利福拉齐
| 中文名称 | 利福拉齐 |
|---|---|
| 中文同义词 | 3'-羟基-5'-(4-异丁基-1-哌嗪)苯噁嗪利福霉素;利福拉齐;3'-羟基-5'-(4-异丁基-1-哌嗪)苯嗪利福霉素;化合物 T16749 |
| 英文名称 | Rifalazil |
| 英文同义词 | RIFALAZIL;KRM 1648;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;Rifalazil USP/EP/BP |
| CAS号 | 129791-92-0 |
| 分子式 | C51H64N4O13 |
| 分子量 | 941.07 |
| EINECS号 | |
| 相关类别 | 标准品 |
| Mol文件 | 129791-92-0.mol |
| 结构式 |  |
利福拉齐 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 | 二甲基亚砜：8.33 mg/mL（8.85 mM） |
| 酸度系数(pKa) | 4.28±0.70(Predicted) |
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. |