BTZ043
BTZ043 Basic information
- Product Name:
- BTZ043
- Synonyms:
-
- BTZ043
- BTZ043 raceMate
- 2-[(2S)-2-Methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-trifluoromethyl-4H-1,3-benzothiazin-4-one
- BTZ 10526043
- PBTZ 169
- 2-[(3S)-3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one
- BTZ043 (BTZ-043
- CS-2310
- CAS:
- 1161233-85-7
- MF:
- C17H16F3N3O5S
- MW:
- 431.39
- Mol File:
- 1161233-85-7.mol
BTZ043 Chemical Properties
- Melting point:
- 190-191°C
- Density
- 1.68
- storage temp.
- -20°C Freezer
- solubility
- Chloroform (Slightly), Methanol (Very Slightly)
- form
- Solid
- color
- White to Pale Yellow
BTZ043 Usage And Synthesis
Uses
BTZ043 is an inhibitor of the essential flavo-enzyme Decaprenylphosphoryl-beta-D-ribose 2-epimerase (DprE1).
Synthesis
1344087-80-4
1344087-73-5
1161233-85-7
Synthesis of 2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one (Compound 1) and (2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decane as 2-(methylsulfanyl)-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one (Compound 1) and (2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decane. -Trifluoromethyl-4H-1,3-benzothiazin-4-one was carried out in the following general steps: 3.0 g of Compound 1 was suspended in 15 mL of ethanol followed by the addition of 1.5 g of (2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decane. The reaction mixture was stirred at room temperature and then heated to 50-60°C maintained for 20 minutes. Upon completion of the reaction, it was cooled to room temperature and a light yellow solid was precipitated by adding 100 mL of water. The product was isolated by filtration in 76% yield (calculated based on 2-chloro-3-nitro-5-trifluoromethylbenzamide).
in vivo
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[2].
References
[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
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