Compounds > 3'-hydroxy-5'-(4-isobutylpiperazinyl)benzoxazinorifamycin
Page last updated: 2024-08-04 04:35:14

3'-hydroxy-5'-(4-isobutylpiperazinyl)benzoxazinorifamycin

Description

KRM 1648: structure in first source [MeSH]

Rifalazil : no description available [CHeBI]

Cross-References

ID SourceID
PubMed CID135431094
CHEMBL ID236297
SCHEMBL ID76007
CHEBI ID188526
MeSH IDM0188424

Synonyms (41)

Synonym
krm-1648 & mao-bushi-saishin-to
krm-1648 & mbst
2,7-(epoxy[1,11,13]pentadecatrienoimino)-6h-benzofuro[4,5-a]phenoxazine-1,6,15(2h)-trione, 25-(acetyloxy)-5,12,21,23-tetrahydroxy-27-methoxy-2,4,16,20,22,24,26-heptamethyl-10-[4-(2-methylpropyl)-1-piperazinyl]-, (2s,16z,18e,20s,21s,22r,23r,24r,25s,26r,27s
krm-1648 and yokuinin
D02550
rlz ,
rifalazil (usan/inn)
benzoxazinorifamycin
krm-1648 & scretory leukocyte protease inhibitor
129791-92-0
3'-hydroxy-5'-(4-isobutylpiperazinyl)benzoxazinorifamycin
krm 1648
krm-1648
[tetrahydroxy-(4-isobutylpiperazin-1-yl)-methoxy-heptamethyl-trioxo-[?]yl] acetate
rifamycin viii, 1',4-didehydro-1-deoxy-1,4-dihydro-3'-hydroxy-5'-[4-(2-methylpropyl)-1-piperazinyl]-1-oxo-
pa-1648
(2s,20s,21s,22r,23r,24r,25s,26r,27s)-5,12,21,23-tetrahydroxy-10-(4-isobutylpiperazin-1-yl)-27-methoxy-2,4,16,20,22,24,26-heptamethyl-1,6,15-trioxo-1,2-dihydro-6h-2,7-(epoxypentadeca[1,11,13]trienoimino)[1]benzofuro[4,5-a]phenoxazin-25-yl acetate
rifalazil
rifalazil [usan:inn]
(2s,16z,18e,20s,21s,22r,23r,24r,25s,26r,27s,28e)-5,12,21,23,25-pentahydroxy-10-(4-isobutyl-1-piperazinyl)-27-methoxy-2,4,16,20,22,24,26-heptamethyl-2,7-(epoxypentadeca(1,11,13)trienimino)-6h-benzofuro(4,5-a)phenoxazine-1(2h),6,15-trione 25-acetate
abi 1648
rifamycin viii, 1',4-didehydro-1-deoxy-1,4-dihydro-3'-hydroxy-5'-(4-(2-methylpropyl)-1-piperazinyl)-1-oxo-
CHEMBL236297
CHEBI:188526
[(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,6,15,17-tetrahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-30-[4-(2-methylpropyl)piperazin-1-yl]-23,32,37-trioxo-8,27,38-trioxa-24,34-diazahexacyclo[23.11.1.14,7.05,36.026,35.028,33]octatriaconta-1,3,
abi1648
abi-1648
unii-s1976te8qk
s1976te8qk ,
3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin
DB04934
SCHEMBL76007
rifalazil [mi]
1',4-didehydro-1-deoxy-1,4-dihydro-3'-hydroxy-5'-(4-(2-methylpropyl)-1-piperazinyl)-1-oxorifamycin viii
rifalazil [usan]
rifalazil [inn]
(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,15,17,32-tetrahydroxy-30-(4-isobutyl-1-piperazinyl)-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23,37-trioxo-8,27,38-trioxa-24,34-diazahexacyclo[23.11;.1.14,7.05,36.026,35.028,33]octatriaconta-1(36),2,4,9,
HY-105099
bdbm50491559
Q7333206
CS-0024983

Drug Classes (1)

ClassDescription
phenoxazine

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
DNA-directed RNA polymerase subunit betaEscherichia coli O127:H6 str. E2348/69IC50188.6667AID748177; AID748178; AID748179

Bioassays (46)

Assay IDTitleYearJournalArticle
AID1653515Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.1 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID669186Antitubercular activity against Mycobacterium tuberculosis H37Rv in aerobic conditions after 7 days by microplate-based alamar blue assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1879496Antibacterial activity against Clostridioides difficile ATCC 96892022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
ISSN: 1520-4804		Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID669178Inhibition of Mycobacterium tuberculosis wild type RNA polymerase by rolling circle transcription assay in the presence of sigmaA factor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1653513Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.025 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID1653516Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.2 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID1653394Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.05 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID1879497Antibacterial activity against Helicobacter pylori ATCC 7003922022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
ISSN: 1520-4804		Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID669180Inhibition of Mycobacterium tuberculosis RNA polymerase S450L mutant by rolling circle transcription assay in the presence of sigmaA factor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1653397Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.05 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID669197Metabolic stability in mouse microsomes assessed as compound remaining after 30 mins2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID301526Antibacterial activity against rifamycin-sensitive Staphylococcus aureus CB190 ATCC 292132007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
ISSN: 0960-894X		Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins.
AID1879495Antibacterial activity against Staphylococcus aureus ATCC 292132022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
ISSN: 1520-4804		Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1653514Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.05 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID1065392Half life in human at 25 mg, po administered through fat rich diet2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
ISSN: 1520-4804		Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties?
AID669191Activation of PXR in human DPX2 cells at 100 uM after 24 hrs by luciferase reporter gene assay relative to control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1653396Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.1 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID341089Antimicrobial activity against Clostridium difficile clinical isolates by agar dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
ISSN: 0066-4804		In vitro activities of 15 antimicrobial agents against 110 toxigenic clostridium difficile clinical isolates collected from 1983 to 2004.
AID1653510Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.2 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID669190Activation of PXR in human DPX2 cells at <100 uM after 24 hrs by luciferase reporter gene assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1653509Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.1 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID1653522Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.2 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID748179Inhibition of rifamycin-resistant Escherichia coli RNA polymerase D516V mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
ISSN: 1520-4804		X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID748180Inhibition of wild type Escherichia coli RNA polymerase after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
ISSN: 1520-4804		X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID669198Metabolic stability in human microsomes assessed as compound remaining after 30 mins2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID669608Half life in human2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID669199Half life in mouse microsomes2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID748178Inhibition of rifamycin-resistant Escherichia coli RNA polymerase H526Y mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
ISSN: 1520-4804		X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID1653395Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.025 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID669179Inhibition of Mycobacterium tuberculosis RNA polymerase D435V mutant by rolling circle transcription assay in the presence of sigmaA factor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID520287Antimicrobial activity against Chlamydia pneumoniae AR39 infected in C57BL/6J mouse at 1 mg/kg, ip assessed as bacterial load measured on day 10 post infection relative to control2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
ISSN: 1098-6596		Efficacy of benzoxazinorifamycins in a mouse model of Chlamydia pneumoniae lung infection.
AID1653393Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.025 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID669187Antitubercular activity against Mycobacterium tuberculosis H37Rv in anaerobic conditions after 11 days by luminescnece-based low-oxygen recovery assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1653521Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.1 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID1653519Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.025 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID669192Cytotoxicity against human DPX2 cells expressing PXR assessed as decrease in cell viability at 100 uM after 24 hrs relative to control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID301527Antibacterial activity against rifamycin-resistance Staphylococcus aureus CB3722007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
ISSN: 0960-894X		Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins.
AID301528Antibacterial activity against rifamycin-resistance Staphylococcus aureus CB3702007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
ISSN: 0960-894X		Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins.
AID1653390Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.2 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID748177Inhibition of rifamycin-resistant Escherichia coli RNA polymerase S531L mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
ISSN: 1520-4804		X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID669176Inhibition of Mycobacterium tuberculosis wild type RNA polymerase by rolling circle transcription assay in the absence of sigmaA factor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID520288Antimicrobial activity against Chlamydia pneumoniae AR39 infected in C57BL/6J mouse at 3 mg/kg, ip assessed as bacterial load measured on day 10 post infection relative to control2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
ISSN: 1098-6596		Efficacy of benzoxazinorifamycins in a mouse model of Chlamydia pneumoniae lung infection.
AID1653520Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.05 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
ISSN: 1464-3391		Insights of synthetic analogues of anti-leprosy agents.
AID520286Antimicrobial activity against Chlamydia pneumoniae TW-183 after 72 hrs by twofold dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
ISSN: 1098-6596		Efficacy of benzoxazinorifamycins in a mouse model of Chlamydia pneumoniae lung infection.
AID669177Inhibition of Mycobacterium tuberculosis RNA polymerase H445Y mutant by rolling circle transcription assay in the presence of sigmaA factor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID669200Half life in human microsomes2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
ISSN: 1520-4804		Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.

Research

Studies (122)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's65 (53.28)18.2507
2000's46 (37.70)29.6817
2010's6 (4.92)24.3611
2020's5 (4.10)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (7.32%)5.53%
Reviews14 (11.38%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other100 (81.30%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
ethoxyresorufin
0
phenoxazine00low000000
resazurin
0
phenoxazine00low000000
phenoxazine
0
phenoxazineferroptosis inhibitor;
radical scavenger		00low000000
resorufin
0
phenoxazine00low000000
3-aminophenoxazone
0
phenoxazine00low000000
oxazine 1
0
organic cation;
phenoxazine		fluorochrome00low000000
cinnabarinic acid
0
phenoxazine00low000000
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
pyrazinamide
1
monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug		201920195.0low000010
ciprofloxacin
1
aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic		201920195.0low000010
clofazimine
1
monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug		201920195.0low000010
dapsone
1
substituted aniline;
sulfone		anti-inflammatory drug;
antiinfective agent;
antimalarial;
leprostatic drug		201920195.0low000010
isoniazid
2
carbohydrazideantitubercular agent;
drug allergen		201220198.5low000020
metronidazole
2
C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic		200720229.5low000101
ofloxacin
1
3-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline		201920195.0low000010
omeprazole
1
aromatic ether;
benzimidazoles;
pyridines;
sulfoxide		202220222.0low000001
aminosalicylic acid
1
aminobenzoic acid;
phenols		antitubercular agent201920195.0low000010
pyrimethamine
1
aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor		201920195.0low000010
gatifloxacin
1
N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor		2007200717.0low000100
thalidomide
1
phthalimides;
piperidones		201920195.0low000010
tinidazole
1
imidazolesantiamoebic agent;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug		2007200717.0low000100
trimethoprim
1
aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic		201920195.0low000010
chloramphenicol
1
C-nitro compound;
carboxamide;
diol;
organochlorine compound		antibacterial drug;
antimicrobial agent;
Escherichia coli metabolite;
geroprotector;
Mycoplasma genitalium metabolite;
protein synthesis inhibitor		201920195.0low000010
kanamycin a
1
kanamycinsbacterial metabolite201920195.0low000010
acedapsone
1
acetamides;
anilide;
secondary carboxamide;
sulfone		antimalarial;
antimicrobial drug		201920195.0low000010
bis(4-hydroxyphenyl)sulfone
1
bisphenol;
sulfone		endocrine disruptor;
metabolite		201920195.0low000010
4,4'-diaminodiphenylmethane
1
aromatic amineallergen;
carcinogenic agent		201920195.0low000010
4,4'-thiodianiline
1
substituted aniline201920195.0low000010
monoacetyldapsone
1
acetamides;
anilide;
secondary carboxamide;
sulfone		201920195.0low000010
ethambutol
1
ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic		201920195.0low000010
vancomycin
2
glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite		200720229.5low000101
streptomycin
2
antibiotic antifungal drug;
antibiotic fungicide;
streptomycins		antibacterial drug;
antifungal agrochemical;
antimicrobial agent;
antimicrobial drug;
bacterial metabolite;
protein synthesis inhibitor		201220198.5low000020
tobramycin
1
amino cyclitol glycosideantibacterial agent;
antimicrobial agent;
toxin		201920195.0low000010
amikacin
1
alpha-D-glucoside;
amino cyclitol glycoside;
aminoglycoside;
carboxamide		antibacterial drug;
antimicrobial agent;
nephrotoxin		201920195.0low000010
nitazoxanide
1
benzamides;
carboxylic ester		2007200717.0low000100
4-amino-4'-hydroxylaminodiphenylsulfone
1
sulfonic acid derivative201920195.0low000010
acediasulfone
1
alpha-amino acid201920195.0medium000010
brodimoprim
1
aminopyrimidine;
bromobenzenes;
methoxybenzenes		antibacterial drug;
antiinfective agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor		201920195.0low000010
epiroprim
1
201920195.0low000010
gentamicin c1a
1
gentamycin C201920195.0low000010
doripenem
1
carbapenems2007200717.0low000100
4-nitro-4'-aminodiphenyl sulfone
1
201920195.0low000010
clarithromycin
1
macrolide antibioticantibacterial drug;
environmental contaminant;
protein synthesis inhibitor;
xenobiotic		202220222.0low000001
imipenem, anhydrous
1
beta-lactam antibiotic allergen;
carbapenems;
zwitterion		antibacterial drug201920195.0low000010
methotrexate
1
dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent		201920195.0low000010
levofloxacin
2
9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor		2007201911.0low000110
moxifloxacin
2
aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug2007201214.5low000110
aminopterin
1
dicarboxylic acidEC 1.5.1.3 (dihydrofolate reductase) inhibitor;
mutagen		201920195.0low000010
tizoxanide
1
salicylamides2007200717.0low000100
meropenem
1
alpha,beta-unsaturated monocarboxylic acid;
carbapenemcarboxylic acid;
organic sulfide;
pyrrolidinecarboxamide		antibacterial agent;
antibacterial drug;
drug allergen		2007200717.0low000100
tacrolimus
1
macrolide lactambacterial metabolite;
immunosuppressive agent		2014201410.0low000010
clindamycin
1
202220222.0low000001
pa 824
2
201220227.0low000011
sitafloxacin
1
fluoroquinolone antibiotic;
quinolines;
quinolone antibiotic		201920195.0low000010
9-benzyl-2-chloro-6-(2-furyl)purine
1
201920195.0medium000010
ethionamide
1
pyridines;
thiocarboxamide		antilipemic drug;
antitubercular agent;
fatty acid synthesis inhibitor;
leprostatic drug;
prodrug		201920195.0low000010
cerulenin
1
epoxide;
monocarboxylic acid amide		antifungal agent;
antiinfective agent;
antilipemic drug;
antimetabolite;
antimicrobial agent;
fatty acid synthesis inhibitor		201920195.0low000010
cyclosporine
1
homodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite		2014201410.0low000010
sirolimus
1
antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor		2014201410.0low000010
rifamycin sv
1
acetate ester;
cyclic ketal;
lactam;
macrocycle;
organic heterotetracyclic compound;
polyphenol;
rifamycins		antimicrobial agent;
antitubercular agent;
bacterial metabolite		2007200717.0low000100
rifaximin
2
acetate ester;
cyclic ketal;
lactam;
macrocycle;
organic heterohexacyclic compound;
rifamycins;
semisynthetic derivative		antimicrobial agent;
gastrointestinal drug;
orphan drug		200720229.5low000101
everolimus
1
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol		anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor		2014201410.0low000010
opc-67683
1
piperidines202220222.0low000001
temsirolimus
1
macrolide lactam2014201410.0low000010
fidaxomicin
1
2007200717.0low000100
jnj-26483327
1
2014201410.0high000010
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene
1
2014201410.0low000010
grazoprevir
1
aromatic ether;
azamacrocycle;
carbamate ester;
cyclopropanes;
lactam;
N-sulfonylcarboxamide;
quinoxaline derivative		antiviral drug;
hepatitis C protease inhibitor;
hepatoprotective agent		2014201410.0low000010
tigecycline
1
2007200717.0low000100
rifampin
6
cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor		200720229.5low000141
rifapentine
1
N-alkylpiperazine;
N-iminopiperazine;
rifamycins		antitubercular agent;
leprostatic drug		2014201410.0low000010
thiolactomycin
1
201920195.0low000010
rifabutin
3
201420225.7medium000021
krm 1657
1
201920195.0high000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
pyrazinamide
3
monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug		1994200026.3low003000
uracil
1
pyrimidine nucleobase;
pyrimidone		allergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
prodrug;
Saccharomyces cerevisiae metabolite		1995199529.0low001000
chlorpromazine
1
organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug		2003200321.0low000100
ciprofloxacin
1
aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic		2000200024.0low001000
clofazimine
3
monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug		1994199728.7low003000
dapsone
4
substituted aniline;
sulfone		anti-inflammatory drug;
antiinfective agent;
antimalarial;
leprostatic drug		1994199728.8low004000
diclofenac
2
amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic		1997199926.0low002000
isoniazid
8
carbohydrazideantitubercular agent;
drug allergen		1994200125.6low206200
metoprolol
1
aromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound		antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic		2008200816.0low000100
ofloxacin
14
3-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline		1995200624.6low0010400
thalidomide
1
phthalimides;
piperidones		1995199529.0low001000
reserpine
1
alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic		2000200024.0low001000
isoflurophate
1
dialkyl phosphate2000200024.0low001000
ethinyl estradiol
1
17-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen2007200717.0low100100
kanamycin a
2
kanamycinsbacterial metabolite1996199628.0low002000
carbostyril
4
monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite1995200027.8low004000
oxazoles
1
1,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene		1998199826.0low001000
alpha-aminopyridine
1
2000200024.0low001000
hematoxylin
1
organic heterotetracyclic compound;
oxacycle;
polyphenol;
tertiary alcohol		histological dye;
plant metabolite		1993199331.0low001000
azomycin
1
C-nitro compound;
imidazoles		antitubercular agent2003200321.0low000100
eosine yellowish-(ys)
1
organic sodium salt;
organobromine compound		fluorochrome;
histological dye		1993199331.0low001000
ethambutol
7
ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic		1994200027.6low007000
vancomycin
2
glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite		2004200619.0low000200
glycyrrhizic acid
1
enone;
glucosiduronic acid;
pentacyclic triterpenoid;
tricarboxylic acid;
triterpenoid saponin		EC 3.4.21.5 (thrombin) inhibitor;
plant metabolite		1999199925.0low001000
streptomycin
1
antibiotic antifungal drug;
antibiotic fungicide;
streptomycins		antibacterial drug;
antifungal agrochemical;
antimicrobial agent;
antimicrobial drug;
bacterial metabolite;
protein synthesis inhibitor		1995199529.0low001000
sparfloxacin
3
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		1995200027.3low003000
oxazolidin-2-one
1
carbamate ester;
oxazolidinone		metabolite2006200618.0low000100
clarithromycin
16
macrolide antibioticantibacterial drug;
environmental contaminant;
protein synthesis inhibitor;
xenobiotic		1994200226.7low1015100
levofloxacin
9
9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor		1997200623.8low006300
torcetrapib
1
(trifluoromethyl)benzenes;
carbamate ester;
quinolines		anticholesteremic drug;
CETP inhibitor		2008200816.0low000100
ritonavir
1
1,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic		1997199727.0low001000
saquinavir
1
L-asparagine derivative;
quinolines		antiviral drug;
HIV protease inhibitor		1997199727.0low001000
linezolid
1
acetamides;
morpholines;
organofluorine compound;
oxazolidinone		antibacterial drug;
protein synthesis inhibitor		2006200618.0low000100
mupirocin
1
alpha,beta-unsaturated carboxylic ester;
epoxide;
monocarboxylic acid;
oxanes;
secondary alcohol;
triol		antibacterial drug;
bacterial metabolite;
protein synthesis inhibitor		2006200618.0low000100
zithromax
3
macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic		2003201416.0low200210
pa 824
1
2003200321.0low000100
u 100480
1
1998199826.0low001000
abt 492
1
2000200024.0low001000
prothionamide
1
pyridines1995199529.0low001000
nadp
1
2000200024.0low001000
bilirubin
1
biladienes;
dicarboxylic acid		antioxidant;
human metabolite;
mouse metabolite		1993199331.0low001000
indinavir sulfate
1
dicarboxylic acid diamide;
N-(2-hydroxyethyl)piperazine;
piperazinecarboxamide		HIV protease inhibitor1997199727.0low001000
sitafloxacin
1
2003200321.0low000100
rifamycins
116
1991202223.7high90733634
minocycline
1
1995199529.0low001000
transforming growth factor beta
3
1997199925.7low003000
cyclosporine
1
2000200024.0low001000
rifampin
34
cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor		1992202223.3low10201103
rifapentine
2
N-alkylpiperazine;
N-iminopiperazine;
rifamycins		antitubercular agent;
leprostatic drug		1996199926.5low002000
krm 1657
4
1991200227.5high003100
rifametane
1
202220222.0medium000001
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acquired Immune Deficiency Syndrome0
2
1992199331.5low002000
Acquired Immunodeficiency Syndrome0
2
1992199331.5low002000
AIDS-Related Opportunistic Infections0
1
1999199925.0low001000
Antibiotic-Associated Colitis0
2
2004200718.5low000200
Arteriosclerosis, Coronary0
1
2006200618.0low000100
Atherogenesis0
2
2006200717.5low000200
Atherosclerosis0
2
2006200717.5low000200
Atypical Mycobacterial Infection, Disseminated0
2
1992200426.0low001100
Bacteremia0
1
1998199826.0low001000
Bacterial Disease0
1
1994199430.0low001000
Bacterial Infections0
1
1994199430.0low001000
Bacterial Sexually Transmitted Disease0
1
2007200717.0low100100
Body Weight0
2
1993200127.0low001100
Buruli Ulcer0
1
202220222.0low000001
Buruli Ulcer Disease0
1
202220222.0low000001
Chlamydia Infections0
9
2003201416.8low300810
Chlamydia pneumoniae Infections0
1
2008200816.0low000100
Communicable Diseases0
1
2003200321.0low000100
Coronary Artery Disease0
1
2006200618.0low000100
Diarrhea0
1
2004200420.0low000100
Disease Exacerbation0
1
1998199826.0low001000
Disease Models, Animal0
13
1993202222.1low009301
Diseases, Peripheral Vascular0
3
2007200916.0low100300
Enterocolitis, Pseudomembranous0
2
2004200718.5low000200
Eperythrozoonosis0
1
2007200717.0low100100
Female Genital Diseases0
1
2014201410.0low100010
Genital Diseases, Female0
1
2014201410.0low100010
Hansen Disease0
5
1993201924.4low004010
Helicobacter Infections0
3
2002202213.3low000201
HIV Coinfection0
1
202220222.0low000001
HIV Infections0
1
202220222.0low000001
Infection, Mycobacterium avium-intracellulare0
13
1992200126.8low0012100
Infections, Chlamydia0
9
2003201416.8low300810
Infections, Helicobacter0
3
2002202213.3low000201
Infections, Mycobacterium0
2
1993200027.5low002000
Infections, Staphylococcal0
2
1994200624.0low001100
Infections, Ureaplasma0
1
2007200717.0low100100
Infectious Diseases0
1
2003200321.0low000100
Intermittent Claudication0
1
2009200915.0low100100
Koch's Disease0
29
1993202225.0medium1025202
Leprosy0
5
1993201924.4low004010
Mycobacterium avium-intracellulare Infection0
13
1992200126.8low0012100
Mycobacterium Infections0
2
1993200027.5low002000
Peripheral Vascular Diseases0
3
2007200916.0low100300
Pulmonary Consumption0
3
1998200124.3low102100
Recrudescence0
2
2001200620.5low100200
Scrofuloderma0
1
2004200420.0low000100
Sensitivity and Specificity0
3
2002200720.3low000300
Sexually Transmitted Diseases, Bacterial0
1
2007200717.0low100100
Staphylococcal Infections0
2
1994200624.0low001100
Tuberculosis0
29
1993202225.0medium1025202
Tuberculosis, Avian0
1
1993199331.0low001000
Tuberculosis, Drug-Resistant0
2
1996199926.5low002000
Tuberculosis, Multidrug-Resistant0
2
1996199926.5low002000
Tuberculosis, Pulmonary0
3
1998200124.3low102100
Urethritis0
1
2007200717.0low100100
Weight Loss0
1
2004200420.0low000100
Weight Reduction0
1
2004200420.0low000100

Safety/Toxicity (1)

ArticleYear
Randomized, double-blind, multicenter safety and efficacy study of rifalazil compared with azithromycin for treatment of uncomplicated genital Chlamydia trachomatis infection in women.
Antimicrobial agents and chemotherapy, , Volume: 58, Issue:7		2014

Pharmacokinetics (4)

ArticleYear
Lack of effect of rifalazil on ethinyl estradiol pharmacokinetics in healthy postmenopausal women.
International journal of clinical pharmacology and therapeutics, , Volume: 45, Issue:7		2007
Effect of food on the pharmacokinetics of rifalazil, a novel antibacterial, in healthy male volunteers.
Journal of clinical pharmacology, , Volume: 47, Issue:7		2007
[Anti-Mycobacterium avium complex activities of KRM-1648, clarithromycin and levofloxacin in 7HSF medium at peak or average blood concentrations after their oral administration of clinical dosages].
Kekkaku : [Tuberculosis], , Volume: 72, Issue:7		1997
Pharmacokinetics of KRM-1648, a new benzoxazinorifamycin, in rats and dogs.
Antimicrobial agents and chemotherapy, , Volume: 40, Issue:12		1996

Bioavailability (2)

ArticleYear
Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties?
Journal of medicinal chemistry, , Jan-23, Volume: 57, Issue:2		2014
Pharmacokinetics of KRM-1648, a new benzoxazinorifamycin, in rats and dogs.
Antimicrobial agents and chemotherapy, , Volume: 40, Issue:12		1996

Dosage (7)

ArticleYear
[In vitro antimicrobial activities of quinolones, rifamycins and macrolides against Mycobacterium tuberculosis and M.avium complex: attempt to establish new assay methods which accurately reflect therapeutic effects of test agents in vivo].
Kekkaku : [Tuberculosis], , Volume: 74, Issue:1		1999
[Therapeutic efficacy of benzoxazinorifamycin KRM-1648 against experimental murine tuberculosis: (1). A study on the efficacy of short course treatment with the intratracheal and intravenous infection model].
Kekkaku : [Tuberculosis], , Volume: 73, Issue:2		1998
Antimicrobial activities of benzoxazinorifamycin KRM-1648, clarithromycin and levofloxacin against intracellular Mycobacterium avium complex phagocytosed by murine peritoneal macrophages.
The Journal of antimicrobial chemotherapy, , Volume: 41, Issue:1		1998
[Anti-Mycobacterium avium complex activities of KRM-1648, clarithromycin and levofloxacin in 7HSF medium at peak or average blood concentrations after their oral administration of clinical dosages].
Kekkaku : [Tuberculosis], , Volume: 72, Issue:7		1997
In vitro and in vivo activities of the benzoxazinorifamycin KRM-1648 against Mycobacterium tuberculosis.
Antimicrobial agents and chemotherapy, , Volume: 39, Issue:10		1995
In vivo antileprosy activity of the newly synthesized benzoxazinorifamycin, KRM-1648.
International journal of leprosy and other mycobacterial diseases : official organ of the International Leprosy Association, , Volume: 61, Issue:2		1993
Activities of the benzoxazinorifamycin KRM 1648 and ethambutol against Mycobacterium avium complex in vitro and in macrophages.
Antimicrobial agents and chemotherapy, , Volume: 38, Issue:8		1994

Interactions (13)

ArticleYear
Enhanced activity of rifalazil in combination with levofloxacin, linezolid, or mupirocin against Staphylococcus aureus in vitro.
The Journal of antibiotics, , Volume: 59, Issue:5		2006
In vitro time-kill activities of rifalazil, alone and in combination with vancomycin, against logarithmic and stationary cultures of Staphylococcus aureus.
The Journal of antibiotics, , Volume: 59, Issue:2		2006
In-vitro activity of sitafloxacin (DU-6859a), either singly or in combination with rifampin analogs, against Mycobacterium leprae.
Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy, , Volume: 9, Issue:1		2003
In vitro activity of KRM-1648, either singly or in combination with ofloxacin, against Mycobacterium ulcerans.
International journal of antimicrobial agents, , Volume: 17, Issue:1		2001
Durable cure for tuberculosis: rifalazil in combination with isoniazid in a murine model of Mycobacterium tuberculosis infection.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, , Volume: 30 Suppl 3		2000
Therapeutic effects of benzoxazinorifamycin KRM-1648 administered alone or in combination with a half-sized secretory leukocyte protease inhibitor or the nonsteroidal anti-inflammatory drug diclofenac sodium against Mycobacterium avium complex infection i
Antimicrobial agents and chemotherapy, , Volume: 43, Issue:2		1999
Activity of KRM 1648 or rifabutin alone or in combination with clarithromycin against Mycobacterium avium complex in human alveolar macrophages.
The international journal of tuberculosis and lung disease : the official journal of the International Union against Tuberculosis and Lung Disease, , Volume: 1, Issue:5		1997
Studies on therapeutic activity of benzoxazinorifamycin KRM-1648 in combination with other antimicrobial agents and biological response modifiers interferon-gamma and granulocyte-macrophage colony-stimulating factor against M. leprae infection in athymic
International journal of leprosy and other mycobacterial diseases : official organ of the International Leprosy Association, , Volume: 65, Issue:3		1997
Activity of KRM-1648 alone or in combination with both ethambutol and kanamycin or clarithromycin against Mycobacterium intracellulare infections in beige mice.
Antimicrobial agents and chemotherapy, , Volume: 40, Issue:2		1996
Activity of KRM-1648 in combination with isoniazid against Mycobacterium tuberculosis in a murine model.
Antimicrobial agents and chemotherapy, , Volume: 40, Issue:2		1996
[Therapeutic efficacy of a benzoxazinorifamycin, KRM-1648, combined with a immunopotentiator, LC9018, in Mycobacterium intracellulare infection induced in beige mice].
Kekkaku : [Tuberculosis], , Volume: 68, Issue:12		1993
Therapeutic efficacy of benzoxazinorifamycin, KRM-1648, in combination with other antimicrobials against Mycobacterium leprae infection induced in nude mice.
International journal of leprosy and other mycobacterial diseases : official organ of the International Leprosy Association, , Volume: 62, Issue:1		1994
Activity of KRM 1648 alone or in combination with ethambutol or clarithromycin against Mycobacterium avium in beige mouse model of disseminated infection.
Antimicrobial agents and chemotherapy, , Volume: 38, Issue:8		1994