| Identification | Back Directory | [Name]
BTZ043 | [CAS]
1161233-85-7 | [Synonyms]
BTZ043
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)- | [Molecular Formula]
C17H16F3N3O5S | [MDL Number]
MFCD17215196 | [MOL File]
1161233-85-7.mol | [Molecular Weight]
431.39 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
BTZ043 is an inhibitor of the essential flavo-enzyme Decaprenylphosphoryl-beta-D-ribose 2-epimerase (DprE1). | [Synthesis]
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]. | [storage]
Store at -20°C | [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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| Company Name: |
D&C Chemicals
|
| Telephone: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
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