Garenoxacin

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
Garenoxacin
DrugBank Accession Number
DB06160
Background

Garenoxacin, a quinolone antibiotic, is being investigated for the treatment of gram-positive and gram-negative bacterial infections.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 426.42
Monoisotopic: 426.139113458
Chemical Formula
C23H20F2N2O4
Synonyms
  • Garenoxacin
  • Garénoxacine
  • Garenoxacino
  • Garenoxacinum
External IDs
  • BMS 284756
  • BMS-284756
  • BMS284756
  • T 3811
  • T-3811

Pharmacology

Indication

Investigated for use/treatment in bacterial infection.

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action
Not Available
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Medicalerrors
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcarboseThe therapeutic efficacy of Acarbose can be increased when used in combination with Garenoxacin.
AcebutololThe risk or severity of QTc prolongation can be increased when Acebutolol is combined with Garenoxacin.
AceclofenacAceclofenac may increase the neuroexcitatory activities of Garenoxacin.
AcemetacinAcemetacin may increase the neuroexcitatory activities of Garenoxacin.
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be increased when used in combination with Garenoxacin.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Garenoxacin.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be increased when used in combination with Garenoxacin.
Acetylsalicylic acidAcetylsalicylic acid may increase the neuroexcitatory activities of Garenoxacin.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Garenoxacin.
AcyclovirThe metabolism of Acyclovir can be decreased when combined with Garenoxacin.
Interactions
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Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Garenoxacin mesylateOXI6EF55FR223652-90-2IGTHEWGRXUAFKF-NVJADKKVSA-N

Categories

ATC Codes
J01MA19 — Garenoxacin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as quinoline carboxylic acids. These are quinolines in which the quinoline ring system is substituted by a carboxyl group at one or more positions.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Quinolines and derivatives
Sub Class
Quinoline carboxylic acids
Direct Parent
Quinoline carboxylic acids
Alternative Parents
Hydroquinolones / Hydroquinolines / Pyridinecarboxylic acids / Isoindolines / Isoindoles / Aralkylamines / Benzenoids / Vinylogous amides / Heteroaromatic compounds / Amino acids
show 10 more
Substituents
Alkyl fluoride / Alkyl halide / Amine / Amino acid / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carboxylic acid
show 24 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
V72H9867WB
CAS number
194804-75-6
InChI Key
NJDRXTDGYFKORP-LLVKDONJSA-N
InChI
InChI=1S/C23H20F2N2O4/c1-11-15-5-2-12(8-13(15)9-26-11)16-6-7-17-19(21(16)31-23(24)25)27(14-3-4-14)10-18(20(17)28)22(29)30/h2,5-8,10-11,14,23,26H,3-4,9H2,1H3,(H,29,30)/t11-/m1/s1
IUPAC Name
1-cyclopropyl-8-(difluoromethoxy)-7-[(1R)-1-methyl-2,3-dihydro-1H-isoindol-5-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
SMILES
C[C@H]1NCC2=CC(=CC=C12)C1=CC=C2C(=O)C(=CN(C3CC3)C2=C1OC(F)F)C(O)=O

References

General References
Not Available
ChemSpider
110579
ChEBI
131716
ChEMBL
CHEMBL215303
ZINC
ZINC000003585048
Wikipedia
Garenoxacin

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0232 mg/mLALOGPS
logP1.71ALOGPS
logP1.62ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)6.05ChemAxon
pKa (Strongest Basic)8.88ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area78.87 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity110.37 m3·mol-1ChemAxon
Polarizability42.39 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
This drug is a fluoroquinolone, and these agents are known to inhibit CYP1A2.
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Rodighiero V: Effects of liver disease on pharmacokinetics. An update. Clin Pharmacokinet. 1999 Nov;37(5):399-431. [PubMed:10589374]
  2. Bril F, Gonzalez CD, Di Girolamo G: Antimicrobial agents-associated with QT interval prolongation. Curr Drug Saf. 2010 Jan;5(1):85-92. [PubMed:20210724]
  3. Zhang L, Wei MJ, Zhao CY, Qi HM: Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes. Acta Pharmacol Sin. 2008 Dec;29(12):1507-14. doi: 10.1111/j.1745-7254.2008.00908.x. [PubMed:19026171]

Drug created on March 19, 2008 16:14 / Updated on February 21, 2021 18:52