129791-92-0
基本信息
3'-羟基-5'-(4-异丁基-1-哌嗪)苯嗪利福霉素
3'-羟基-5'-(4-异丁基-1-哌嗪)苯噁嗪利福霉素
RIFALAZIL
Rifalazil USP/EP/BP
3'-Hydroxy-5'-(4-isobutylpiperazinyl)benzoxazinorifamycin
1-Deoxy-1'-dehydro-1-oxo-3'-hydroxy-5'-[4-(2-methylpropyl)piperazino]rifamycin VIII
5,12-Dihydroxy-2,4-dimethyl-10-[4-(2-methyl-propyl)-l-piperazinyl]-2,7-[oxy(5-acetoxy-7,9-dihydroxy-3-methoxy-4,6,8,10,14-pentamethyl-15-oxo-l,ll,13-pentadecatriene-l,15-diyl)imino]-6H-benzofuro[4,5-a]phenoxazine-l(2H),6-dione
物理化学性质
| 熔点 | 195-200° (dec) |
| 沸点 | 1065.6±65.0 °C(Predicted) |
| 密度 | 1.36±0.1 g/cm3(Predicted) |
| 储存条件 | 4°C, away from moisture |
| 溶解度 | DMSO: 8.33 mg/mL (8.85 mM) |
| 酸度系数(pKa) | 4.28±0.70(Predicted) |
| 形态 | Solid |
| 颜色 | Blue to dark blue |
常见问题列表
IC50: RNA polymerase
Rifalazil exhibits antimicrobal activity against Gram-positive enteric bacteria, inhibits Clostridium difficile , Clostridium perfringens , Bacteroides fragilis with MIC 50 value of 0.0015, 0.0039, 0.0313 µg/ml, respectively. Rifalazil exhibits antimicrobal activity against Gram-negative enteric bacteria, inhibits Escherichia coli and Klebsiella pneumoniae with MIC 50 value of 16 and 16 µg/ml, respectively. Rifalazil exhibits antimicrobal activity against non-enteric Gram-positive bacteria, inhibits Methicillin-susceptible Staphylococcus aureus , Methicillin-resistant S. aureus , Methicillin- and quinolone-resistant S. aureus , Staphylococcus epidermidis , Streptococcus pyogenes , Streptococcus pneumoniae with MIC 50 value of 0.0078, 0.0078, 0.0078, 0.0078, 0.0002, 0.0001 µg/ml, respectively. Rifalazil exhibits antimicrobal activity against Helicobacter pylori , Chlamydia pneumoniae and Chlamydia trachomatis with MIC 50 value of 0.004, 0.000125 and 0.00025 µg/ml, respectively.
Rifalazil (oral gavage; 20, 25, and 150 mg/kg; 6-8 weeks) combines with isoniazid (INH) for 6 weeks or greater significantly reduced the number of mice per group in which M. tuberculosis is detected in both spleens and lungs compared to the reductions for the early and late controls. And the addition of Pyrazinamide (PZA) does not significantly improve RLZ-INH therapy at any time point.
| Animal Model: | Female CD-1 mice infected with 5.2 × 10 7 viable mycobacteria |
| Dosage: | 20, 25, and 150 mg/kg; 6-8 weeks |
| Administration: | Oral gavage |
| Result: | Combined with isoniazid (INH) showed its potential for short-course treatment of Mycobacterium tuberculosis infection. |