Compounds > rufloxacin
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rufloxacin

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Description

Rulofloxacin is a synthetic fluoroquinolone antibiotic that exhibits a broad spectrum of activity against gram-positive and gram-negative bacteria, including multidrug-resistant strains. Its mechanism of action involves inhibiting bacterial DNA gyrase and topoisomerase IV, essential enzymes for DNA replication. Rulofloxacin is known for its excellent oral bioavailability and prolonged half-life, making it a promising candidate for treating infections. It has demonstrated efficacy in treating urinary tract infections, respiratory tract infections, and skin infections. Studies have explored its potential in treating tuberculosis and other resistant infections. Its unique chemical structure and pharmacological properties make it a subject of ongoing research for developing new and more effective antibiotics.'

rufloxacin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID58258
CHEMBL ID295619
CHEBI ID8909
SCHEMBL ID135502
MeSH IDM0167683

Synonyms (66)

Synonym
9-fluoro-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7h-[1,4]thiazino[2,3,4-ij]quinoline-6-carboxylic acid
HMS3393K22
AB00474020-20
mf 934
9-fluoro-2,3-dihydro-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acid
monos
MLS001424127
rufloxacin
101363-10-4
smr000466373
MLS000759502
rufloxacin (inn)
D02474
NCGC00074024-02
HMS2090N07
HMS2051K22
CHEMBL295619
chebi:8909 ,
nsc-759835
AKOS004120047
HMS3264M18
STK711124
rufloxacin [inn:ban]
9-fluoro-2,3-dihydro-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido(1,2,3-de)-1,4-benzothiazine-6-carboxylic acid
unii-y521xm2900
rufloxacinum [latin]
nsc 759835
y521xm2900 ,
rufloxacine [french]
rufloxacino [spanish]
BBL008945
nsc759835
pharmakon1600-01502335
rufloxacine
rufloxacinum
rufloxacino
c17h18fn3o3s
CCG-100908
FT-0631011
rufloxacin [mi]
rufloxacin [who-dd]
rufloxacin [inn]
AB00474020-18
SCHEMBL135502
NC00158
CS-4367
DTXSID6048412
HY-B0902
AB00474020_21
7-fluoro-6-(4-methylpiperazin-1-yl)-10-oxo-4-thia-1-azatricyclo[7.3.1.0^{5,13}]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
sr-01000612324
SR-01000612324-5
SR-01000612324-6
HMS3715P09
rkl10066
9-fluoro-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7h-[1,4]thiazino[2,3,4-ij]quinoline-6-carboxylic acid;9-fluoro-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7h-[1,4]thiazino[2,3,4-ij]quinoline-6-carboxylic acid
9-fluoro-10-(4-methylpiperazin-1-yl)-7-oxo-3,7-dihydro-2h-[1,4]thiazino[2,3,4-ij]quinoline-6-carboxylic acid
8-fluoro-9-(4-methyl-piperazin-1-yl)-6-oxo-2,3-dihydro-6h-1-thia-3a-aza-phenalene-5-carboxylic acid
Q3942356
DB13772
8-fluoro-9-(4-methylpiperazin-1-yl)-6-oxo-2,3-dihydro-6h-1-thia-3a-aza-phenalene-5-carboxylic acid
7h-pyrido[1,2,3-de]-1,4-benzothiazine-6-carboxylic acid, 9-fluoro-2,3-dihydro-10-(4-methyl-1-piperazinyl)-7-oxo-
7-fluoro-6-(4-methylpiperazin-1-yl)-10-oxo-4-thia-1-azatricyclo[7.3.1.0^{5,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
AS-79943
7-fluoro-6-(4-methylpiperazin-1-yl)-10-oxo-4-thia-1-azatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
gtpl12473

Research Excerpts

Overview

Rufloxacin is an antibacterial fluoroquinolone that exhibits UVA photosensitization properties. Once daily is a good alternative in the outpatient treatment of acute uncomplicated pyelonephritis.

ExcerptReferenceRelevance
"Rufloxacin (RFX) is an antibacterial fluoroquinolone that exhibits UVA photosensitization properties. "( Photosensitization induced by the antibacterial fluoroquinolone Rufloxacin leads to mutagenesis in yeast.
Angelin, AR; Catalfo, A; de Guidi, G; Sage, E; Serrentino, ME, 2010)		2.04
"Rufloxacin once daily is a good alternative in the outpatient treatment of acute uncomplicated pyelonephritis."( Rufloxacin once daily versus ciprofloxacin twice daily in the treatment of patients with acute uncomplicated pyelonephritis.
Bach, D; Cesana, M; Hübner, A; Plétan, Y; van Breukelen, G; van den Berg-Segers, A, 1995)		3.18
"Rufloxacin is a new once-daily antibacterial fluoroquinolone with a long half-life. "( Biliary excretion of rufloxacin in humans.
Cesana, M; Colturani, F; Faleschini, E; Franzini, P; Imbimbo, BP; Lombardi, F; Nicastro, G; Privitera, G; Tagliabue, G; Visconti, M, 1993)		2.05
"Rufloxacin is a new broad-spectrum fluoroquinolone antibacterial agent. "( Pharmacokinetics of rufloxacin in healthy volunteers after repeated oral doses.
Bonfiglio, G; Cesana, M; Cocuzza, CE; Gulisano, G; Imbimbo, BP; Mattina, R, 1991)		2.05
"Rufloxacin is a new long-acting, once-daily quinolone antibacterial agent. "( Inter- and intrasubject variabilities in the pharmacokinetics of rufloxacin after single oral administration to healthy volunteers.
Attardo-Parrinello, G; Broccali, G; Cesana, M; Crema, F; Imbimbo, BP, 1991)		1.96
"Rufloxacin (MF-934) is a new quinolone which shows in vitro antibacterial activity against E. "( Rufloxacin (MF-934): in vitro and in vivo antibacterial activity.
Colombrita, D; Foresti, I; Peroni, L; Pinsi, G; Pirali, F; Ravizzola, G; Turano, A, 1989)		3.16

Toxicity

ExcerptReferenceRelevance
" On the whole, the treatments were well tolerated, but some minor adverse events (mainly headache, insomnia, or abdominal discomfort) were reported for 7 subjects on abnormalities were detected in the laboratory examinations or in ocular function tests."( Multiple-dose pharmacokinetics and safety of rufloxacin in normal volunteers.
Cohen, GM; Griess, RS; Imbimbo, BP; Kisicki, JC; McCormack, RJ; Ott, CL; Troetel, WM, 1992)		0.54
" The only adverse event possibly related to the study drug was a case of transient mild tiredness and nervousness."( An open multicentre study on the efficacy and safety of rufloxacin in patients with chronic bacterial prostatitis.
Bischoff, W; Boerema, JB; Focht, J; Naber, KG, 1991)		0.53

Pharmacokinetics

The study investigated the ability of sub-MICs of rufloxacin, an orally absorbed monofluorinated quinolone with a long half-life (28 to 30 h) to interfere with the bacterial virulence parameters.

ExcerptReferenceRelevance
" The elimination half-life was 28."( Steady-state pharmacokinetics of rufloxacin in elderly patients with lower respiratory tract infections.
Cogo, R; Imbimbo, BP; Mattina, R; Rimoldi, R, 1992)		0.56
" An example of a pharmacokinetic study of rufloxacin and its metabolites in monkeys is shown."( High-performance liquid chromatography and preliminary pharmacokinetics of rufloxacin and its metabolites, N-desmethylrufloxacin and rufloxacinsulfoxide, in urine of rhesus monkey Macaca mulatta.
Imbimbo, BP; Peeters, A; van den Biggelaar-Martea, M; Vree, TB, 1992)		0.78
"The pharmacokinetic properties of rufloxacin, a new quinolone antibacterial agent, were evaluated in ten patients with lower respiratory tract infections."( Pharmacokinetics of rufloxacin once daily in patients with lower respiratory tract infections.
Albrici, A; Fioretti, M; Imbimbo, BP; Rimoldi, R, )		0.73
" absorption and a higher tissue/plasma concentration than that of other quinolones, are its interesting pharmacokinetic properties."( Ocular pharmacokinetics of rufloxacin a new fluoroquinolone antibiotic.
Brancato, R; Cremonesi, F; Ghione, M; Lombardo, N; Manitto, MP; Nucci, P, 1992)		0.58
" The drug was rapidly absorbed (absorption half-life 17 +/- 6 min in the 300 + 150 mg and 11 +/- 5 min in the 400 + 200 mg dose regimen group) and reached maximal serum concentrations (2."( Pharmacokinetics of rufloxacin in healthy volunteers after repeated oral doses.
Bonfiglio, G; Cesana, M; Cocuzza, CE; Gulisano, G; Imbimbo, BP; Mattina, R, 1991)		0.6
" The mean plasma elimination half-life was 28."( Pharmacokinetics and tissue penetration of rufloxacin, a long acting quinolone antimicrobial agent.
Andrews, JM; Imbimbo, BP; Johnson, J; O'Sullivan, N; Wise, R, 1991)		0.54
" There were considerable variations in the plasma concentration-time profiles among subjects; for example, the elimination half-life in plasma varied from 14."( Inter- and intrasubject variabilities in the pharmacokinetics of rufloxacin after single oral administration to healthy volunteers.
Attardo-Parrinello, G; Broccali, G; Cesana, M; Crema, F; Imbimbo, BP, 1991)		0.52
" A two-compartment model was used to calculate rufloxacin pharmacokinetic parameters."( Pharmacokinetics of rufloxacin in patients with impaired renal function.
Imbimbo, BP; Mant, TG; Morrison, PJ; Perry, G; Sacks, S; Wise, R; Woodcook, J, 1993)		0.87
" A one-compartment model applied to the high-performance liquid chromatography data was used to calculate the pharmacokinetic parameters of rufloxacin."( Multiple-dose pharmacokinetics of rufloxacin in patients with cirrhosis.
Granai, F; Imbimbo, BP; Triger, DR; Wise, R; Woodcock, J, 1993)		0.77
" In addition, urine levels, drug level/MIC ratio, and urine antibacterial activity 72 to 84 h after treatment initiation were determined in a subgroup of patients for pharmacodynamic assessment."( Single-dose rufloxacin versus 3-day norfloxacin treatment of uncomplicated cystitis: clinical evaluation and pharmacodynamic considerations.
Aguilar, L; Caffaratti, J; Dal-Ré, R; Dalet, F; Del Río, G, 1996)		0.67
" To compare the treatments, analysis of variance-based point estimates and 90% confidence intervals (given in parentheses) were calculated for the mean ratios of the pharmacokinetic parameters from the test (rufloxacin coadministration) over those from the reference (theophylline without rufloxacin) period."( Absence of effect of rufloxacin on theophylline pharmacokinetics in steady state.
Cesana, M; Fuhr, U; Kinzig-Schippers, M; Müller, C; Rietbrock, S; Sörgel, F; Staib, AH, 1998)		0.81
" The present study investigated the ability of sub-MICs of rufloxacin, an orally absorbed monofluorinated quinolone with a long half-life (28 to 30 h), to interfere with the bacterial virulence parameters of adhesiveness, hemagglutination, hydrophobicity, motility, and filamentation, as well as their interactions with host neutrophilic defenses such as phagocytosis, killing, and oxidative bursts."( Pharmacodynamic effects of subinhibitory concentrations of rufloxacin on bacterial virulence factors.
Braga, PC; Dal Sasso, M; Sala, MT, 1999)		0.79
"To evaluate the aqueous humor pharmacokinetics of rufloxacin in rabbits after topical administration of different formulations, and to individuate the ones showing the best pharmacokinetic profile."( Rufloxacin eyedrops: effect of different formulations on ocular pharmacokinetics in rabbits.
Burgalassi, S; Cappello, B; Chetoni, P; Iervolino, M; Monti, D; Saettone, MF, )		1.83
" The main pharmacokinetic parameters of RUF in the aqueous humor produced by the different formulations were calculated and statistical differences were assessed."( Rufloxacin eyedrops: effect of different formulations on ocular pharmacokinetics in rabbits.
Burgalassi, S; Cappello, B; Chetoni, P; Iervolino, M; Monti, D; Saettone, MF, )		1.57

Compound-Compound Interactions

Qianlie Jiedu Capsule combined with Rufloxacin is highly effective for CP by relieving pain and voiding symptoms,decreasing the leukocyte count in EPS and improving the life quality of the patients.

ExcerptReferenceRelevance
"The in vitro activity of rufloxacin, alone and in combination with its metabolite (MF 922) against common respiratory and urinary tract pathogens and anaerobes was assessed."( Bactericidal activity, morphological alterations, and synergistic interactions of rufloxacin, a new fluoroquinolone, alone and in combination with its N-desmethylate D derivative (MF 922).
Debbia, EA; Marchese, A; Pesce, A; Schito, GC, )		0.66
"Qianlie Jiedu Capsule combined with Rufloxacin is highly effective for CP by relieving pain and voiding symptoms,decreasing the leukocyte count in EPS and improving the life quality of the patients."( [Qianlie Jiedu capsule combined with rufloxacin for chronic prostatitis: a randomized double-blind controlled clinical trial].
Chen, YP; Fu, LJ; Lu, QM; Xu, JC, 2010)		0.91

Bioavailability

ExcerptReferenceRelevance
" In these animals the bioavailability is equal to 60%."( A new tricyclic fluoroquinolone, rufloxacin (MF-934), with interesting antibacterial and pharmacokinetic characteristics.
Cerretani, D; Cerri, D; Moltoni, L; Segre, G, 1988)		0.56
"The present study was designed to determine the effects of an antacid suspension containing magnesium hydroxide and aluminum hydroxide (30 ml of Maalox) on the oral bioavailability of rufloxacin (400 mg)."( Effects of magnesium-aluminum hydroxide antacid on absorption of rufloxacin.
Bargiggia, S; Bianchi Porro, G; Broccali, G; Dal Bo, L; Imbimbo, BP; Lazzaroni, M; Sangaletti, O, 1993)		0.72
" The overall results provide a clear example demonstrating how a bio-compatible trace element influences efficiently not only the bioavailability of a drug but also its molecular mechanism of photodegradation and photosensitization."( Effects of bio-compatible metal ions on rufloxacin photochemistry, photophysics and photosensitization: copper(II).
Belvedere, A; Catalfo, A; Cuquerella, MC; de Guidi, G; Miranda, MA; Scaiano, JC, 2010)		0.63

Dosage Studied

Rufloxacin may be used in routine clinical practice as a preoperative prophylactic antibiotic due to its low cost, its documented efficacy and its simple once daily dosage regimen. In patients with moderate renal failure, dosage adjustment of rufloxAcin is not needed.

ExcerptRelevanceReference
" Rufloxacin was administered orally at the dosage of 400 mg/die the first day; 200 mg/die the following 6 days or more."( [Treatment with rufloxacin of complicated urinary tract infections].
Caglio, G; Cantoni, L; Carmignani, G; Gusmitta, A; Maffezzini, M; Monti Bragadin, C; Samer, L, 1992)		1.54
" These findings indicate that sub-inhibitory concentrations of rufloxacin, which may be present in vivo in the mucosae in the troughs of the dosage cycle, significantly inhibit the adhesive properties of bacteria involved in mucosal colonization."( Favourable effects of sub-MIC rufloxacin concentrations in decreasing the pathogen-host cell adhesion.
Braga, PC; Piatti, G, )		0.66
"In a double-blind, randomized, multicenter study, the efficacy and safety of two dosage schedules of rufloxacin once daily were compared with those of amoxicillin three times a day in the treatment of 192 outpatients with exacerbations of chronic bronchitis."( Double-blind, comparative study of rufloxacin once daily versus amoxicillin three times a day in treatment of outpatients with exacerbations of chronic bronchitis.
Cesana, M; Focht, J; Klietmann, W; Rondel, RK, 1993)		0.78
" In patients with moderate renal failure, dosage adjustment of rufloxacin is not needed."( Pharmacokinetics of rufloxacin in patients with impaired renal function.
Imbimbo, BP; Mant, TG; Morrison, PJ; Perry, G; Sacks, S; Wise, R; Woodcook, J, 1993)		0.85
" Inaccurate estimations of ex vivo antibacterial activity of a suspected active metabolite (as with rufloxacin) when an adequate cutoff is not established may have dosing implications."( Suspicion of quinolone active metabolite following discrepancy between predicted and experimental urine bactericidal activities.
Aguilar, L; Costa, J; Dal-Ré, R; Giménez, MJ; Prieto, J, 1997)		0.51
" Results of the present study show that single dose oral rufloxacin may be used in routine clinical practice as a preoperative prophylactic antibiotic due to its low cost, its documented efficacy and its simple once daily dosage regimen."( Comparison of single preoperative oral rufloxacin versus perioperative ciprofloxacin as prophylactic agents in transurethral surgery.
Belgrano, E; Buttazzi, L; Ciampalini, S; Lissiani, A; Plaino, F; Raber, M; Savoca, G, 2000)		0.82
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (3)

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.
quinolone antibioticAn organonitrogen heterocyclic antibiotic whose structure contains a quinolone or quinolone-related skeleton.
fluoroquinolone antibioticAn organonitrogen heterocyclic antibiotic containing a quinolone (or quinolone-like) moiety and which have a fluorine atom attached to the central ring system.
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.18380.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency50.11875.623417.292931.6228AID485281
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.12510.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency7.94330.035520.977089.1251AID504332
mitogen-activated protein kinase 1Homo sapiens (human)Potency6.30960.039816.784239.8107AID1454
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency15.84890.00419.962528.1838AID2675
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency22.38720.251215.843239.8107AID504327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (127)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID29528Tissue levels determined 15 hr after peroral dose of 50 mg/kg in brain1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID16290Total clearance was determined in rat at 25 mg/kg os dosage;ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID584111Bacteriostatic activity against Escherichia coli K-12 DM41002010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID197873Minimal inhibitory concentration against Streptococcus aureus ATCC 6538 strain1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID15451Peak plasma concentration at a dose of 50 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID207117The compound was tested for in vitro antibacterial activity against Staphylococcus aureus MPR 5 (Gram positive) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID166957Lethal dose after single iv administration to rabbit was determined1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22640Urinary excretion for the compound was evaluated as percent dose excreted at 400 mg/kg oral dosage in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID65047Minimal inhibitory concentration against Escherichia coli ISF 432 strain1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID23790Half life period was determined for the compound at 50 mg/kg concentration, os route1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID15447Peak plasma concentration at a dose of 20 mg/kg, oral route in monkey (Macaca fascicularis) suspended in carboxymethyl cellulose (CMC);Range is between (5.5-6)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID198003Minimal inhibitory concentration against Shigella enteritidis strain1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID22641Urinary excretion for the compound was evaluated as percent dose excreted at 50 mg/kg os dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22419Volume of distribution at a dose of 100 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC);ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22637Urinary excretion for the compound was evaluated as percent dose excreted at 200 mg/kg oral dosage in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID198025Minimal inhibitory concentration against Streptococcus faecalis LEP strain1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID232333Ratio of AUC from os administration to AUC from ip administration at a dose of 25 mg/kg1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID30224Time taken for peak plasma concentration at a dose of 200 mg/kg, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID231323Ratio of tissue (liver) levels to plasma levels after 15 hr of treatment1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID206437In vitro antibacterial activity against clinical isolates of Staphylococcus aureus 18773 (gram-positive) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID14679Plasma concentration level in rat after 15 hours of oral administration at 50 mg/kg1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID27907Urinary clearance was determined at 100 mg/kg oral dosage in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID28622Plasma levels determined 1 hr after peroral dose of 50 mg/kg1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID27230Half life period was determined for the compound at 20 mg/kg concentration, oral route in dog(beagle)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID24239Time taken for peak plasma concentration at a dose of 25 mg/kg, ip route in rat suspended in carboxymethyl cellulose (CMC);ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID71902Lethal dose after single iv administration to female rat was determined1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID70947In vitro antibacterial activity against clinical isolates of Escherichia coli 15 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID23786Half life period was determined for the compound at 10 mg/kg concentration, intraperitoneal route1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID14380Urinary excretion in rat after 0-4 hours of oral administration at 50 mg/kg1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID151667Minimal inhibitory concentration against Pseudomonas aeruginosa ATCC 9027 strain1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID29530Tissue levels determined 1 hr after peroral dose of 50 mg/kg in heart1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID81946In vitro toxicity to C8166 (human CD4) cells.2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
6-Aminoquinolones as new potential anti-HIV agents.
AID163765The compound was tested for in vitro antibacterial activity against Pseudomonas aeruginosa ATCC 9027 (Gram negative) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID27904Total clearance in rat was determined at 50 mg/kg os dosage;ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID24048Time taken for peak plasma concentration at a dose of 100 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID231175Ratio of tissue (kidney) levels to plasma levels after 15 hr of treatment1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID15445Peak plasma concentration at a dose of 10 mg/kg, ip route in rat suspended in carboxymethyl cellulose (CMC);ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID23788Half life period was determined for the compound at 25 mg/kg concentration, intraperitoneal route1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID203051Antibacterial activity against Shigella enteritidis (Gram negative) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID26216Peak plasma concentration at a dose of 400 mg/kg, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID68201In vitro antibacterial activity against clinical isolates of Enterobacter cloacae 041 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID96264In vitro antibacterial activity against clinical isolates of Klebsiella pneumoniae-4 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22638Urinary excretion for the compound was evaluated as percent dose excreted at 25 mg/kg intraperitoneal dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID27905Total clearance was determined in rat at 100 mg/kg os dosage;ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22421Volume of distribution at a dose of 25 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC);ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID106819Lethal dose after single iv administration to male rat was determined1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID14382Urinary excretion in rat after 8-24 hours of oral administration at 50 mg/kg1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID20560Tissue levels determined 15 hr after peroral dose of 50 mg/kg in heart1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID20559Tissue levels for the compound was determined at 15 hr after peroral dose of 50 mg/kg in liver1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID23787Half life period was determined for the compound at 100 mg/kg concentration, os route1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID16288Urinary clearance was determined in rat at 100 mg/kg os dosage;ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID30412The compound was tested for in vitro antibacterial activity against Acinetobacter calcoaceticus OSMPV 113 (Gram negative) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID15449Peak plasma concentration at a dose of 25 mg/kg, ip route in rat suspended in carboxymethyl cellulose (CMC);ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22635Urinary excretion for the compound was evaluated as percent dose excreted at 10 mg/kg intraperitoneal dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID24049Time taken for peak plasma concentration at a dose of 20 mg/kg, oral route in dog(beagle) suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID70454The compound was tested for in vitro antibacterial activity against Escherichia coli ATCC 8739 (Gram negative) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID584112Bactericidal activity against Escherichia coli K-12 DM4100 after 2 hrs in presence of protein synthesis inhibitor chloramphenicol treated 10 mins before compound challenge2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID231322Ratio of tissue (kidney) levels to plasma levels after 1 hr of treatment1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID16294Urinary clearance was determined at 20 mg/kg oral dosage in dog(beagle);ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID24241Time taken for peak plasma concentration at a dose of 400 mg/kg, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID24046Time taken for peak plasma concentration at a dose of 10 mg/kg, ip route in rat suspended in carboxymethyl cellulose (CMC);ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID27842Urinary excretion for the compound was evaluated as percent dose excreted at 100 mg/kg oral dosage in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID21690Plasma levels of compound determined 15 hr after peroral dose of 50 mg/kg1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID151379Minimal inhibitory concentration against Proteus vulgaris CNUR6 strain1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID30223Time taken for peak plasma concentration at a dose of 20 mg/kg, oral route in monkey (Macaca fascicularis) suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID25690Half life period was determined for the compound at 20 mg/kg concentration, oral route in monkey (Macaca fascicularis)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID231171Ratio of tissue (brain) levels to plasma levels after 15 hr of treatment1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID27229Half life period was determined for the compound at 100 mg/kg concentration, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID16289Total clearance was determined in rat at 10 mg/kg intraperitoneal dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID26215Peak plasma concentration at a dose of 20 mg/kg, oral route in dog(beagle) suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID16293Urinary clearance was determined at 100 mg/kg oral dosage in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID24242Time taken for peak plasma concentration at a dose of 50 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID16292Urinary clearance was determined in rat at 25 mg/kg os dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID14381Urinary excretion in rat after 4-8 hours of oral administration at 50 mg/kg1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID66093Antibacterial activity against Enterobacter cloacae OMNFI 174 (Gram negative) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID206062Antibacterial activity against Staphylococcus epidermidis CPHL A2 (Gram positive) strain, activity is expressed as log2MIC.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID22422Volume of distribution at a dose of 50 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC);ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID584113Ratio of LD99 for Escherichia coli K-12 DM4100 to MIC for Escherichia coli K-12 DM41002010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID15450Peak plasma concentration at a dose of 25 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID163751Antibacterial activity against Providencia stuartii CNUR 5(Gram negative) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID231366Ratio of urinary excretion after os administration to ip administration1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID184638Lethal dose after single iv administration to rat was determined1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID27843Urinary excretion for the compound was evaluated as percent dose excreted at 20 mg/kg oral dosage in dog (beagle);Range is between (8-10).1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID165055In vitro antibacterial activity against clinical isolates of Pseudomonas aeruginosa 2437 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID15446Peak plasma concentration at a dose of 100 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID27231Half life period was determined for the compound at 400 mg/kg concentration, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID162914In vitro antibacterial activity against clinical isolates of Proteus morganii 27 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID231173Ratio of tissue (heart) levels to plasma levels after 15 hr of treatment1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID70456The compound was tested for in vitro antibacterial activity against Escherichia coli ISF 432 (Gram negative) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID207115The compound was tested for in vitro antibacterial activity against Staphylococcus aureus ATCC 6538 (Gram positive) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID22634Urinary excretion for the compound was evaluated as percent dose excreted at 100 mg/kg os dosage;ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID231172Ratio of tissue (brain) levels to plasma levels after 1 hr of treatment1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22639Urinary excretion for the compound was evaluated as percent dose excreted at 25 mg/kg os dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22420Volume of distribution at a dose of 25 mg/kg, intraperitoneal route in rat suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22636Urinary excretion for the compound was evaluated as percent dose excreted at 20 mg/kg oral dosage in monkey (macaca fascicularis); ND is defined as no-data.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID231174Ratio of tissue (heart) levels to plasma levels after 1 hr of treatment1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID29529Tissue levels determined 15 hr after peroral dose of 50 mg/kg in kidney1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID20561Tissue levels determined 1 hr after peroral dose of 50 mg/kg in brain1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID23789Half life period was determined for the compound at 25 mg/kg concentration, os route1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID63909Minimal inhibitory concentration against Enterobacter cloacae OMNFI174 strain1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID209400Antibacterial activity against Streptococcus faecalis LEP Br (Gram positive) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID14678Plasma concentration level in rat after 1 hour of oral administration at 50 mg/kg1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID15448Peak plasma concentration at a dose of 200 mg/kg, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID94208Antibacterial activity against Klebsiella pneumoniae ATCC 10031 (Gram negative) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID94299Minimal inhibitory concentration against Klebsiella pneumoniae ATCC 10031 strain1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID29531Tissue levels determined 1 hr after peroral dose of 50 mg/kg in liver1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID206059Antibacterial activity against Staphylococcus epidermidis HCF Berset C (Gram positive) strain.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Chemometric methodologies in a quantitative structure-activity relationship study: the antibacterial activity of 6-aminoquinolones.
AID27903Total clearance was determined in rat at 25 mg/kg intraperitoneal dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID24240Time taken for peak plasma concentration at a dose of 25 mg/kg, os route in rat suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID26214Peak plasma concentration at a dose of 100 mg/kg, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID25691Half life period was determined for the compound at 200 mg/kg concentration, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID24047Time taken for peak plasma concentration at a dose of 100 mg/kg, oral route in human1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID22418Volume of distribution at a dose of 10 mg/kg, intraperitoneal route in rat suspended in carboxymethyl cellulose (CMC)1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID81099In vitro antiviral activity against HIV-1 IIIB in C8166 (human CD4) cells.2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
6-Aminoquinolones as new potential anti-HIV agents.
AID20562Tissue levels determined 1 hr after peroral dose of 50 mg/kg in kidney1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID135327BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID134576Lethal dose after single iv administration to mouse was determined1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID231324Ratio of tissue (liver) levels to plasma levels after 1 hr of treatment1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID27906Urinary clearance was determined in rat at 25 mg/kg intraperitoneal dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID27908Urinary clearance was determined at 20 mg/kg oral dosage in monkey (macaca fascicularis).1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID14680Plasma concentration level in rat after 4 hours of oral administration at 50 mg/kg1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
AID16291Urinary clearance was determined in rat at 10 mg/kg intraperitoneal dosage1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID42400Selectivity index in HIV-1 infected C8166 (human CD4) cells.2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
6-Aminoquinolones as new potential anti-HIV agents.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (88)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906 (6.82)18.7374
1990's60 (68.18)18.2507
2000's14 (15.91)29.6817
2010's8 (9.09)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: 26.33

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 Index26.33 (24.57)
Research Supply Index4.81 (2.92)
Research Growth Index5.36 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (26.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials20 (19.61%)5.53%
Reviews2 (1.96%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other80 (78.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
formaldehyde
paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy		2.0310aldehyde;
one-carbon compound		allergen;
carcinogenic agent;
disinfectant;
EC 3.5.1.4 (amidase) inhibitor;
environmental contaminant;
Escherichia coli metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		210organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
theophylline
[no description available]		4.6232dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
astemizole
Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.		210benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
atenolol
Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.		210ethanolamines;
monocarboxylic acid amide;
propanolamine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
caffeine
[no description available]		8.7821purine alkaloid;
trimethylxanthine		adenosine A2A receptor antagonist;
adenosine receptor antagonist;
adjuvant;
central nervous system stimulant;
diuretic;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
environmental contaminant;
food additive;
fungal metabolite;
geroprotector;
human blood serum metabolite;
mouse metabolite;
mutagen;
plant metabolite;
psychotropic drug;
ryanodine receptor agonist;
xenobiotic
carbonyl cyanide m-chlorophenyl hydrazone
Carbonyl Cyanide m-Chlorophenyl Hydrazone: A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.. CCCP : A member of the class of monochlorobenzenes that is benzene substituted by 2-(1,3-dinitrilopropan-2-ylidene)hydrazinyl and chloro groups at positions 1 and 3, respectively. It is a mitochondrial depolarizing agent that induces reactive oxygen species mediated cell death.		210hydrazone;
monochlorobenzenes;
nitrile		antibacterial agent;
geroprotector;
ionophore
cetirizine
Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.		210ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines		anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
chlorpromazine
Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.		210organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
cimetidine
Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.		210aliphatic sulfide;
guanidines;
imidazoles;
nitrile		adjuvant;
analgesic;
anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
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.		7.25102aminoquinoline;
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
clobazam
Clobazam: A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.. clobazam : 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics.		2101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
GABA modulator
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		210clonidine;
imidazoline
deferiprone
Deferiprone: A pyridone derivative and iron chelator that is used in the treatment of IRON OVERLOAD in patients with THALASSEMIA.. deferiprone : A member of the class of 4-pyridones that is pyridin-4(1H)-one substituted at positions 1 and 2 by methyl groups and at position 3 by a hydroxy group. A lipid-soluble iron-chelator used for treatment of thalassaemia.		2104-pyridonesiron chelator;
protective agent
desipramine
Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.		210dibenzoazepine;
secondary amino compound		adrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
cholinergic antagonist;
drug allergen;
EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
serotonin uptake inhibitor
nordazepam
Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.. nordazepam : A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety.		2101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
GABA modulator;
human metabolite;
sedative
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		2101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
diphenhydramine
Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.		210ether;
tertiary amino compound		anti-allergic agent;
antidyskinesia agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
antitussive;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
oneirogen;
sedative
domperidone
Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.		210benzimidazoles;
heteroarylpiperidine		antiemetic;
dopaminergic antagonist
ebastine
[no description available]		210organic molecular entity
enoxacin
Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.. enoxacin : A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea.		2.4201,8-naphthyridine derivative;
amino acid;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-arylpiperazine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor
fenbufen
fenbufen: structure; RN given refers to parent cpd		6.99104-oxo monocarboxylic acid;
biphenyls		non-steroidal anti-inflammatory drug
fleroxacin
Fleroxacin: A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.. fleroxacin : A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria.		7.3920difluorobenzene;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
quinolines		antibacterial drug;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
furazolidone
Furazolidone: A nitrofuran derivative with antiprotozoal and antibacterial activity. Furazolidone acts by gradual inhibition of monoamine oxidase. (From Martindale, The Extra Pharmacopoeia, 30th ed, p514). furazolidone : A member of the class of oxazolidines that is 1,3-oxazolidin-2-one in which the hydrogen attached to the nitrogen is replaced by an N-{[(5-nitro-2-furyl)methylene]amino} group. It has antibacterial and antiprotozoal properties, and is used in the treatment of giardiasis and cholera.		8.4511nitrofuran antibiotic;
oxazolidines		antibacterial drug;
antiinfective agent;
antitrichomonal drug;
EC 1.4.3.4 (monoamine oxidase) inhibitor
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		210chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		210aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
imipramine
Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.		210dibenzoazepineadrenergic uptake inhibitor;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
lomefloxacin
lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.		3.5220fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antimicrobial agent;
antitubercular agent;
photosensitizing agent
loperamide
Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.		210monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol		anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
loratadine
Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.		210benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
mefloquine hydrochloride
[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4.		210organofluorine compound;
piperidines;
quinolines;
secondary alcohol
nalidixic acid
[no description available]		2101,8-naphthyridine derivative;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
DNA synthesis inhibitor
norfloxacin
Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase.		7.4795fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug;
DNA synthesis inhibitor;
environmental contaminant;
xenobiotic
ofloxacin
Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-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 : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.		6.191013-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
oxazepam
Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.		2101,4-benzodiazepinone;
organochlorine compound		anxiolytic drug;
environmental contaminant;
xenobiotic
pantoprazole
Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2.		3.4511aromatic ether;
benzimidazoles;
organofluorine compound;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
environmental contaminant;
xenobiotic
perphenazine
Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.		210N-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
organochlorine compound;
phenothiazines		antiemetic;
dopaminergic antagonist;
phenothiazine antipsychotic drug
pipemidic acid
Pipemidic Acid: Antimicrobial against Gram negative and some Gram positive bacteria. It is protein bound and concentrated in bile and urine and used for gastrointestinal, biliary, and urinary infections.. pipemidic acid : A pyridopyrimidine that is 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid substituted at position 2 by a piperazin-1-yl group and at position 8 by an ethyl group. A synthetic broad-spectrum antibacterial, it is used for treatment of gastrointestinal, biliary, and urinary infections.		1.9710amino acid;
monocarboxylic acid;
N-arylpiperazine;
pyridopyrimidine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor
pirenzepine
Pirenzepine: An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.		210pyridobenzodiazepineanti-ulcer drug;
antispasmodic drug;
muscarinic antagonist
promazine
Promazine: A phenothiazine with actions similar to CHLORPROMAZINE but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic.. promazine : A phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position.		210phenothiazines;
tertiary amine		antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
muscarinic antagonist;
phenothiazine antipsychotic drug;
serotonergic antagonist
pyrilamine
Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.. mepyramine : An ethylenediamine derivative that is ethylenediamine in which one of the amino nitrogens is substituted by two methyl groups and the remaining amino nitrogen is substituted by a 4-methoxybenzyl and a pyridin-2-yl group.		210aromatic ether;
ethylenediamine derivative		H1-receptor antagonist
ranitidine
[no description available]		210aralkylamine
gatifloxacin
Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.		2.0510N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
thioridazine
Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.		210phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
corticosterone
[no description available]		21011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone		human metabolite;
mouse metabolite
aldosterone
[no description available]		21011beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde		human metabolite;
mouse metabolite
chloramphenicol
Amphenicol: Chloramphenicol and its derivatives.		2.0510C-nitro compound;
carboxamide;
diol;
organochlorine compound		antibacterial drug;
antimicrobial agent;
Escherichia coli metabolite;
geroprotector;
Mycoplasma genitalium metabolite;
protein synthesis inhibitor
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		210aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
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.		11.197617monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		210amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
ampicillin
Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group.		1.9810beta-lactam antibiotic;
penicillin allergen;
penicillin		antibacterial drug
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		8.3711penicillin allergen;
penicillin		antibacterial drug
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		210azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
carbidopa
[no description available]		210catechols;
hydrate;
hydrazines;
monocarboxylic acid		antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
tiotidine
tiotidine: UD gives slightly different structure for this cpd; RN given refers to parent cpd; structure in first source		210thiazoles
pefloxacin
Pefloxacin: A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.. pefloxacin : A quinolone that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6 and 7 by ethyl, carboxy, fluorine, and 4-methylpiperazin-1-yl groups, respectively.		10.1831fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
antiinfective agent;
DNA synthesis inhibitor
temelastine
[no description available]		210pyrimidone
difloxacin
difloxacin: RN & structure given in first source. difloxacin : A quinolone that is pefloxacin in which the ethyl group at position 1 of the quinolone has been replaced by a p-fluorophenyl group. A broad-spectrum antibiotic effective against both Gram-positive and Gram-negative bacteria, it is used (usually as the monohydrochloride salt) for the treatment of bacterial infections in dogs.		210fluoroquinolone antibiotic;
monocarboxylic acid;
monofluorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
Mycoplasma genitalium metabolite
carmoxirole
carmoxirole : An indolecarboxylic acid that is indole-5-carboxylic acid bearing an additional 4-(4-phenyl-1,2,3,6-tetrahydropyridin-1-yl)butyl substituent at position 3. Selective, peripherally acting dopamine D2 receptor agonist. Modulates noradrenalin release and sympathetic activation. Displays antihypertensive properties in vivo.		210indolecarboxylic acid;
tertiary amino compound;
tetrahydropyridine		antihypertensive agent;
dopamine agonist;
platelet aggregation inhibitor
clinafloxacin
clinafloxacin: structure given in first source; RN given is for monoHCl		210quinolines
sparfloxacin
[no description available]		2.420fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
marbofloxacin
[no description available]		2.0510quinolines
carebastine
carebastine: active carboxylic acid metablite of ebastine; structure given in first source		210diarylmethane
pazufloxacin
[no description available]		2.0510quinolines
enrofloxacin
Enrofloxacin: A fluoroquinolone antibacterial and antimycoplasma agent that is used in veterinary practice.. enrofloxacin : A quinolinemonocarboxylic acid that is 1,4-dihydroquinoline-3-carboxylic acid substituted by an oxo group at position 4, a fluoro group at position 6, a cyclopropyl group at position 1 and a 4-ethylpiperazin-1-yl group at position 7. It is a veterinary antibacterial agent used for the treatment of pets.		210cyclopropanes;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone		antibacterial agent;
antimicrobial agent;
antineoplastic agent
rivastigmine
[no description available]		210carbamate ester;
tertiary amino compound		cholinergic drug;
EC 3.1.1.8 (cholinesterase) inhibitor;
neuroprotective agent
cp094
1,2-diethyl-3-hydroxypyridin-4-one: structure given in first source		210
sk&f 95282
zolantidine: structure given in first source		210piperidines
cp 41
CP 41: structure in first source		210
1-ethyl-2-methyl-3-hydroxypyridin-4-one
[no description available]		210
imipenem, anhydrous
Imipenem: Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with CILASTATIN, a renal dipeptidase inhibitor.. imipenem : A broad-spectrum, intravenous beta-lactam antibiotic of the carbapenem subgroup.		1.9810beta-lactam antibiotic allergen;
carbapenems;
zwitterion		antibacterial drug
levalbuterol
Levalbuterol: The R-isomer of albuterol.		210albuterol
n-desmethylrufloxacin
N-desmethylrufloxacin: structure given in first source; metabolite of rufloxacin found in urine of Rhesus monkey Macaca mulatta		7.8940
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.		5.22319-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.		2.0510aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
singlet oxygen
Singlet Oxygen: An excited state of molecular oxygen generated photochemically or chemically. Singlet oxygen reacts with a variety of biological molecules such as NUCLEIC ACIDS; PROTEINS; and LIPIDS; causing oxidative damages.		2.0510chalcogen;
monoatomic oxygen;
nonmetal atom		macronutrient
furprofen
furprofen: structure given in first source		6.9910
1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride
[no description available]		1.9910
asimadoline
asimadoline: structure in first source		210
roxindole
[no description available]		210indolesalpha-adrenergic antagonist;
serotonergic drug
trimethoprim, sulfamethoxazole drug combination
Trimethoprim, Sulfamethoxazole Drug Combination: A drug combination with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.. co-trimoxazole : A two-component mixture comprising trimethoprim and sulfamethoxazole.		1.9810
devazepide
Devazepide: A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.. devazepide : An indolecarboxamide obtained by formal condensation of the carboxy group of indole-2-carboxylic acid with the exocyclic amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one. A cholecystokinin antagonist used for treatment of gastrointestinal disorders.		2101,4-benzodiazepinone;
indolecarboxamide		antineoplastic agent;
apoptosis inducer;
cholecystokinin antagonist;
gastrointestinal drug
mf 5137
[no description available]		2.420
pd 135042
PD 135042: inhibits DNA gyrase and topoisomerase IV; structure in first source		2.0510
thiopental
Thiopental: A barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration.. thiopental : A barbiturate, the structure of which is that of 2-thiobarbituric acid substituted at C-5 by ethyl and sec-pentyl groups.		210barbituratesanticonvulsant;
drug allergen;
environmental contaminant;
intravenous anaesthetic;
sedative;
xenobiotic
u-50488
3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer: A non-peptide, kappa-opioid receptor agonist which has also been found to stimulate the release of adrenocorticotropin (ADRENOCORTICOTROPIC HORMONE) via the release of hypothalamic arginine vasopressin (ARGININE VASOPRESSIN) and CORTICOTROPIN-RELEASING HORMONE. (From J Pharmacol Exp Ther 1997;280(1):416-21). U50488 : A monocarboxylic acid amide obtained by formal condensation between the carboxy group of 3,4-dichlorophenylacetic acid and the secondary amino group of (1R,2R)-N-methyl-2-(pyrrolidin-1-yl)cyclohexanamine		210dichlorobenzene;
monocarboxylic acid amide;
N-alkylpyrrolidine		analgesic;
antitussive;
calcium channel blocker;
diuretic;
kappa-opioid receptor agonist
ici 199441
[no description available]		210acetamides
tamitinol
[no description available]		210
lupitidine
[no description available]		210
flupenthixol
cis-flupenthixol : A flupenthixol in which the double bond adopts a cis-configuration.		210flupenthixoldopaminergic antagonist
nalorphine
Nalorphine: A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.		210morphinane alkaloid
morphine
Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.		210morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
l 365260
L 365260: a CCK-B antagonist; structure given in first source; potent & selective CCK-B & gastrin receptor ligand; L 365260 and L 365346 are (R)- and (S)-stereoisomers, respectively		210benzodiazepine
levallorphan
Levallorphan: An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)		210morphinane alkaloid
naltrexone
Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.		210cyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound		antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
morphine-6-glucuronide
morphine-6-glucuronide: RN given refers to (5alpha,6alpha)-isomer		210morphinane alkaloid
aluminum hydroxide, magnesium hydroxide, drug combination
aluminum hydroxide, magnesium hydroxide, simethicone drug combination: antacid contains aluminum hydroxide, magnesium hydroxide and simethicone; mylanta II contains aluminum/magnesium hydroxide mixture		3.3711
gr 103545
[no description available]		210
l 365260
[no description available]		210
bismuth tripotassium dicitrate
bismuth tripotassium dicitrate: contains tripotassium di-citratobismuthate used in gastric & duodenal ulcer therapy; do not confuse with colloidal bismuth subnitrate		3.4511
colistin
Colistin: Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally.. colistin : A multi-component mixture comprising mostly of colistin A (R = Me) and B (R = H), with small amounts of colistin C and other polymyxins, produced by certain strains of Bacillus polymyxa var. colistinus. An antibiotic, it is used as its sulfate salt (for oral or topical use) or as the sodium salt of the N-methylsulfonic acid derivative (the injectable form) in the treatment of severe Gram-negative infections, partiularly those due to Pseudomonas aeruginosa.		1.9810
piroxicam
[no description available]		210benzothiazine;
monocarboxylic acid amide;
pyridines		analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
mobic
Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis.		2101,3-thiazoles;
benzothiazine;
monocarboxylic acid amide		analgesic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
mobiflex
tenoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It is also indicated for short term treatment of acute musculoskeletal disorders including strains, sprains and other soft-tissue injuries.		210heteroaryl hydroxy compound;
monocarboxylic acid amide;
pyridines;
thienothiazine		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
isoxicam
isoxicam : A monocarboxylic acid amide that is piroxicam in which the pyrid-2-yl group is replaced by a 5-methyl-1,2-oxazol-3-yl group. A non-steroidal anti-inflammatory drug, it was withdrawn from the market in the 1980s following its association with cases of Stevens-Johnson syndrome.		210benzothiazine;
isoxazoles;
monocarboxylic acid amide		antirheumatic drug;
non-steroidal anti-inflammatory drug
deoxyguanosine
[no description available]		7.7230purine 2'-deoxyribonucleoside;
purines 2'-deoxy-D-ribonucleoside		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
guanine
[no description available]		7.43202-aminopurines;
oxopurine;
purine nucleobase		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
8-hydroxyguanine
7,8-dihydro-8-oxoguanine: was substituted for guanine at G(8), G(9), G(14), or G(15) in the human telomeric oligonucleotide 5'-d[AGGGTTAG(8)G(9)GTT AG(14)G(15)GTTAGGGTGT]-3'. 7,8-dihydro-8-oxoguanine : An oxopurine that is guanine in which the hydrogen at position 8 is replaced by an oxo group and in which the nitrogens at positions 7 and 9 each bear a hydrogen.		2.0510oxopurine
8-hydroxy-2'-deoxyguanosine
8-Hydroxy-2'-Deoxyguanosine: Common oxidized form of deoxyguanosine in which C-8 position of guanine base has a carbonyl group.. 8-hydroxy-2'-deoxyguanosine : Guanosine substituted at the purine 8-position by a hydroxy group. It is used as a biomarker of oxidative DNA damage.		2.0210guanosinesbiomarker
biphenylylacetic acid
biphenylylacetic acid: metabolite of BHD 7538; RN given refers to cpd with unspecified locants for acetic acid moities		1.9910
ConditionIndicatedRelationship StrengthStudiesTrials
Anemia, Fanconi
[description not available]		02.1310
Fanconi Anemia
Congenital disorder affecting all bone marrow elements, resulting in ANEMIA; LEUKOPENIA; and THROMBOPENIA, and associated with cardiac, renal, and limb malformations as well as dermal pigmentary changes. Spontaneous CHROMOSOME BREAKAGE is a feature of this disease along with predisposition to LEUKEMIA. There are at least 7 complementation groups in Fanconi anemia: FANCA, FANCB, FANCC, FANCD1, FANCD2, FANCE, FANCF, FANCG, and FANCL. (from Online Mendelian Inheritance in Man, http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227650, August 20, 2004)		02.1310
Chronic Illness
[description not available]		05.2143
Acute Bacterial Prostatitis
[description not available]		04.3522
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		05.2143
Prostatitis
Infiltration of inflammatory cells into the parenchyma of PROSTATE. The subtypes are classified by their varied laboratory analysis, clinical presentation and response to treatment.		04.3522
Actinic Reticuloid Syndrome
[description not available]		02.0510
Infections, Helicobacter
[description not available]		03.4511
Helicobacter Infections
Infections with organisms of the genus HELICOBACTER, particularly, in humans, HELICOBACTER PYLORI. The clinical manifestations are focused in the stomach, usually the gastric mucosa and antrum, and the upper duodenum. This infection plays a major role in the pathogenesis of type B gastritis and peptic ulcer disease.		03.4511
Infections, Pseudomonas
[description not available]		02.0210
Infections, Staphylococcal
[description not available]		03.7921
Keratitis
Inflammation of the cornea.		07.0210
Pseudomonas Infections
Infections with bacteria of the genus PSEUDOMONAS.		02.0210
Staphylococcal Infections
Infections with bacteria of the genus STAPHYLOCOCCUS.		03.7921
Acute Disease
Disease having a short and relatively severe course.		04.7121
Cystitis
Inflammation of the URINARY BLADDER, either from bacterial or non-bacterial causes. Cystitis is usually associated with painful urination (dysuria), increased frequency, urgency, and suprapubic pain.		05.7742
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.6930
E coli Infections
[description not available]		05.3953
Necrotizing Pyelonephritis
[description not available]		03.3711
Escherichia coli Infections
Infections with bacteria of the species ESCHERICHIA COLI.		05.3953
Pyelonephritis
Inflammation of the KIDNEY involving the renal parenchyma (the NEPHRONS); KIDNEY PELVIS; and KIDNEY CALICES. It is characterized by ABDOMINAL PAIN; FEVER; NAUSEA; VOMITING; and occasionally DIARRHEA.		08.3711
Candida Infection
[description not available]		01.9810
Infections, Klebsiella
[description not available]		01.9810
Candidiasis
Infection with a fungus of the genus CANDIDA. It is usually a superficial infection of the moist areas of the body and is generally caused by CANDIDA ALBICANS. (Dorland, 27th ed)		01.9810
Klebsiella Infections
Infections with bacteria of the genus KLEBSIELLA.		01.9810
Bile Duct Obstruction, Extrahepatic
[description not available]		01.9810
Infections, Respiratory
[description not available]		02.8940
Respiratory Tract Infections
Invasion of the host RESPIRATORY SYSTEM by microorganisms, usually leading to pathological processes or diseases.		07.8940
Bacteroides Infections
Infections with bacteria of the genus BACTEROIDES.		01.9810
Bronchitis
Inflammation of the large airways in the lung including any part of the BRONCHI, from the PRIMARY BRONCHI to the TERTIARY BRONCHI.		08.7721
Chronic Kidney Failure
[description not available]		01.9810
Kidney Failure, Chronic
The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.		01.9810
Bacterial Disease
[description not available]		04.2841
Bacterial Infections
Infections by bacteria, general or unspecified.		16.2841
Urinary Tract Infections
Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA.		02.3920
Cirrhosis, Liver
[description not available]		03.7821
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		03.7821
Bacteriuria
The presence of bacteria in the urine which is normally bacteria-free. These bacteria are from the URINARY TRACT and are not contaminants of the surrounding tissues. Bacteriuria can be symptomatic or asymptomatic. Significant bacteriuria is an indicator of urinary tract infection.		03.3711
Recrudescence
[description not available]		03.3711
Benign Neoplasms
[description not available]		03.3711
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.3711
Neisseria gonorrhoeae Infection
[description not available]		03.3811
Gonorrhea
Acute infectious disease characterized by primary invasion of the urogenital tract. The etiologic agent, NEISSERIA GONORRHOEAE, was isolated by Neisser in 1879.		03.3811
Urethritis
Inflammation involving the URETHRA. Similar to CYSTITIS, clinical symptoms range from vague discomfort to painful urination (DYSURIA), urethral discharge, or both.		03.3811
Extravascular Hemolysis
[description not available]		0210
Hemolysis
The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.		0210
Pachymeningitis
[description not available]		0210
Meningitis
Inflammation of the coverings of the brain and/or spinal cord, which consist of the PIA MATER; ARACHNOID; and DURA MATER. Infections (viral, bacterial, and fungal) are the most common causes of this condition, but subarachnoid hemorrhage (HEMORRHAGES, SUBARACHNOID), chemical irritation (chemical MENINGITIS), granulomatous conditions, neoplastic conditions (CARCINOMATOUS MENINGITIS), and other inflammatory conditions may produce this syndrome. (From Joynt, Clinical Neurology, 1994, Ch24, p6)		0210
Primary Peritonitis
[description not available]		03.3911
Peritonitis
INFLAMMATION of the PERITONEUM lining the ABDOMINAL CAVITY as the result of infectious, autoimmune, or chemical processes. Primary peritonitis is due to infection of the PERITONEAL CAVITY via hematogenous or lymphatic spread and without intra-abdominal source. Secondary peritonitis arises from the ABDOMINAL CAVITY itself through RUPTURE or ABSCESS of intra-abdominal organs.		08.3911
Diathesis
[description not available]		01.9810
Salmonella Infections, Animal
Infections in animals with bacteria of the genus SALMONELLA.		01.9810
Infectious Skin Diseases
[description not available]		01.9710
Skin Diseases, Infectious
Skin diseases caused by bacteria, fungi, parasites, or viruses.		01.9710