| Identification | Back Directory | [Name]
(S)-2-nitro-6-((6-(4-(trifluoroMethoxy)phenyl)pyridin-3-yl)Methoxy)-6,7-dihydro-5H-iMidazo[2,1-b][1,3]oxazine | [CAS]
1257426-19-9 | [Synonyms]
TBA-354
CS-1782
EOS-60528
TBA 354 ;TBA354
(S)-2-Nitro-6-((6-(4-(trifluoromethoxy)phenyl)pyridin-3-yl)methoxy)-6,7-dihydro-5H-imidazo[2,1
(S)-2-nitro-6-((6-(4-(trifluoroMethoxy)phenyl)pyridin-3-yl)Methoxy)-6,7-dihydro-5H-iMidazo[2,1-b][1,3]oxazine
(6S)-2-nitro-6-({6-[4-(trifluoromethoxy)phenyl]-3-pyridinyl}methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine
(6S)-6,7-Dihydro-2-nitro-6-[[6-[4-(trifluoromethoxy)phenyl]-3-pyridinyl]methoxy]-5H-imidazo[2,1-b][1,3]oxazine
5H-Imidazo[2,1-b][1,3]oxazine, 6,7-dihydro-2-nitro-6-[[6-[4-(trifluoromethoxy)phenyl]-3-pyridinyl]methoxy]-, (6S)-
BX471(6S)-2-nitro-6-({6-[4-(trifluoromethoxy)phenyl]-3-pyridinyl}methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine | [Molecular Formula]
C19H15F3N4O5 | [MDL Number]
MFCD28009369 | [MOL File]
1257426-19-9.mol | [Molecular Weight]
436.34 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in EtOH; insoluble in H2O; ≥17.6 mg/mL in DMSO | [form ]
solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
TBA-354 is a nitroimidazole antitubercular agent. It is active against clinical isolates of drug-resistant and -sensitive replicating M. tuberculosis (MICs = <0.02-0.36 μM). It is selective for M. tuberculosis over M. scrofulaceum, M. gilvum, M. fortuitum, M. triviale, and M. smegmatis (MICs = >11.5 μM) but is active against M. bovis and M. kansasii (MICs = <0.179 and 2.2 μM, respectively). TBA-354 (100 mg/kg per day) reduces lung colony forming units (CFUs) in mouse models of acute and chronic M. tuberculosis infection. | [Uses]
TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains.
IC50 value:
Target: Anti-tuberculosis agent
in 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. | [References]
[1]. upton am, cho s, yang tj, et al. in vitro and in vivo activities of the nitroimidazole tba-354 against mycobacterium tuberculosis. antimicrob agents chemother, 2015, 59(1): 136-144.
[2]. tasneen r, williams k, amoabeng o, 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, 59 :129-135. |
|
| Company Name: |
DKMbiochem.Co. Ltd
|
| Telephone: |
15901859516 |
| Website: |
http://www.dkmbiochem.com/ |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
|