Compounds > azd0914
Page last updated: 2024-11-13

azd0914

Description

zoliflodacin: a DNA gyrase inhibitor for treatment of gonorrhea [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID76685216
CHEMBL ID3544978
SCHEMBL ID15879500
MeSH IDM000607498

Synonyms (40)

Synonym
SCHEMBL15879500
bdbm139376
us8889671, 5
zoliflodacin [who-dd]
spiro(isoxazolo(4,5-g)(1,4)oxazino(4,3-a)quinoline-5(6h),5'(2'h)-pyrimidine)-2',4',6'(1'h,3'h)-trione, 11-fluoro-1,2,4,4a-tetrahydro-2,4-dimethyl-8-((4s)-4-methyl-2-oxo-3-oxazolidinyl)-, (2r,4s,4as)-
zoliflodacin [inn]
(2r,4s,4as)-11-fluoro-2,4-dimethyl-8-((4s)-4-methyl-2-oxo-1,3-oxazolidin-3-yl)-1,2,4,4a-tetrahydro-2'h,6h-spiro((1,2)-oxazolo(4,5-g)(1,4)oxazino(4,3-a)quinoline-5,5'-pyrimidine)-2',4',6'(1'h,3'h)-trione
unii-fwl2263r77
1620458-09-4
etx-0914
zoliflodacin [usan]
zoliflodacin
fwl2263r77 ,
azd-0914
etx0914
azd0914
CHEMBL3544978
(2r,4s,4as)-11-fluoro-2,4-dimethyl-8-((s)-4-methyl-2-oxooxazolidin-3-yl)-1,2,4,4a-tetrahydro-2'h,6h-spiro[isoxazolo[4,5-g][1,4]oxazino[4,3-a]quinoline-5,5'-pyrimidine]-2',4',6'(1'h,3'h)-trione
CS-0016917
HY-17647
DB12817
(2r,4s,4as)-11-fluoro-2,4-dimethyl-8-((s)-4-methyl-2-oxooxazolidin-3-yl)-2,4,4a,6-tetrahydro-1h,1'h-spiro[isoxazolo[4,5-g][1,4]oxazino[4,3-a]quinoline-5,5'-pyrimidine]-2',4',6'(3'h)-trione
etx0914; azd0914; zoliflodacin
EX-A2620
(4'r,6's,7's)-17'-fluoro-4',6'-dimethyl-13'-[(4s)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]spiro[1,3-diazinane-5,8'-5,15-dioxa-2,14-diazatetracyclo[8.7.0.02,7.012,16]heptadeca-1(17),10,12(16),13-tetraene]-2,4,6-trione
zoliflodacin(azd0914)
zoliflodacin (usan/inn)
D11726
gtpl10875
ext0914
ext-0914
azd 0914 - bio-x
Q27278240
MS-29053
azd0914etx0914
AC-35757
BA164192
azd 0914
r8u ,
DTXSID101028418

Research Excerpts

Overview

AZD0914 is a novel bacterial gyrase inhibitor that possesses potent in vitro activities against isolates with high-level resistance to ciprofloxacin and extended-spectrum cephalosporins. It is currently in clinical development for the treatment of N. difficile.

ExcerptReferenceRelevance
"AZD0914 is a new spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor with potent in vitro antibacterial activity against key Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae), fastidious Gram-negative (Haemophilus influenzae and Neisseria gonorrhoeae), atypical (Legionella pneumophila), and anaerobic (Clostridium difficile) bacterial species, including isolates with known resistance to fluoroquinolones. "( In vitro antibacterial activity of AZD0914, a new spiropyrimidinetrione DNA gyrase/topoisomerase inhibitor with potent activity against Gram-positive, fastidious Gram-Negative, and atypical bacteria.
Alm, RA; Basarab, GS; Bradford, PA; Giacobbe, RA; Huband, MD; Johnstone, MR; Kutschke, AC; Miller, PF; Mueller, JP; Otterson, LG; Patey, SA; Potter, ME, 2015)		2.14
"AZD0914 is a novel bacterial gyrase inhibitor that possesses potent in vitro activities against isolates with high-level resistance to ciprofloxacin and extended-spectrum cephalosporins, and it is currently in clinical development for the treatment of N."( Characterization of the novel DNA gyrase inhibitor AZD0914: low resistance potential and lack of cross-resistance in Neisseria gonorrhoeae.
Alm, RA; Gardner, H; Huband, MD; Kutschke, A; Lahiri, SD; Lewis, LA; McLaughlin, RE; Mueller, JP; Otterson, LG; Su, X; Whiteaker, JD, 2015)		1.39

Compound-Compound Interactions

ExcerptReferenceRelevance
" Zoliflodacin was evaluated alone or combined with ceftriaxone, cefixime, spectinomycin, gentamicin, tetracycline, cethromycin or sitafloxacin in chequerboard assays, time-kill curve analysis and selection-of-resistance studies."( In vitro antimicrobial combination testing of and evolution of resistance to the first-in-class spiropyrimidinetrione zoliflodacin combined with six therapeutically relevant antimicrobials for Neisseria gonorrhoeae.
Alirol, E; Drusano, G; Foerster, S; Golparian, D; Neely, M; Piddock, LJV; Unemo, M, 2019)		0.51
"Zoliflodacin alone or in combination with all six antimicrobials showed rapid growth inhibition against all examined strains."( In vitro antimicrobial combination testing of and evolution of resistance to the first-in-class spiropyrimidinetrione zoliflodacin combined with six therapeutically relevant antimicrobials for Neisseria gonorrhoeae.
Alirol, E; Drusano, G; Foerster, S; Golparian, D; Neely, M; Piddock, LJV; Unemo, M, 2019)		0.51
"Zoliflodacin, alone or in combination with sexually transmitted infection therapeutic antimicrobials, rapidly kills gonococci with infrequent resistance emergence."( In vitro antimicrobial combination testing of and evolution of resistance to the first-in-class spiropyrimidinetrione zoliflodacin combined with six therapeutically relevant antimicrobials for Neisseria gonorrhoeae.
Alirol, E; Drusano, G; Foerster, S; Golparian, D; Neely, M; Piddock, LJV; Unemo, M, 2019)		0.51

Dosage Studied

ExcerptRelevanceReference
" Dosing ETX0914 in human volunteers showed sufficient exposure and minimal adverse effects to expect a highly efficacious anti-gonorrhea therapy."( Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases.
Alm, RA; Barvian, K; Basarab, GS; Doig, P; Galullo, V; Gardner, H; Gowravaram, M; Huband, M; Kern, GH; Kimzey, A; Kutschke, A; Lahiri, SD; Lawrence, K; McNulty, J; Morningstar, M; Mueller, JP; Newman, JV; Perros, M; Schuck, VJ; Singh, R; Tommasi, R; Vishwanathan, K; Walkup, G, 2015)		0.42
" Increasing the dosage regimen can be applied to ceftriaxone and azithromycin, but the emergence of high-level resistance has already been reported."( New treatment options for infections caused by increasingly antimicrobial-resistant Neisseria gonorrhoeae.
Chong, Y; Lee, H; Lee, K, 2016)		0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA gyrase subunit BStaphylococcus aureusIC50 (µMol)4.30000.00401.50207.7000AID1909942
DNA gyrase subunit AStaphylococcus aureusIC50 (µMol)4.30000.00401.98397.7000AID1909942
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC50 (µMol)32.00000.01502.467610.0000AID1909946
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC50 (µMol)32.00000.01503.477310.0000AID1909946
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID1909942Inhibition of Staphylococcus aureus ATTC 25923 DNA gyrase2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1909951Antibacterial activity against Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph assessed as inhibition of bacterial growth incubated for 11 days2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724612Protein binding in human plasma assessed as unbound fraction at 10 uM measured after 16 hrs by LC-MS/MS based equilibrium dialysis method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909950Antibacterial activity against wild type Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 11 days2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724622Protein binding in rat plasma assessed as unbound fraction at 10 uM measured after 16 hrs by LC-MS/MS based equilibrium dialysis method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724623Plasma clearance in CD-1 mouse at 3 mg/kg, iv administered as 15 mins infusion by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724628Volume of distribution at steady state in Wistar Han rat at 3 mg/kg, iv administered as 15 mins infusion by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724614Antibacterial activity against methicillin sensitive Staphylococcus aureus ARC516 in presence of human serum by broth microdilution method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724625Unbound plasma clearance in CD-1 mouse at 3 mg/kg, iv administered as 15 mins infusion by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724631Oral bioavailability in CD-1 mouse at 10 mg/kg by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909946Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724613Antibacterial activity against methicillin sensitive Staphylococcus aureus ARC516 by broth microdilution method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724617Antibacterial activity against Escherichia coli ARC523 by broth microdilution method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909948Antibacterial activity against Staphylococcus aureus ATTC 25923 assessed as inhibition of bacterial growth measured after 8 days by Alamar blue reagent based broth microdilution method2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724626Unbound plasma clearance in Wistar Han rat at 3 mg/kg, iv administered as 15 mins infusion by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724630Half life in Wistar Han rat at 3 mg/kg, iv administered as 15 mins infusion by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909952Selectivity ratio of MIC50 for wild type Mycobacterium tuberculosis H37Rv to MIC50 for Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724641Antibacterial activity against methicillin sensitive Staphylococcus aureus ARC516 infected in CD-1 mouse neutropenic thigh infection model assessed as reduction in colony forming unit at 20 mg/kg, ip bid in presence of ABT2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724621Protein binding in mouse plasma assessed as unbound fraction at 10 uM measured after 16 hrs by LC-MS/MS based equilibrium dialysis method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724610n-octanol/phosphate buffer partition coefficient, log D of the compound at pH 7.4 measured after 1 hr by UV-LC/MS based shake flask method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724632Oral bioavailability in Wistar Han rat at 10 mg/kg by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909947Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth measured after 8 days by Alamar blue reagent based broth microdilution method2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724624Plasma clearance in Wistar Han rat at 3 mg/kg, iv administered as 15 mins infusion by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909953Selectivity ratio of MIC99 for wild type Mycobacterium tuberculosis H37Rv to MIC99 for Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724615Antibacterial activity against methicillin/quinolone-resistant Staphylococcus aureus ARC517 by broth microdilution method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909945Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1909943Kinetic solubility of compound at 200 uM incubated for 20 hrs by shake flask method based HPLC-DAD analysis2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724627Volume of distribution at steady state in CD-1 mouse at 3 mg/kg, iv administered as 15 mins infusion by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724640Antibacterial activity against methicillin sensitive Staphylococcus aureus ARC516 infected in CD-1 mouse neutropenic thigh infection model assessed as log reduction in colony forming unit at 100 mg/kg, ip bid in presence of ABT relative to initial treatme2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724616Ratio of MIC for antibacterial activity against methicillin/quinolone-resistant Staphylococcus aureus ARC517 to protein binding in human plasma assessed as unbound fraction2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909944n-Octanol/phosphate buffer partition coefficient, logD of the compound at pH 7.4 incubated for 3 hrs by shake flask method based HPLC-DAD analysis2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724611Solubility of the compound by high throughput solubility assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724609Inhibition of recombinant Escherichia coli DNA gyrase AB expressed in Escherichia coli BL21 (DE3) using relaxed pJT519 DNA as substrate preincubated for 20 mins followed by 5'-BODIPY-TMR-TTCTTCTTCT addition and measured after 1 hr by fluorescence anisotro2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1909949Antibacterial activity against Escherichia coli ATTC 25922 assessed as inhibition of bacterial growth measured after 8 days by Alamar blue reagent based broth microdilution method2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1724642Genotoxicity in mouse L5178Y cells using DAPI staining by microscopy based micronucleation assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
AID1724629Half life in CD-1 mouse at 3 mg/kg, iv administered as 15 mins infusion by LC-MS/MS analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (33)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's22 (66.67)24.3611
2020's11 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.09

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.09 (24.57)
Research Supply Index3.74 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (24.24%)5.53%
Reviews3 (9.09%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		3.2110isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
cefixime
Cefixime: A third-generation cephalosporin antibiotic that is stable to hydrolysis by beta-lactamases.. cefixime : A third-generation cephalosporin antibiotic bearing vinyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(carboxymethoxy)imino]acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. It is used in the treatment of gonorrhoea, tonsilitis, pharyngitis, bronchitis, and urinary tract infections.		2.1110
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.		4.6651aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		2.610monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		3.2110pyrrole;
secondary amine
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		3.2110indazole
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		12.13288isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		3.2110
spectinomycin
Spectinomycin: An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of GONORRHEA.. spectinomycin dihydrochloride : A hydrochloride obtained by combining spectinomycin with two molar equivalents of hydrochloric acid. An antibiotic that is active against gram-negative bacteria and used (as its pentahydrate) to treat gonorrhea.. spectinomycin : A pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis.		3.2310cyclic acetal;
cyclic hemiketal;
cyclic ketone;
pyranobenzodioxin;
secondary alcohol;
secondary amino compound		antibacterial drug;
antimicrobial agent;
bacterial metabolite
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		5.86311,2,3-triazole
oxazolidin-2-one
Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.		12.29299carbamate ester;
oxazolidinone		metabolite
garenoxacin
garenoxacin: a des-fluoro(6) quinolone with antibacterial activity. garenoxacin : A quinolinemonocarboxylic acid that is 1,4-dihydroquinoline-3-carboxylic acid that is substituted by a cyclopropyl group at position 1, an oxo group at position 4, a (1R)-1-methyl-2,3-dihydro-1H-isoindol-5-yl group at position 7, and a difluoromethoxy group at position 8.		3.2110aromatic ether;
cyclopropanes;
isoindoles;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic		antibacterial drug;
non-steroidal anti-inflammatory drug
levofloxacin
Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.		2.51209-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		2.4110aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		5.8761macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
abt 492
WQ 3034: structure in first source		3.2110
gemifloxacin
Gemifloxacin: A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.. gemifloxacin : A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position.		2.25101,8-naphthyridine derivative;
fluoroquinolone antibiotic;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
topoisomerase IV inhibitor
ro13-9904
Ceftriaxone: A broad-spectrum cephalosporin antibiotic and cefotaxime derivative with a very long half-life and high penetrability to meninges, eyes and inner ears.. ceftriaxone : A third-generation cephalosporin compound having 2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetylamino and [(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)sulfanyl]methyl side-groups.		7.2152
cem 101
solithromycin: an antibacterial fluoroketolide; structure in first source		5.8631
tetracycline
Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.		2.1310
kibdelomycin
kibdelomycin: an antibiotic that inhibits both gyrase and DNA topoisomerase IV; isolated from Kibdelosporangium; structure in first source		3.2110
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.4110cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.9521
Infections, Staphylococcal
[description not available]		04.331
Staphylococcal Infections
Infections with bacteria of the genus STAPHYLOCOCCUS.		04.331
Neisseria gonorrhoeae Infection
[description not available]		011.431810
Electrocardiogram QT Prolonged
[description not available]		07.7444
Gonorrhea
Acute infectious disease characterized by primary invasion of the urogenital tract. The etiologic agent, NEISSERIA GONORRHOEAE, was isolated by Neisser in 1879.		118.431810
Long QT Syndrome
A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.		07.7444
Sexually Transmitted Diseases
Diseases due to or propagated by sexual contact.		03.5911
Diseases of Pharynx
[description not available]		04.4811
Anorectal Diseases
[description not available]		04.4811
Male Genitourinary Diseases
[description not available]		04.4811
Female Genitourinary Diseases
[description not available]		04.4811
Rectal Diseases
Pathological developments in the RECTUM region of the large intestine (INTESTINE, LARGE).		04.4811
Urethritis
Inflammation involving the URETHRA. Similar to CYSTITIS, clinical symptoms range from vague discomfort to painful urination (DYSURIA), urethral discharge, or both.		02.5320
Infections, Neisseriaceae
[description not available]		03.0410
Sore Throat
[description not available]		03.0410
Pharyngitis
Inflammation of the throat (PHARYNX).		03.0410
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