| Identification | Back Directory | [Name]
BTZ043 (BTZ038, BTZ044) | [CAS]
957217-65-1 | [Synonyms]
BTZ038
BTZ044
BTZ 10526038
BTZ038; BTZ044
BTZ043 (BTZ038, BTZ044)
Benzothiazinone 10526038
2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one
4H-1,3-Benzothiazin-4-one, 2-(2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-8-nitro-6-(trifluoromethyl)-
2-(2-Methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one
2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one BTZ043 Racemate | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C17H16F3N3O5S | [MDL Number]
MFCD22420808 | [MOL File]
957217-65-1.mol | [Molecular Weight]
431.39 |
| Chemical Properties | Back Directory | [Boiling point ]
547.6±60.0 °C(Predicted) | [density ]
1.68±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥10.4 mg/mL in DMSO with gentle warming; ≥3.27 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
-0.51±0.20(Predicted) |
| Hazard Information | Back Directory | [Biological Activity]
mic: 1 ng/ml (2.3 nm) for m. tuberculosis h37rv and 4 ng/ml (9.2 nm) for mycobacterium smegmatisthe loss of human lives to tuberculosis (tb) continues unabated as a result of poverty, synergy with the hiv/aids pandemic, and the emergence of multidrug- and extensively drug-resistant strains of mycobacterium tuberculosis. btz043 is the most advanced candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant tb. | [in vitro]
btz043 displayed similar activity against all clinical isolates of m. tuberculosis that were tested, including extensively drug-resistant and multidrug-resistant strains, indicating that it targets a previously unknown biological function. btz043 is bactericidal, reducing viability in vitro by more than 1000-fold in under 72 hours, which is comparable to the inh killing effect [1]. | [in vivo]
the in vivo efficacy of btz043 was assessed 4 weeks after a low-dose aerosol infection of in the chronic balb/c mice model of tb. four weeks of treatment with btz043 reduced the bacterial load in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. additional findings suggest that btz efficacy is time- rather than dose-dependent [1]. | [target]
| [References]
[1] makarov v, manina g, mikusova k, et al. benzothiazinones kill mycobacterium tuberculosis by blocking arabinan synthesis. science. 2009 may 8;324(5928):801-4. |
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