TBA-354

Modify Date: 2025-08-25 15:55:38

TBA-354 Structure
TBA-354 structure
Common Name TBA-354
CAS Number 1257426-19-9 Molecular Weight 436.341
Density 1.5±0.1 g/cm3 Boiling Point 570.0±60.0 °C at 760 mmHg
Molecular Formula C19H15F3N4O5 Melting Point N/A
MSDS N/A Flash Point 298.5±32.9 °C

 Use of TBA-354


TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.IC50 value:Target: Anti-tuberculosis agentin vitro: TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates [1]. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy [2].in vivo: TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.

 Names

Name (6S)-2-nitro-6-({6-[4-(trifluoromethoxy)phenyl]-3-pyridinyl}methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
Synonym More Synonyms

 TBA-354 Biological Activity

Description TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.IC50 value:Target: Anti-tuberculosis agentin vitro: TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates [1]. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy [2].in vivo: TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.
Related Catalog
References

[1]. Upton AM, et al. In Vitro and In Vivo Activities of the Nitroimidazole TBA-354 against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59(1):136-44.

[2]. Tasneen R, et al. Contribution of the Nitroimidazoles PA-824 and TBA-354 to the Activity of Novel Regimens in Murine Models of Tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59(1):129-35.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 570.0±60.0 °C at 760 mmHg
Molecular Formula C19H15F3N4O5
Molecular Weight 436.341
Flash Point 298.5±32.9 °C
Exact Mass 436.099457
PSA 104.22000
LogP 3.02
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.623
Storage condition 2-8℃

 Synonyms

(6S)-2-Nitro-6-({6-[4-(trifluoromethoxy)phenyl]-3-pyridinyl}methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
(S)-2-nitro-6-((6-(4-(trifluoromethoxy)phenyl)pyridine-3-yl)methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
(6S)-2-nitro-6-({6-[4-(trifluoromethoxy)phenyI]-3-pyridinyI}methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
SN31354
5H-Imidazo[2,1-b][1,3]oxazine, 6,7-dihydro-2-nitro-6-[[6-[4-(trifluoromethoxy)phenyl]-3-pyridinyl]methoxy]-, (6S)-
(S)-2-nitro-6-((6-(4-(trifluoroMethoxy)phenyl)pyridin-3-yl)Methoxy)-6,7-dihydro-5H-iMidazo[2,1-b][1,3]oxazine
TBA-354
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