Compounds > rwj-416457
Page last updated: 2024-11-12

rwj-416457

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Description

RWJ-416457: pyrrolopyrazolyl-substituted oxazolidinone; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID15984076
CHEMBL ID221877
SCHEMBL ID1888395
MeSH IDM0508089

Synonyms (13)

Synonym
rwj-416457
CHEMBL221877
SCHEMBL1888395
rwj 416457
y4n7w2yxf4 ,
474016-05-2
acetamide, n-(((5s)-3-(4-(2,6-dihydro-2-methylpyrrolo(3,4-c)pyrazol-5(4h)-yl)-3-fluorophenyl)-2-oxo-5-oxazolidinyl)methyl)-
unii-y4n7w2yxf4
(s)-n-((3-(3-fluoro-4-(2-methyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)acetamide
n-{(5s)-3-[4-(5,6-dihydro-2h,4h-2- methylpyrrolo[3,4-c]pyrazol-5-yl)-3-fluorophenyl]-2-oxo-1,3- oxazolidin-5-yl}acetamide
n-[[(5s)-3-[3-fluoro-4-(2-methyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
rwj416457
n-(((5s)-3-(4-(2,6-dihydro-2-methylpyrrolo(3,4-c)pyrazol-5(4h)-yl)-3-fluorophenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The goal of the present study was to develop a general pharmacokinetic (PK)-pharmacodynamic (PD) model that allows the characterization and comparison of the in vitro activities of oxazolidinones, determined in time-kill curve experiments, against MRSA."( Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
Abbanat, D; Barbour, A; Derendorf, H; Manitpisitkul, P; Sabarinath, SN; Schmidt, S; Sha, S, 2009)		0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (115)

Assay IDTitleYearJournalArticle
AID574085Ratio of fAUC (24 hrs) for penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected sc dosed mouse to MIC for penicillin-susceptible Streptococcus pneumoniae ATCC 63012009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283620Antimicrobial activity against Enterococcus faecium 31 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID278926Antibacterial activity against Moraxella catarrhalis2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283623Antimicrobial activity against Enterococcus faecium 16 with homozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID573889AUC (0 to 24 hrs) in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574083Ratio of fAUC (24 hrs) for community-associated methicillin-resistant Staphylococcus aureus OC8525 infected iv dosed mouse to MIC for community-associated methicillin-resistant Staphylococcus aureus OC85252009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283638Antimicrobial activity against Staphylococcus aureus ST/02/21212007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID278917Antibacterial activity against linezolid-susceptible Enterococcus faecium2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573886Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected in po dosed CF-1 mouse administered at 24 hrs post infection measured after 48 hrs relative to Linezolid2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283635Antimicrobial activity against Staphylococcus aureus RN4220 deltamutS with 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID278918Antibacterial activity against linezolid-resistant Enterococcus faecium2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574077Apparent oral clearance in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278909Antibacterial activity against vancomycin-intermediate methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278906Antibacterial activity against Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573882Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in SKH1 mouse assessed as log reduction in CFU/g skin up to 320 mg/kg/day, po administered post infection measured after 48 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278910Antibacterial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573877Bacteriostatic activity against methicillin-susceptible Staphylococcus aureus Smith ATCC 13709 infected in SKH1 mouse at 20 mg/kg/day, po administered post infection measured after 48 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278931Antibacterial activity against Enterococcus faecalis ATCC 51922 by time kill experiments2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574067fCmax in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573874Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected in iv dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573875Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith ATCC 13709 infected in SKH1 mouse assessed as log reduction in CFU/g skin at => 80 mg/kg/day, po administered post infection measured after 48 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278921Antibacterial activity against Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574065Cmax in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573865Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 after 16 to 20 hrs by broth microdilution method relative to Linezolid2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574066fCmax in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283633Antimicrobial activity against Staphylococcus aureus RN4220 with 23S rRNA G2447T mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID278908Antibacterial activity against methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283610Antimicrobial activity against Enterococcus faecalis 1 L2 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID278925Antibacterial activity against Haemophilus influenzae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574076Apparent oral clearance in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278920Antibacterial activity against macrolide-resistant Streptococcus pyogenes2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278915Antibacterial activity against linezolid-susceptible Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID562237Chemical stability of the compound assessed as compound degradation at 16 times MIC after 24 hrs by RP-HPLC analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
AID278911Antibacterial activity against community-acquired methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573891fAUC (0 to 24 hrs) in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574064Cmax in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283612Antimicrobial activity against Enterococcus faecalis 37 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID283616Antimicrobial activity against Enterococcus faecium 28 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID278912Antibacterial activity against coagulase-negative staphylococci2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278923Antibacterial activity against macrolide-resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278916Antibacterial activity against linezolid-resistant Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574086Ratio of fAUC (24 hrs) for penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected iv dosed mouse to MIC for penicillin-susceptible Streptococcus pneumoniae ATCC 63012009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278913Antibacterial activity against methicillin-susceptible coagulase-negative staphylococci2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278927Antibacterial activity against Legionella pneumophila2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574063Cmax in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278929Antibacterial activity against Chlamydophila pneumoniae in HEp2 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278924Antibacterial activity against fluoroquinolone-resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278928Antibacterial activity against Mycoplasma pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573860Antibacterial activity against Methicillin-susceptible Staphylococcus aureus ATCC 13709 after 16 to 20 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278922Antibacterial activity against penicillin-resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283622Antimicrobial activity against Enterococcus faecium 3 with homozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID573870Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in sc dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574082Ratio of fAUC (24 hrs) for community-associated methicillin-resistant Staphylococcus aureus OC8525 infected sc dosed mouse to MIC for community-associated methicillin-resistant Staphylococcus aureus OC85252009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573867Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in po dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283641Antimicrobial activity against Staphylococcus aureus RN4220 deltamutS2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID573866Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 13709 infected in po dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283632Antimicrobial activity against Staphylococcus aureus RN42202007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID574088Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as skin lesion size2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283614Antimicrobial activity against Enterococcus faecalis 9 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID278914Antibacterial activity against methicillin-resistant coagulase-negative staphylococci2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283634Antimicrobial activity against Staphylococcus aureus RN4220 with 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID278919Antibacterial activity against linezolid-resistant Enterococcus gallinarum2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283630Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4280-0258 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID573863Antibacterial activity against Methicillin-susceptible Staphylococcus aureus ATCC 13709 after 16 to 20 hrs by broth microdilution method relative to Linezolid2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574080Ratio of fAUC (24 hrs) for Methicillin-susceptible Staphylococcus aureus ATCC 13709 infected iv dosed mouse to MIC for Methicillin-susceptible Staphylococcus aureus ATCC 13702009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283611Antimicrobial activity against Enterococcus faecalis 25 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID574071Tmax in CF-1 mouse serum at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283609Antimicrobial activity against Enterococcus faecalis Ho 4450-0446 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID283639Antimicrobial activity against Staphylococcus aureus ST/02/2121 with 23S rRNA T2504C mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID283626Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4536-0367 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID283629Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4280-0257 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID574079Ratio of fAUC (24 hrs) for Methicillin-susceptible Staphylococcus aureus ATCC 13709 infected sc dosed mouse to MIC for Methicillin-susceptible Staphylococcus aureus ATCC 13702009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283628Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4536-0368 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID283617Antimicrobial activity against Enterococcus faecium 44 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID574078Ratio of fAUC (24 hrs) for Methicillin-susceptible Staphylococcus aureus ATCC 13709 infected po dosed mouse to MIC for Methicillin-susceptible Staphylococcus aureus ATCC 13702009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278907Antibacterial activity against methicillin-susceptible Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283613Antimicrobial activity against Enterococcus faecalis 45 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID562236Antibacterial activity against methicillin-resistant Staphylococcus aureus OC2878 assessed as inhibition of bacterial regrowth at 16 times MIC after 24 hrs by dynamic time kill study2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
AID573892fAUC (0 to 24 hrs) in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573887AUC (0 to 24 hrs) in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573890fAUC (0 to 24 hrs) in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574074Half life in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283640Antimicrobial activity against Staphylococcus aureus ST/02/2121 with 23S rRNA G2447T mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID283636Antimicrobial activity against Staphylococcus aureus RN4220 deltamutS revertant with 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID283619Antimicrobial activity against Enterococcus faecium 18 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID573862Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 after 16 to 20 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573861Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 after 16 to 20 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283618Antimicrobial activity against Enterococcus faecium Ho 4418-0062 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID573869Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 13709 infected in sc dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574068fCmax in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573872Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 13709 infected in iv dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574075Clearance in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283625Antimicrobial activity against Enterococcus faecium Ho 4136-00422007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID283615Antimicrobial activity against Enterococcus faecium Ho 5114-0276 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID574072Half life in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574070Tmax in CF-1 mouse serum at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574073Half life in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573873Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in iv dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283621Antimicrobial activity against Enterococcus faecium 2 L1 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID574087Antibacterial activity against Methicillin-susceptible Staphylococcus aureus assessed as skin lesion size2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573888AUC (0 to 24 hrs) in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573876Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith ATCC 13709 infected in SKH1 mouse assessed as log reduction in CFU/g skin at 5 mg/kg/day, po administered post infection measured after 48 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283637Antimicrobial activity against Staphylococcus aureus RN4220 deltamutS with 23S rRNA G2576U and A2503G mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID573871Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected in sc dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283624Antimicrobial activity against Enterococcus faecium 34 with homozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID573864Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 after 16 to 20 hrs by broth microdilution method relative to Linezolid2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID562234Antibacterial activity against methicillin-resistant Staphylococcus aureus OC2878 assessed as log reduction in bacterial count at 8 times MIC after 24 hrs by time kill study2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
AID574081Ratio of fAUC (24 hrs) for community-associated methicillin-resistant Staphylococcus aureus OC8525 infected po dosed mouse to MIC for community-associated methicillin-resistant Staphylococcus aureus OC85252009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283627Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4280-0256 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID574084Ratio of fAUC (24 hrs) for penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected po dosed mouse to MIC for penicillin-susceptible Streptococcus pneumoniae ATCC 63012009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID278930Antibacterial activity against methicillin-resistant Staphylococcus aureus OC 2878 by time kill experiments2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID573868Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected in po dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283631Antimicrobial activity against methicillin-resistant Staphylococcus aureus B2 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID562233Antibacterial activity against methicillin-resistant Staphylococcus aureus OC2878 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
AID573881Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in SKH1 mouse assessed as log reduction in CFU/g skin at 5 mg/kg/day, po administered post infection measured after 48 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (50.00)29.6817
2010's4 (50.00)24.3611
2020's0 (0.00)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 (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
pyrazinamide
pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.		2.1310monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug
penicillin g
Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group.		2.0310penicillin allergen;
penicillin		antibacterial drug;
drug allergen;
epitope
oxacillin
Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta.		2.0310penicillinantibacterial agent;
antibacterial drug
oxazoles
Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.		2.13101,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
azomycin
azomycin: RN given refers to parent cpd with specified locant; structure		2.1310C-nitro compound;
imidazoles		antitubercular agent
erythromycin
Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.		2.0310cyclic ketone;
erythromycin
vancomycin
Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.		2.4420glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite
oxazolidin-2-one
Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.		3.5680carbamate ester;
oxazolidinone		metabolite
levofloxacin
Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.		2.03109-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
azd2563
posizolid: an antitubercular agent; structure in first source		2.1310
linezolid
[no description available]		8.1550acetamides;
morpholines;
organofluorine compound;
oxazolidinone		antibacterial drug;
protein synthesis inhibitor
pa 824
pretomanid: nitroimidazopyran derived from 5-nitroimidazoles; a prodrug that requires activation by a bacterial F420-depedent glucose-6-phosphate dehydrogenase (Fgd) and nitroreductase to activate components that then inhibit bacterial mycolic acid and protein synthesis; structure in first source		2.1310
u 100480
U 100480: structure given in first source		2.1310
bedaquiline
bedaquiline: a diarylquinoline Antitubercular Agent. bedaquiline : A quinoline-based antimycobacterial drug used (as its fumarate salt) for the treatment of pulmonary multi-drug resistant tuberculosis by inhibition of ATP synthase, an enzyme essential for the replication of the mycobacteria.		2.1310aromatic ether;
naphthalenes;
organobromine compound;
quinolines;
tertiary alcohol;
tertiary amino compound		antitubercular agent;
ATP synthase inhibitor
tedizolid phosphate
tedizolid phosphate: a prodrug of DA-7157; structure in first source. tedizolid phosphate : A phosphate monoester resulting from the formal condensation of equimolar amounts of phosphoric acid with the hydroxy group of tedizolid . It is a prodrug of tedizolid, used for the treatment of acute bacterial skin infections caused by certain susceptible bacteria, including Staphylococcus aureus (including methicillin-resistant strains (MRSA) and methicillin-susceptible strains), various Streptococcus species, and Enterococcus faecalis.		2.1310carbamate ester;
organofluorine compound;
oxazolidinone;
phosphate monoester;
pyridines;
tetrazoles		antimicrobial agent;
prodrug;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.4820
Infections, Pneumococcal
[description not available]		02.0510
Infections, Staphylococcal
[description not available]		02.0510
Infections, Staphylococcal Skin
[description not available]		02.0510
Pneumococcal Infections
Infections with bacteria of the species STREPTOCOCCUS PNEUMONIAE.		02.0510
Staphylococcal Infections
Infections with bacteria of the genus STAPHYLOCOCCUS.		02.0510
Staphylococcal Skin Infections
Infections to the skin caused by bacteria of the genus STAPHYLOCOCCUS.		02.0510
Pulmonary Consumption
[description not available]		02.1310
Tuberculosis, Pulmonary
MYCOBACTERIUM infections of the lung.		02.1310