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| | PBTZ169 Basic information |
| Product Name: | PBTZ169 | | Synonyms: | 2-(4-(Cyclohexylmethyl)piperazin-1-yl)-8-nitro-6-trifluoromethyl-4H-1,3-benzothiazin-4-one;Macozinone;PBTZ169;PBTZ-169;PBTZ 169;CS-2309;PBTZ169 (PBTZ 169; 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)-;2-(4-(Cyclohexylmethyl)piperazin-1-yl)-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one | | CAS: | 1377239-83-2 | | MF: | C20H23F3N4O3S | | MW: | 456.48 | | EINECS: | | | Product Categories: | | | Mol File: | 1377239-83-2.mol |  |
| | PBTZ169 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO:4.6(Max Conc. mg/mL);10.1(Max Conc. mM) | | form | A crystalline solid | | color | Light yellow to yellow |
| | PBTZ169 Usage And Synthesis |
| Description | PBTZ169 is an antibiotic with antimycobacterial activity. It is an irreversible inhibitor of DprE1, an essential enzyme for cell wall synthesis in mycobacteria. PBTZ169 is active against M. tuberculosis in vitro (MIC = ≤0.19 ng/ml) without inducing cytotoxicity in Vero cells when used at concentrations up to 125 μM. It reduces the bacterial burden in the lung and spleen in a mouse model of chronic tuberculosis when administered at a dose of 50 mg/kg per day. | | Uses | PBTZ169 is a potent irreversible inhibitor of decaprenylphosphoryl-beta-D-ribose 2-epimerase (DprE1), and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. | | References | [1] CUI-TING PENG . Synthesis and antitubercular evaluation of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives[J]. Bioorganic & Medicinal Chemistry Letters, 2015, 25 7: Pages 1373-1376. DOI: 10.1016/j.bmcl.2015.02.061
[2] VADIM MAKAROV. Towards a new combination therapy for tuberculosis with next generation benzothiazinones.[J]. EMBO Molecular Medicine, 2014, 6 3: 372-383. DOI: 10.1002/emmm.201303575 |
| | PBTZ169 Preparation Products And Raw materials |
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