Page last updated: 2024-12-05

pipemidic acid

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

Description

Pipemidic acid is a synthetic antibacterial agent of the quinolone class. It is a potent inhibitor of bacterial DNA gyrase, an enzyme essential for DNA replication. Pipemidic acid has been used to treat urinary tract infections, but its use has been limited due to the development of resistance in bacteria. The compound's importance lies in its potential to serve as a scaffold for the development of novel antibacterial agents with improved activity and resistance profiles.'

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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

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. [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]

Cross-References

ID SourceID
PubMed CID4831
CHEMBL ID30116
CHEBI ID75250
SCHEMBL ID135557
MeSH IDM0016881

Synonyms (155)

Synonym
BIDD:GT0126
pipemidic
palin
pyrido(2,3-d)pyrimidine-6-carboxylic acid, 5,8-dihydro-8-ethyl-5-oxo-2-(1-piperazinyl)-
brn 0626575
acidum pipemidicum [inn-latin]
pipemid
pyrido(2,3-d)pyrimidine-6-carboxylic acid, 8-ethyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)-
acide pipemidique [inn-french]
deblaston
pipram
acido pipemidico [inn-spanish]
rb 1489
pipedac
acido pipemidico [spanish]
8-ethyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)pyrido(2,3-d)pyrimidine-6-carboxylic acid
einecs 257-530-2
uromidin
dolcol
1489 rb
acide ethyl-8 oxo-5 piperazinyl-2 dihydro-5,8 pyrido(2,3-d)pyrimidine-6 carboxylique [french]
BRD-K08999871-001-05-5
51940-44-4
8-ethyl-5-oxo-2-piperazin-1-yl-pyrido[2,3-d]pyrimidine-6-carboxylic acid
5,8-dihydro-8-ethyl-5-oxo-2-(1-piperazinyl)pyrido(2,3-d)pyrimidine-6-carboxylic acid
pipemidic acid
KBIO1_000651
DIVK1C_000651
8-ethyl-5-oxo-2-piperazin-1-yl-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
SPECTRUM_001387
nuril
BPBIO1_000786
cas-51940-44-4
NCGC00016866-01
IDI1_000651
SMP1_000242
SPECTRUM5_001214
NCGC00178314-01
NCGC00178314-02
BSPBIO_000714
AB00490004
BSPBIO_003073
PRESTWICK2_000897
NCGC00023999-04
NCGC00023999-03
smr000058711
MLS000028608 ,
KBIO3_002573
KBIOSS_001867
KBIO2_004435
KBIO2_007003
KBIO2_001867
KBIOGR_000630
SPBIO_001229
SPECTRUM2_001185
PRESTWICK1_000897
PRESTWICK0_000897
SPECTRUM3_001487
NINDS_000651
SPECTRUM4_000155
SPBIO_002923
SPECTRUM1502024
PRESTWICK3_000897
NCGC00016866-02
nsc-758160
pi-coli
uroval
chebi:75250 ,
uropimid
pipemidic acid anhydrous
pipeacid
pipemidate
memento 400
urosten
tractur
CHEMBL30116
filtrax
pipemidic acid hydrate
pipurin
pipemidic acid (inn)
D08379
nuril (tn)
HMS502A13
HMS1921F04
HMS1570D16
STK686262
8-ethyl-5-oxo-2-(piperazin-1-yl)-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
AKOS005599752
HMS2097D16
SR-01000000245-4
sr-01000000245
8-ethyl-5-oxo-2-piperazinyl-8-hydropyridino[2,3-d]pyrimidine-6-carboxylic acid
5,8-dihydro-8-ethyl-2-(1-piperazinyl)-5-oxopyrido[2,3-d]pyrimidine-6-carboxylic acid
7-(1-piperazinyl)-1-ethyl-4-oxo-1,4-dihydro-6,8-diazaquinoline-3-carboxylic acid
2-(1-piperazinyl)-5,8-dihydro-8-ethyl-5-oxopyrido[2,3-d]pyrimidine-6-carboxylic acid
2-(1-piperazinyl)-8-ethyl-5,8-dihydro-5-oxopyrido[2,3-d]pyrimidine-6-carboxylic acid
JOHZPMXAZQZXHR-UHFFFAOYSA-N
5,8-dihydro-8-ethyl-2-(1-piperazinyl)-5-oxopyrido-[2,3-d]pyrimidine-6-carboxylic acid
A828860
nsc758160
pharmakon1600-01502024
dtxsid3023479 ,
tox21_110655
dtxcid803479
8-ethyl-5-oxo-2-(piperazin-1-yl)-5h,8h-pyrido[2,3-d]pyrimidine-6-carboxylic acid
acide pipemidique
acidum pipemidicum
acido pipemidico
-ethyl-5-oxo-2-(piperazin-1-yl)-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
NCGC00016866-07
NCGC00016866-08
NCGC00016866-06
NCGC00016866-03
NCGC00016866-05
NCGC00016866-04
unii-lt12j5hvr8
lt12j5hvr8 ,
pipemidic acid [inn:ban:dcf]
acide ethyl-8 oxo-5 piperazinyl-2 dihydro-5,8 pyrido(2,3-d)pyrimidine-6 carboxylique
nsc 758160
ccris 8517
S5051
pipemidic acid [who-dd]
pipemidic acid [jan]
pipemidic acid [inn]
pipemidic acid [mart.]
pipemidic acid [mi]
CCG-220897
SCHEMBL135557
NCGC00016866-11
tox21_110655_1
CS-4838
P-6835
pipemidic acid, antibiotic for culture media use only
HY-B1210
OPERA_ID_1142
AB00052258_14
SR-01000000245-3
8-ethyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)pyrido[2,3-d]pyrimidine-6-carboxylic acid; pipemidic acid
SR-01000000245-2
SBI-0051703.P002
HMS3714D16
pipemidicacid
F15437
gtpl12774
8-ethyl-5-oxo-2-piperazin-1-ylpyrido[6,5-d]pyrimidine-6-carboxylic acid
DB13823
AS-47690
pipemidic acid,(s)
deblaston; pipram; uromidin; rb 1489; rb-1489; rb1489
BCP13633
Q754986
BRD-K08999871-001-13-9
pipemidic-acid
8-ethyl-5-oxo-2-piperazino-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid

Research Excerpts

Overview

Pipemidic acid (HPPA) is a quinolone antibacterial agent used mostly to treat gram-negative infections of the urinary tract. Its therapeutic use is limited because of its low solubility.

ExcerptReferenceRelevance
"Pipemidic acid (HPPA) is a quinolone antibacterial agent used mostly to treat gram-negative infections of the urinary tract, but its therapeutic use is limited because of its low solubility. "( A New Approach for Improving the Antibacterial and Tumor Cytotoxic Activities of Pipemidic Acid by Including It in Trimethyl-β-cyclodextrin.
Di Donato, C; Iacovino, R; Isidori, M; Lavorgna, M; Piscitelli, C; Russo, C, 2019
)
2.18
"Pipemidic acid is a bactericidal quinolone derivate, with a wide spectrum against gram positive and negative bacteria."( Treatment of acute urinary tract infection in children with pipemidic acid.
Gunawan, R; Kosnadi, L; Wastoro, D; Widayat, R; Yunanto, A,
)
1.09

Effects

ExcerptReferenceRelevance
"The pipemidic acid has shown to have activity against the stocks of B.coli and Proteus."( [In vitro antimicrobial activity of pipemidic acid on strains isolated from urine cultures of hospitalized and nonhospitalized subjects].
Ceddia, T; Marinucci, MC, 1980
)
1.02

Pharmacokinetics

The pharmacokinetic variables differed significantly between single doses of 10 and 30 mg of pipemidic acid/kg. The study used a new, sensitive, high-pressure liquid chromatography procedure.

ExcerptReferenceRelevance
"Quinolone is reported to interact with caffeine, often resulting in an increase both in the plasma half-life and AUC, a decrease in total plasma clearance, and little change in the absorption rate constant and maximum plasma level."( Pharmacokinetic determination of relative potency of quinolone inhibition of caffeine disposition.
Barnett, G; Carbó, M; de la Torre, R; Segura, J, 1990
)
0.28
" The pharmacokinetic variables differed significantly between single doses of 10 and 30 mg of pipemidic acid/kg."( Pharmacokinetics of pipemidic acid in chickens after single intravenous and oral dosings.
Anadón, A; Bringas, P; Díaz, MJ; Martínez-Larrañaga, MR; Vélez, C, 1990
)
0.82
"The pharmacokinetic profile of pipemidic acid was studied in two groups of young healthy volunteers by using a new, sensitive, high-pressure liquid chromatography procedure for quantitation of pipemidic acid in biological fluids."( Single- and multiple-dose pharmacokinetics of pipemidic acid in normal human volunteers.
Hänninen, U; Klinge, E; Männistö, PT; Mäntylä, R; Mattila, J, 1984
)
0.81

Bioavailability

The relative bioavailability of a single 500 mg tablet of pipemidic acid was good. The bioavailability was 39% at 10 mg of pipEMidic Acid/kg and 61% at 30 mg of PipemidIC acid/kg. In a study in middle-aged female volunteers, the relative bioavailable of a one 500 mg tablets of pip Emidicacid was good (39%)

ExcerptReferenceRelevance
"Quinolone is reported to interact with caffeine, often resulting in an increase both in the plasma half-life and AUC, a decrease in total plasma clearance, and little change in the absorption rate constant and maximum plasma level."( Pharmacokinetic determination of relative potency of quinolone inhibition of caffeine disposition.
Barnett, G; Carbó, M; de la Torre, R; Segura, J, 1990
)
0.28
" The bioavailability was 39% at 10 mg of pipemidic acid/kg and 61% at 30 mg of pipemidic acid/kg."( Pharmacokinetics of pipemidic acid in chickens after single intravenous and oral dosings.
Anadón, A; Bringas, P; Díaz, MJ; Martínez-Larrañaga, MR; Vélez, C, 1990
)
0.87
" In a study in middle-aged female volunteers, the relative bioavailability of a single 500 mg tablet of pipemidic acid was good."( Pharmacokinetics of pipemidic acid in healthy middle-aged volunteers and elderly patients with renal insufficiency.
Gordin, A; Hänninen, U; Männistö, P; Mäntylä, R; Niinistö, L; Salo, H; Solkinen, A, 1984
)
0.81
" Oral bioavailability was 93."( Single- and multiple-dose pharmacokinetics of pipemidic acid in normal human volunteers.
Hänninen, U; Klinge, E; Männistö, PT; Mäntylä, R; Mattila, J, 1984
)
0.53
" The use of β-CD allows an increase in the aqueous solubility of the drug, its bioavailability and then its bioactivity."( β-Cyclodextrin inclusion complex to improve physicochemical properties of pipemidic acid: characterization and bioactivity evaluation.
Caso, JV; Iacovino, R; Isernia, C; Isidori, M; Lavorgna, M; Malgieri, G; Rapuano, F; Russo, A; Russo, C; Russo, L, 2013
)
0.62
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The simultaneous determination of pipemidic acid and proline in human urine is of significance for quality control of the dosage and clinical study. The urine of men dosed orally with pipemdic acid, contained the metabolites acetylpipmidic, formylpimidic and oxopipemidics.

ExcerptRelevanceReference
"5 to 36 ml/mn the dosage was 11."( [Utilisation of pipemidic acid as antibiotic in patients with renal failure insufficiency. Kinetics of serum and urinary concentrations (author's transl)].
Kourilsky, O; Le Verge, R; Meyrier, A; Montay, G, 1979
)
0.61
" Daily dosage of LFLX and PPA was 600 mg and 2000 mg, respectively administered orally divided into 4 doses."( [Comparison of clinical efficacy of lomefloxacin (LFLX, NY-198) and pipemidic acid (PPA) in the treatment of infectious enteritis by a double-blind method. The Japan Research Committee of Lomefloxacin Research Group Enteritis].
Aoki, T; Kanehisa, N; Matsubara, Y; Murata, M; Nitta, Y; Sagara, H; Seo, T; Shimizu, N; Takizawa, Y; Tomizawa, I, 1989
)
0.51
" No clear dose-response curve was obtained."( Evaluation of the DNA-damaging and mutagenic activity of oxolinic and pipemidic acids by the granuloma pouch assay.
Maura, A; Pino, A, 1988
)
0.51
" Fecal samples were collected before, during, and after therapy from 23 adults who were undergoing treatment of urinary tract infections with pipemidic acid at a dosage of 200 mg orally four times daily for 10 days."( Selective decontamination of the digestive tract by pipemidic acid.
Boerema, HB; Muytjens, HL; van der Ros-van de Repe, J; van der Waaij, D; van Veldhuizen, GL; Welling, GW, 1983
)
0.72
" In addition, predictive calculations of serum levels reached after multiple dosing indicate that at an administration rate of 500 mg every 6 or preferably every 4 hours, Cinoxacin concentrations should be sufficiently high to be of interest in the treatment of systemic infections by sensitive organisms."( Comparative pharmacokinetic profiles of cinoxacin and pipemidic acid in humans.
Brogard, JM; Comte, F; Lavillaureix, J,
)
0.38
" Even in severely impaired kidney function urine concentrations averaged 230 micrograms/ml, which indicates that therapeutically sufficient concentrations can be maintained by regular administration of normal doses at unaltered dosage intervals."( [Studies on the pharmacokinetics of pipemidic acid in renal insufficiency (author's transl)].
Brühl, P; Gundlach, G; Köhler, T; Krasemann, C, 1981
)
0.54
" The urine of men dosed orally with pipemidic acid, contained the metabolites acetylpipemidic, formylpipemidic and oxopipemidic acids together with unchanged pipemidic acid."( Metabolites of pipemidic acid in human urine.
Kurobe, N; Nakamura, S; Shimizu, M, 1980
)
0.89
" The simultaneous determination of pipemidic acid and proline in human urine is of significance for quality control of the dosage and clinical study."( Simultaneous determination of proline and pipemidic acid in human urine by capillary electrophoresis with electrochemiluminescence detection.
Li, L; Su, M; Sun, H, 2010
)
0.9
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
DNA synthesis inhibitorAny substance that inhibits the synthesis of DNA.
[role 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]

Drug Classes (5)

ClassDescription
monocarboxylic acidAn oxoacid containing a single carboxy group.
amino acidA carboxylic acid containing one or more amino groups.
N-arylpiperazine
pyridopyrimidineAny organic heterobicyclic compound consisting of a pyridine ring ortho-fused at any position to a pyrimidine ring.
quinolone antibioticAn organonitrogen heterocyclic antibiotic whose structure contains a quinolone or quinolone-related skeleton.
[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)
USP1 protein, partialHomo sapiens (human)Potency39.81070.031637.5844354.8130AID504865
AR proteinHomo sapiens (human)Potency0.00060.000221.22318,912.5098AID743042
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency33.49150.003041.611522,387.1992AID1159552; AID1159553
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency7.75430.005612.367736.1254AID624032
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency6.30960.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
exodeoxyribonuclease V subunit RecBEscherichia coli str. K-12 substr. MG1655IC50 (µMol)0.10000.10000.10000.1000AID623918
exodeoxyribonuclease V subunit RecCEscherichia coli str. K-12 substr. MG1655IC50 (µMol)0.10000.10000.10000.1000AID623918
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (169)

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.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID563510Antimicrobial activity against cetylpyridinium chloride-resistant Serratia marcescens HMS011 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1600112Bactericidal activity against methicillin resistant Staphylococcus aureus 6347 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID563511Antimicrobial activity against cetylpyridinium chloride-resistant Serratia marcescens HMS011 harboring plasmid STV28 expressing sdeB gene by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1600114Bactericidal activity against methicillin resistant Staphylococcus epidermidis ATCC 13199 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1600110Bactericidal activity against Proteus vulgaris NCTC 4635 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID68965Median effective dose against Escherichia coli P-5101 causing systemic infections1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Pyridonecarboxylic acids as antibacterial agents. 2. Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent.
AID205854Minimum inhibitory concentration required against Staphylococcus aureus MRSA 494, methicillin resistant SA isolate2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus.
AID205856Minimum inhibitory concentration required against Staphylococcus aureus SA 1199B, constitutively overexpresses norA and harbors a topoisomerase IV A subunit substitution (A116E)2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus.
AID205713Minimum inhibitory concentration tested against vancomycin-insensitive SA (GISA 992 strain)2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus.
AID1600115Antibacterial activity against Streptococcus pneumoniae cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1546163Antimicrobial activity against Bacillus megaterium2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1600095Antibacterial activity against Staphylococcus aureus ATCC 6538 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1493766Antibacterial activity against Streptococcus pyogenes ATCC 19615 after 18 hrs by agar dilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates.
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.
AID1600106Bactericidal activity against Escherichia coli ATCC 8739 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID563504Antimicrobial activity against Serratia marcescens ATCC 13880 harboring plasmid STV29 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1600101Antibacterial activity against Enterococcus hirae ATCC 1052 cultured in BHI medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID205712Minimum inhibitory concentration tested against methicillin resistant Staphylococcus aureus 494 strain (MRSA 494)2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus.
AID1530021Antibacterial activity against glycopeptide-intermediate Staphylococcus aureus2019European journal of medicinal chemistry, Jan-01, Volume: 161Quinoline and quinolone dimers and their biological activities: An overview.
AID210022Antibacterial activity against Streptococcus pneumoniae (SV-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID116912Compound was tested for acute toxicity test with a single oral administration in mice and the median lethal dose as calculated.1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Pyridonecarboxylic acids as antibacterial agents. 2. Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent.
AID69782Antibacterial activity against Escherichia coli (H560)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID1600104Bactericidal activity against Bacillus subtilis ATCC 6633 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
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.
AID164385Antibacterial activity against Pseudomonas aeruginosa (UI-18)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID1530020Antibacterial activity against Staphylococcus aureus 1199B2019European journal of medicinal chemistry, Jan-01, Volume: 161Quinoline and quinolone dimers and their biological activities: An overview.
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.
AID1125372Antibacterial activity against Staphylococcus aureus RN4220 assessed as growth inhibition at 100 ug/ml after 16 hrs by spectrophotometric analysis2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID1600100Bactericidal activity against Staphylococcus epidermidis ATCC 14990 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1125383Antibacterial activity against Bacillus subtilis 168 assessed as growth inhibition at 40 ug/ml after 16 hrs by spectrophotometric analysis2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID563508Antimicrobial activity against cetylpyridinium chloride-sensitive Serratia marcescens 79 harboring plasmid STV29 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1600103Antibacterial activity against Bacillus subtilis ATCC 6633 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID164550In vitro antibacterial activity against Gram-negative Pseudomonas aeruginosa V-1.1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids.
AID1600094Lipophilicity, log k of the compound at 100 ug/ml by micellar electrokinetic chromatography2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1600118Bactericidal activity against Serratia marcescens ATCC 12795 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1600111Antibacterial activity against methicillin resistant Staphylococcus aureus 6347 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1600117Antibacterial activity against Serratia marcescens ATCC 12795 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID164220Median effective dose against Pseudomonas aeruginosa 12 causing systemic infections1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Pyridonecarboxylic acids as antibacterial agents. 2. Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent.
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.
AID563505Antimicrobial activity against cetylpyridinium chloride-resistant Serratia marcescens 01 harboring plasmid STV29 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID563503Antimicrobial activity against cetylpyridinium chloride-sensitive Serratia marcescens 79 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1546105Antimicrobial activity against Bacillus subtilis2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID1600096Bactericidal activity against Staphylococcus aureus ATCC 6538 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1600097Antibacterial activity against methicillin resistant Staphylococcus aureus N315 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID563512Antimicrobial activity against cetylpyridinium chloride-resistant Serratia marcescens 011 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1600105Antibacterial activity against Escherichia coli ATCC 8739 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1600109Antibacterial activity against Proteus vulgaris NCTC 4635 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1125373Antibacterial activity against Staphylococcus aureus RN4220 assessed as growth inhibition at 50 ug/ml after 16 hrs by spectrophotometric analysis2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID563509Antimicrobial activity against cetylpyridinium chloride-sensitive Serratia marcescens 79 harboring plasmid STV29 expressing hasF gene by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID69746Antibacterial activity against Escherichia coli NIHJ JC-21984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Pyridonecarboxylic acids as antibacterial agents. 2. Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1546111Antimicrobial activity against Salmonella typhimurium2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
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.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
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.
AID69784Antibacterial activity against Escherichia coli (vogel)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID1600099Antibacterial activity against Staphylococcus epidermidis ATCC 14990 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1493767Antibacterial activity against Salmonella typhi ATCC 19430 after 18 hrs by agar dilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates.
AID563500Antimicrobial activity against Serratia marcescens ATCC 13880 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1600108Bactericidal activity against Pseudomonas aeruginosa ATCC 9027 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1125387Antibacterial activity against Bacillus subtilis 168 assessed as growth inhibition at 20 ug/ml after 16 hrs by spectrophotometric analysis2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID1530018Antibacterial activity against Staphylococcus aureus 11992019European journal of medicinal chemistry, Jan-01, Volume: 161Quinoline and quinolone dimers and their biological activities: An overview.
AID205855Minimum inhibitory concentration required against Staphylococcus aureus SA 1199-3, laboratory-derived mutant of SA 1199 that inducibly overexpresses norA, no gyrase or topoisomerase IV mutations2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus.
AID1546175Antibacterial activity against Micrococcus luteus2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1493768Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by agar dilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates.
AID78707MIC at which cleaved DNA (linear) is observed at an intensity relative to oxolinic acid at 10 ug/mL by using Gyrase Induced DNA-Cleavage assay1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID207933In vitro antibacterial activity against Gram-positive, Staphylococcus aureus 209 P1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids.
AID205711Minimum inhibitory concentration tested against Staphylococcus aureus 1199B strain2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID95885Antibacterial activity against Klebsiella pneumonia (MGH-2)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID164236Antibacterial activity against Pseudomonas aeruginosa Tsuchijima1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Pyridonecarboxylic acids as antibacterial agents. 2. Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID70411In vitro for antibacterial activity against Gram-negative Escherichia coli NIJH JC-2.1980Journal of medicinal chemistry, Dec, Volume: 23, Issue:12
Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids.
AID563506Antimicrobial activity against cetylpyridinium chloride-sensitive Serratia marcescens 71 harboring plasmid STV29 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1600098Bactericidal activity against methicillin resistant Staphylococcus aureus N315 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1125394Antibacterial activity against Escherichia coli DH5alpha assessed as growth inhibition at 10 ug/ml after 16 hrs by spectrophotometric method2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID1546087Antimicrobial activity against Escherichia coli2019European journal of medicinal chemistry, Dec-15, Volume: 184Current scenario of tetrazole hybrids for antibacterial activity.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID563501Antimicrobial activity against cetylpyridinium chloride-resistant Serratia marcescens 01 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID207175Antibacterial activity against Staphylococcus aureus (H228)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID206858Antibacterial activity against Staphylococcus aureus 209PJC-11984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Pyridonecarboxylic acids as antibacterial agents. 2. Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent.
AID1125396Antibacterial activity against Escherichia coli DH5alpha assessed as growth inhibition at 2.5 ug/ml after 16 hrs by spectrophotometric method2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID78688Inhibitory concentration in supercoiling inhibition Escherichia coli DNA gyrase assay1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID1530019Antibacterial activity against Staphylococcus aureus 1199-32019European journal of medicinal chemistry, Jan-01, Volume: 161Quinoline and quinolone dimers and their biological activities: An overview.
AID1493765Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by agar dilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates.
AID1600113Antibacterial activity against methicillin resistant Staphylococcus epidermidis ATCC 13199 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1125367Antibacterial activity against Staphylococcus aureus RN4220 assessed as growth inhibition at 200 ug/ml after 16 hrs by spectrophotometric analysis2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1125388Antibacterial activity against Bacillus subtilis 168 assessed as growth inhibition at 10 ug/ml after 16 hrs by spectrophotometric analysis2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID205857Minimum inhibitory concentration required against Staphylococcus aureus SA-1199, wild-type isolate2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus.
AID1125395Antibacterial activity against Escherichia coli DH5alpha assessed as growth inhibition at 5 ug/ml after 16 hrs by spectrophotometric method2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID205710Minimum inhibitory concentration tested against Staphylococcus aureus 1199-3 strain2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus.
AID205853Minimum inhibitory concentration required against Staphylococcus aureus GISA 992, vancomycin-insensitive SA.2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus.
AID205709Minimum inhibitory concentration tested against Staphylococcus aureus 1199 strain2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus.
AID1493764Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 18 hrs by agar dilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates.
AID67545Activity against Enterobacter aerogenes2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Search compounds with antimicrobial activity by applying molecular topology to selected quinolones.
AID1600107Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID206570Median effective dose against Staphylococcus aureus 50774 causing systemic infections1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Pyridonecarboxylic acids as antibacterial agents. 2. Synthesis and structure-activity relationships of 1,6,7-trisubstituted 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids, including enoxacin, a new antibacterial agent.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID563502Antimicrobial activity against cetylpyridinium chloride-sensitive Serratia marcescens 71 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID563507Antimicrobial activity against cetylpyridinium chloride-sensitive Serratia marcescens 71 harboring plasmid STV29 expressing hasF gene by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID563513Antimicrobial activity against cetylpyridinium chloride-resistant Serratia marcescens 011 harboring plasmid STV28 expressing sdeB gene by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (230)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990133 (57.83)18.7374
1990's26 (11.30)18.2507
2000's26 (11.30)29.6817
2010's35 (15.22)24.3611
2020's10 (4.35)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 55.97

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index55.97 (24.57)
Research Supply Index5.71 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index92.24 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (55.97)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials32 (11.90%)5.53%
Reviews5 (1.86%)6.00%
Case Studies8 (2.97%)4.05%
Observational0 (0.00%)0.25%
Other224 (83.27%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]