|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|CsnPharm

CAS No.: 1161233-85-7

BTZ043 Catalog No. CSN17371

Synonyms: BTZ043

BTZ043 is an antimycobacterial working by targeting mycobacterial cell wall synthesis by inhibiting DprE1.

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生物活性

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技术信息

生物活性

描述DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) catalyzes the conversion of decaprenylphosphoryl-β-d-ribose (DPR) to its arabinose counterpart decaprenylphosphoryl-β-d-arabinose (DPA), which is the sole donor of arabinose sugars that are essential for cell wall biosynthesis in M. tuberculosis and other Corynebacterineae species. BTZ043 inhibits DprE1 and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. Complete inhibition of DPA synthesis was obtained in the presence of only 25 μg/ml BTZ043^[2]. The MIC (minimal inhibitory concentration) of BTZ043 against M. tuberculosis H37Rv and Mycobacterium smegmatis were 1 ng/ml (2.3 nM) and 4 ng/ml (9.2 nM), respectively. The in vivo efficacy of BTZ043 was assessed 4 weeks after a low-dose aerosol infection of BALB/c mice in the chronic model of TB (tuberculosis). Four weeks of treatment with BTZ043 reduced the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively^[3]. Pharmacokinetic (PK) study of PyrBTZ01 in BALB/c mice showed that BTZ043 had a half-live of ∼100 min. The higher maximum concentration (C_max) observed for BTZ043 was 1,923 ng/ml. Mice were infected by intravenous injection of M. tuberculosis H37Rv and then treated with BTZ043. BTZ043 was effective leading to ∼3.2-log-unit decreases in the numbers of CFU (colony-forming units) over 4 weeks, compared to the untreated control group^[2].
作用机制The 8-nitro group of BTZ043 scaffold involves formation of a semimercaptal bond with Cys387 in the active site of DprE1^[2].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03590600	Tuberculosis ... more >>Tuberculosis, Pulmonary Bacterial Infections Lung Diseases Mycobacterium Infections Collapse <<	Phase 1	Active, not recruiting	February 15, 2019	Germany ... more >> Nuvisan Neu-Ulm, Bavaria, Germany, 89231 Collapse <<

参考文献

[1] Gonzalez-Martinez NA, Lozano-Garza HG, et al. In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis. PLoS Negl Trop Dis. 2015 Oct 16;9(10):e0004022.
[2] The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis
[3] Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3181 mL
- 11.5905 mL
- 23.1811 mL
- 5 mM
- 0.4636 mL
- 2.3181 mL
- 4.6362 mL
- 10 mM
- 0.2318 mL
- 1.1591 mL
- 2.3181 mL

技术信息

CAS号

1161233-85-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H16F3N3O5S

运输

蓝冰

分子量

431.39

别名

BTZ043

溶解度

DMSO	13.3 mg/mL (30.8 mM)
Water	Insoluble

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