureus (MRSA) and penicillin-resistant Streptococcus pneumoniae, makes it a valuable therapeutic option. Premafloxacin's unique chemical structure and mechanism of action make it a subject of continued research and development, aimed at optimizing its therapeutic efficacy and addressing potential side effects. Premafloxacin's importance lies in its potential to address the growing issue of antibiotic resistance and provide effective treatment for a wide range of infections.'

Cross-References

ID SourceID
PubMed CID71455
CHEMBL ID230599
CHEBI ID188832
SCHEMBL ID1230382
MeSH IDM0274116

Synonyms (27)

Synonym
143383-65-7
premafloxacin (usan/inn)
D05605
premafloxacin
CHEMBL230599 ,
u-95376
remafloxacin
1-cyclopropyl-6-fluoro-8-methoxy-7-[(3r)-3-[(1s)-1-(methylamino)ethyl]pyrrolidin-1-yl]-4-oxoquinoline-3-carboxylic acid
1-cyclopropyl-6-fluoro-8-methoxy-7-((r)-3-((s)-1-(methylamino)ethyl)pyrrolidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
bdbm50205462
CHEBI:188832
1-cyclopropyl-6-luoro-8-methoxy-7-[(3r)-3-[(1s)-1-(methylamino)ethyl]pyrrolidin-1-yl]-4-oxoquinoline-3-carboxylic acid
uom2hmo524 ,
premafloxacin [usan:inn]
unii-uom2hmo524
1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-((3r)-3-((1s)-1-(methylamino)ethyl)-1-pyrrolidinyl)-4-oxo-3-quinolinecarboxylic acid
3-quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-(1-(methylamino)ethyl)-1-pyrrolidinyl)-4-oxo-, (s-(r*,s*))-
premafloxacin [inn]
premafloxacin [usan]
1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(3r)-3-[(1s)-1-(methylamino)ethyl]-1-pyrrolidinyl]-4-oxo-3-quinolinecarboxylic acid
SCHEMBL1230382
DTXSID70162407
1-cyclopropyl-6-fluoro-8-methoxy-7-((r)-3-((s)-1-(methylamino)ethyl)pyrrolidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylicacid
gtpl10848
u95376
compound 21 [pmid: 17303420]
Q27291171

Research Excerpts

Overview

Premafloxacin is a novel 8-methoxy fluoroquinolone with enhanced activity against Staphylococcus aureus.

ExcerptReferenceRelevance
"Premafloxacin is a novel 8-methoxy fluoroquinolone with enhanced activity against Staphylococcus aureus. "( Mechanisms and frequency of resistance to premafloxacin in Staphylococcus aureus: novel mutations suggest novel drug-target interactions.
Hooper, DC; Ince, D, 2000
)
2.01
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinolinesA class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki150.00000.00211.840710.0000AID290345
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID290342Antibacterial activity against Streptococcus pneumoniae SV12007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
AID290343Antibacterial activity against fluoroquinolone resistance Streptococcus pneumoniae SP37652007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
AID290353Displacement of [3H]dofetilide from human ERG at 300 uM2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
AID290340Antibacterial activity against Staphylococcus aureus UC762007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
AID290344Antibacterial activity against Haemophilus influenzae HI35422007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
AID290346Antibacterial activity against Moraxella catarrhalis BC-35312007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
AID290341Antibacterial activity against Staphylococcus aureus SA25522007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
AID290345Displacement of [3H]dofetilide from human ERG by fliter binding assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (33.33)18.2507
2000's5 (55.56)29.6817
2010's1 (11.11)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.99

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.99 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.30 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.99)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]