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| 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 |
| Synonyms: | PBTZ169,PBTZ-169,PBTZ 169 |
| SMILES: | O=C1N=C(N2CCN(CC3CCCCC3)CC2)SC4=C([N+]([O-])=O)C=C(C(F)(F)F)C=C14 |
| Formula: | C20H23F3N4O3S |
| M.Wt: | 456.48 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| 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] |