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PBTZ169
Axon 2626
CAS:
1377239-83-2
Purity:
100%
- Soluble in DMSO and EtOH
- MF: C20H23F3N4O3S
- MW: 456.48
Description
Potent irreversible DprE1 inhibitor (MIC value <0.19 ng/mL and <0.004 µM against M. tuberculosis H37Ra) with improved stability against nitroreductase metabolism, and good efficacy at lower concentrations in the murine model of chronic tuberculosis (TB); an attractive drug candidate to treat TB in humans. The combination of PBTZ169, BDQ and pyrazinamide was found to be more efficacious than the standard three drug treatment in a murine model of chronic disease.
More Information
| Parent CAS No. | 1377239-83-2 |
|---|---|
| Chemical Name | 2-(4-(cyclohexylmethyl)piperazin-1-yl)-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one |
| SMILES | C1C([N+]([O-])=O)=C2SC(N3CCN(CC4CCCCC4)CC3)=NC(=O)C2=CC=1C(F)(F)F |
| MFCD | N.A. |
| InChi | InChI=1S/C20H23F3N4O3S/c21-20(22,23)14-10-15-17(16(11-14)27(29)30)31-19(24-18(15)28)26-8-6-25(7-9-26)12-13-4-2-1-3-5-13/h10-11,13H,1-9,12H2 |
| InChiKey | BJDZBXGJNBMCAV-UHFFFAOYSA-N |
| CID | 57331386 |
| Short Description | DprE1 inhibitor |
References
- V Makarov et al. Towards a new combination therapy for tuberculosis with next generation benzothiazinones. EMBO Mol Med. 2014 Mar; 6(3): 372–383.
- CT Peng et al. Synthesis and antitubercular evaluation of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1373-6.
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