Page last updated: 2024-12-08

u 100480

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

Description

U 100480: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID465951
CHEMBL ID288149
SCHEMBL ID2152517
MeSH IDM0257537

Synonyms (58)

Synonym
pnu 100480
n-[[(5s)-3-(3-fluoro-4-thiomorpholino-phenyl)-2-oxo-oxazolidin-5-yl]methyl]acetamide
nsc742407
oxazolidininone
n-{[3-(3-fluoro-4-(1,4-thiazaperhydroin-4-yl)phenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamide
u-100480
168828-58-8
sutezolid
pnu-100480
pf-02341272
u 100480
CHEMBL288149
n-[[(5s)-3-(3-fluoro-4-thiomorpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
acetamide, n-[[(5s)-3-[3-fluoro-4-(thiomorpholinyl)-phenyl]-2-oxo--5-oxazolidinyl]methyl]-
nsc-742407
pnu-480
pf-2341272
sutezolid (usan/inn)
D10167
SCHEMBL2152517
n-((3-(3-fluoro-4-(1,4-thiazaperhydroin-4-yl)phenyl)-2-oxo-1,3-oxazolidin-5-yl)methyl)acetamide
sutezolid [usan:inn]
unii-3a71182l8p
3a71182l8p ,
nsc 742407
NCGC00348189-01
sutezolid [usan]
sutezolid [who-dd]
u100480
n-({(5s)-3-[3-fluoro-4-(thiomorpholin-4-yl)phenyl]-2-oxooxazolidin-5-yl}methyl) acetamide
(s)-n-((3-(3-fluoro-4-thiomorpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide
acetamide, n-(((5s)-3-(3-fluoro-4-(4-thiomorpholinyl)phenyl)-2-oxo-5-oxazolidinyl) methyl)-
u-480
acetamide, n-((3-(3-fluoro-4-(4-thiomorpholinyl)phenyl)-2-oxo-5-oxazolidinyl)methyl)-, (s)-
sutezolid [inn]
(s)-n-[[3-[3-fluoro-4-(4-thiomorpholinyl)phenyl]-2-oxo-5-oxazolidinyl] methyl]acetamide
FNDDDNOJWPQCBZ-ZDUSSCGKSA-N
(s)-n-[[3-[3-fluoro-4-(4-thiomorpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide
pf 02341272
DTXSID20168611
HY-10392
CS-5568
n-{[(5s)-3-[3-fluoro-4-(thiomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamide
AKOS030238954
AS-74370
sutezolid, >=98% (hplc)
NCGC00348189-02
9en ,
mmv688756
sutezolid (pnu-100480)
DB11905
acetamide, n-[[(5s)-3-[3-fluoro-4-(4-thiomorpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-
bdbm50560041
gtpl12772
Q15427841
W13554
sr-05000022502
SR-05000022502-1

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" All doses were safe and well tolerated."( Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis.
Bedarida, G; Campbell, S; Jakubiec, W; Kumar, V; Ladutko, L; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, A; Wallis, RS; Zhu, T, 2011
)
0.37

Pharmacokinetics

ExcerptReferenceRelevance
" The relationships between the plasma concentrations of U-480 and U-603 and intracellular whole-blood bactericidal activity (WBA) in ex vivo cultures were examined using a direct competitive population pharmacokinetic (PK)/pharmacodynamic 4-parameter sigmoid model."( Population pharmacokinetic/pharmacodynamic analysis of the bactericidal activities of sutezolid (PNU-100480) and its major metabolite against intracellular Mycobacterium tuberculosis in ex vivo whole-blood cultures of patients with pulmonary tuberculosis.
Diacon, A; Friedrich, SO; Wallis, RS; Zhu, T, 2014
)
0.4

Compound-Compound Interactions

ExcerptReferenceRelevance
"Rifampin (RIF) plus clarithromycin (CLR) for 8 weeks is now the standard of care for Buruli ulcer (BU) treatment, but CLR may not be an ideal companion for rifamycins due to bidirectional drug-drug interactions."( Oxazolidinones Can Replace Clarithromycin in Combination with Rifampin in a Mouse Model of Buruli Ulcer.
Almeida, DV; Converse, PJ; Grosset, JH; Lee, J; Li, SY; Nuermberger, EL; Omansen, TF, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" PNU-100480 doses to 1000 mg were well absorbed and showed approximately proportional increases in exposures of parent and metabolites."( Pharmacokinetics and whole-blood bactericidal activity against Mycobacterium tuberculosis of single doses of PNU-100480 in healthy volunteers.
Campbell, S; Dimitrova, D; Friedland, G; Jakubiec, WM; Kumar, V; Ladutko, L; Li, X; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, AM; Wallis, RS, 2010
)
0.36
"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

ExcerptRelevanceReference
" A dose-response study was performed with PNU-100480 and linezolid (both at 25, 50, and 100 mg/kg of body weight)."( Activities of several novel oxazolidinones against Mycobacterium tuberculosis in a murine model.
Chase, S; Cynamon, MH; Klemens, SP; Sharpe, CA, 1999
)
0.3
" There were no hematologic or other safety signals during 28 days of dosing at 600 mg twice daily."( Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis.
Bedarida, G; Campbell, S; Jakubiec, W; Kumar, V; Ladutko, L; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, A; Wallis, RS; Zhu, T, 2011
)
0.37
" Model parameters were used to simulate in vivo activity after oral dosing with sutezolid at 600 mg twice a day (BID) and 1,200 mg once a day (QD)."( Population pharmacokinetic/pharmacodynamic analysis of the bactericidal activities of sutezolid (PNU-100480) and its major metabolite against intracellular Mycobacterium tuberculosis in ex vivo whole-blood cultures of patients with pulmonary tuberculosis.
Diacon, A; Friedrich, SO; Wallis, RS; Zhu, T, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency30.11160.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency30.11160.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency30.11160.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency30.11160.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency30.11160.01238.964839.8107AID1645842
[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)
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)13.00000.00002.37899.7700AID1721079
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50 (µMol)0.70000.00001.89149.5700AID1721080
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (60)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (27)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (59)

Assay IDTitleYearJournalArticle
AID1721018Stability in CD-1 mouse liver microsome at 1 uM measured after 30 mins in absence of NADPH by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID144888Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID143113In vitro anti-mycobacterial activity against ethambutol resistant Mycobacterium tuberculosis ATCC 35837 determined by the MTT method2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID319148Aqueous solubility of the compound2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID143873Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium avium complex (MAC) ATCC 496011996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID1654505Drug metabolism assessed as CYP3A4 (unknown origin)-mediated N-[[(5S)-3-[4-(1,1-dioxo-1,4-thiazinan-4-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-yl]methyl]acetamide metabolite formation2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Effective Application of Metabolite Profiling in Drug Design and Discovery.
AID1721020Antitubercular activity against linezolid-resistant Mycobacterium tuberculosis incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID144302Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium simiae1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID143127In vitro anti-mycobacterial activity against multiple sensitive strains of Mycobacterium tuberculosis at 0.50 ug/mL1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID144564In vitro anti-mycobacterial activity against Mycobacterium smegmatis was determined2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID1654506Drug metabolism assessed as FMO (unknown origin)-mediated N-[[(5S)-3-[4-(1,1-dioxo-1,4-thiazinan-4-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-yl]methyl]acetamide metabolite formation2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Effective Application of Metabolite Profiling in Drug Design and Discovery.
AID1721017Stability in CD-1 mouse liver microsome assessed as parent compound remaining at 1 uM measured after 30 mins in presence of NADPH by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1654504Drug metabolism assessed as FMO (unknown origin)-mediated N-[[(5S)-3-[3-fluoro-4-(1-oxidothiomorpholin-1-ium-4-yl)phenyl]-2-oxo-oxazolidin-5-yl]methyl]acetamide metabolite formation2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Effective Application of Metabolite Profiling in Drug Design and Discovery.
AID143124In vitro anti-mycobacterial activity against multiple resistant strains of Mycobacterium tuberculosis at 0.50 ug/mL1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID143875Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium avium complex by 90%1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID143437Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium xenopi1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID104797Cytotoxicity of compound against mock-infected MT-4 cells was evaluated by MTT assay2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID319147Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1721080Inhibition of recombinant human MAOB expressed in baculovirus infected insect cells using kynuramine as substrate measured after 20 mins by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1721019Antitubercular activity against Mycobacterium tuberculosis isolate 12525 incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1871982Antimycobacterial activity against Mycobacterium tuberculosis2022European journal of medicinal chemistry, Feb-05, Volume: 229Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance.
AID1659809Antimycobacterial activity against Mycobacterium tuberculosis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Molecule Property Analyses of Active Compounds for
AID143115In vitro anti-mycobacterial activity against pirazynamide resistant Mycobacterium tuberculosis ATCC 35828 determined by the MTT method2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID698994Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1883681Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID1721021Ratio of MIC for antitubercular activity against linezolid-resistant Mycobacterium tuberculosis to MIC for antitubercular activity against Mycobacterium tuberculosis H37Rv2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1721079Inhibition of recombinant human MAOA expressed in baculovirus infected insect cells using kynuramine as substrate measured after 20 mins by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID144016In vitro anti-mycobacterial activity against Mycobacterium fortuitum was determined2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID144294Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium malmoense1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID143110In vitro anti-mycobacterial activity against Mycobacterium tuberculosis ATCC 27294, determined by the MTT method2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID145301In vitro anti-mycobacterial activity against Mycobacterium tuberculosis C.I. 1104 was determined2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID143126In vitro anti-mycobacterial activity against multiple sensitive strains of Mycobacterium tuberculosis at 0.125 ug/mL1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID143699Compound was evaluated for in vitro anti-mycobacterial activity against MAC 1011996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID1721016Inhibition of mitochondrial protein synthesis in rat H9c2 cells measured after 5 days by ELISA2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID143123In vitro anti-mycobacterial activity against multiple resistant strains of Mycobacterium tuberculosis at 0.125 ug/mL1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID143111In vitro anti-mycobacterial activity against Mycobacterium tuberculosis C.I. 1104, determined by the MTT method2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID145303In vitro anti-mycobacterial activity against ethambutol resistant Mycobacterium tuberculosis ATCC 35837 was determined2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID143117In vitro anti-mycobacterial activity against streptomycin resistant Mycobacterium tuberculosis ATCC 35820 determined by the MTT method2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID145300In vitro anti-mycobacterial activity against Mycobacterium tuberculosis ATCC 27294 was determined2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID143872In vitro anti-mycobacterial activity against Mycobacterium smegmatis determined by the MTT method2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID1721015Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID143125In vitro anti-mycobacterial activity against multiple sensitive strains of Mycobacterium tuberculosis at 0.03 ug/mL1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID144566In vitro anti-mycobacterial activity against Mycobacterium smegmatis determined by the MTT method2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID143871In vitro anti-mycobacterial activity against Mycobacterium avium complex was determined2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID1721062Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID144014Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium fortuitum1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID145305In vitro anti-mycobacterial activity against pirazynamide resistant Mycobacterium tuberculosis ATCC 35828 was determined2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID698995Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID143104In vitro anti-mycobacterial activity against streptomycin resistant Mycobacterium tuberculosis ATCC 35820 was determined2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.
AID1162168Antitubercular activity against Mycobacterium tuberculosis assessed as growth inhibition2014European journal of medicinal chemistry, Oct-30, Volume: 86SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID143874Compound was evaluated for in vitro anti-mycobacterial activity against Mycobacterium avium complex by 50%1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
AID1721014Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1654503Drug metabolism assessed as CYP3A4 (unknown origin)-mediated N-[[(5S)-3-[3-fluoro-4-(1-oxidothiomorpholin-1-ium-4-yl)phenyl]-2-oxo-oxazolidin-5-yl]methyl]acetamide metabolite formation2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Effective Application of Metabolite Profiling in Drug Design and Discovery.
AID370056Antimycobacterial activity against Mycobacterium tuberculosis2005Antimicrobial agents and chemotherapy, Jun, Volume: 49, Issue:6
New small-molecule synthetic antimycobacterials.
AID1347160Primary screen NINDS Rhodamine 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.
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.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (9.30)18.2507
2000's4 (9.30)29.6817
2010's25 (58.14)24.3611
2020's10 (23.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (6.98%)5.53%
Reviews10 (23.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other30 (69.77%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]