1161233-85-7
1161233-85-7 结构式
基本信息
DPRE1抑制剂(BTZ043)
DPRE1抑制剂(PBTZ169)
2-[(2S)-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基]-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮
CS-2310
PBTZ 169
BTZ 10526043
BTZ043 raceMate
BTZ043 (BTZ-043
BTZ043
BTZ-043
BTZ 043
2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one
2-[(2S)-2-Methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-trifluoromethyl-4H-1,3-benzothiazin-4-one
4H-1,3-Benzothiazin-4-one, 2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-
制备方法
![(S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decane](/CAS/20200401/GIF/1344087-80-4.gif)
1344087-80-4
![2-(Methylthio)-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one](/CAS/20200331/GIF/1344087-73-5.gif)
1344087-73-5
1161233-85-7
以2-(甲硫基)-8-硝基-6-(三氟甲基)-4H-苯并[e][1,3]噻嗪-4-酮（化合物1）和（2S）-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷为原料，合成2-[(2S)-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基]-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮的一般步骤如下：将3.0 g化合物1悬浮于15 mL乙醇中，随后加入1.5 g（2S）-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷。反应混合物在室温下搅拌后，加热至50-60℃维持20分钟。反应完成后，冷却至室温，加入100 mL水析出淡黄色固体。通过过滤分离产物，产率为76%（基于2-氯-3-硝基-5-三氟甲基苯甲酰胺计算）。
参考文献：
[1] Patent: EP2380886, 2011, A1. Location in patent: Page/Page column 8
[2] Patent: WO2011/132070, 2011, A1. Location in patent: Page/Page column 12-13
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/05/22 | HY-13579A | 2-[(2S)-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基]-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮 BTZ043 Racemate | 1161233-85-7 | 5 mg | 900元 |
| 2025/05/22 | HY-13579A | 2-[(2S)-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基]-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮 BTZ043 Racemate | 1161233-85-7 | 10 mM * 1 mLin DMSO | 990元 |
| 2025/05/22 | HY-13579A | 2-[(2S)-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基]-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮 BTZ043 Racemate | 1161233-85-7 | 10mg | 1200元 |
常见问题列表
DprE1.
The MIC of BTZ043 against M. tuberculosis H37Rv and Mycobacterium smegmatis are 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively. The in vitro activity of BTZ043 against 30 Nocardia brasiliensis isolates is also tested. The MIC50 and MIC90 values for BTZ043 are 0.125 and 0.25 μg/mL. The MIC for N. carnea ATCC 6847 is 0.003μg/mL, for N. transvalensis ATCC 6865 is 0.003μg/mL, for N. brasiliensis NCTC10300 is 0.03 μg/mL, and for N. brasiliensis HUJEG-1 is 0.125μg/mL. The MIC value for M. tuberculosis H37Rv is 0.000976 μg/mL. The MIC value of BTZ-043 is >64 μg/mL for Escherichia coli ATCC 25922 and S. aureus ATCC 29213.
Four weeks of treatment with BTZ043 reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. Additional results suggest that BTZ043 efficacy is time-rather than dose-dependent. Acute (5 g/kg) and chronic (25 and 250 mg/kg) toxicology studies in uninfected mice show that, even at the highest dose tested, there are no adverse anatomical, behavioral, or physiological effects after one month.