PBTZ169

Modify Date: 2024-01-13 16:21:40

PBTZ169 Structure
PBTZ169 structure
Common Name PBTZ169
CAS Number 1377239-83-2 Molecular Weight 456.482
Density 1.5±0.1 g/cm3 Boiling Point 555.6±60.0 °C at 760 mmHg
Molecular Formula C20H23F3N4O3S Melting Point N/A
MSDS N/A Flash Point 289.8±32.9 °C

 Use of PBTZ169


Macozinone is a new drug candicate that inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043target: DprE1In vitro: PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. [1]In vivo: PBTZ169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL.[2] PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB). [3]

 Names

Name 2-[4-(Cyclohexylmethyl)-1-piperazinyl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
Synonym More Synonyms

 PBTZ169 Biological Activity

Description Macozinone is a new drug candicate that inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043target: DprE1In vitro: PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. [1]In vivo: PBTZ169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL.[2] PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB). [3]
Related Catalog
References

[1]. [1] Makarov V et al. The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52.

[2]. [2] González-Martínez NA et al. In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis. PLoS Negl Trop Dis. 2015 Oct 16;9(10):e0004022.

[3]. [3] Makarov V et al. Towards a new combination therapy for tuberculosis with next generation benzothiazinones.EMBO Mol Med. 2014 Mar;6(3):372-83.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 555.6±60.0 °C at 760 mmHg
Molecular Formula C20H23F3N4O3S
Molecular Weight 456.482
Flash Point 289.8±32.9 °C
Exact Mass 456.144287
LogP 3.83
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.660

 Synonyms

2-[4-(Cyclohexylmethyl)-1-piperazinyl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
4H-1,3-Benzothiazin-4-one, 2-[4-(cyclohexylmethyl)-1-piperazinyl]-8-nitro-6-(trifluoromethyl)-
PBTZ169
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