1377239-83-2

1377239-83-2 structure

Name: PBTZ169
Chemical Name: 2-[4-(Cyclohexylmethyl)-1-piperazinyl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
CAS Number: 1377239-83-2
Molecular Formula: C₂₀H₂₃F₃N₄O₃S
Molecular Weight: 456.482
Catalog: Research Areas Cancer
Create Date: 2018-06-07 08:02:07
Modify Date: 2024-01-13 16:21:40
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]

Name	2-[4-(Cyclohexylmethyl)-1-piperazinyl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
Synonyms	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)- PBTZ169

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]
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
References	[1]. [1] Makarov V et al. The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52. [2]. [2] González-Martínez NA et al. In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis. PLoS Negl Trop Dis. 2015 Oct 16;9(10):e0004022. [3]. [3] Makarov V et al. Towards a new combination therapy for tuberculosis with next generation benzothiazinones.EMBO Mol Med. 2014 Mar;6(3):372-83.