Interesting scientific research on (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine

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Reference of 300543-56-0, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 300543-56-0, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine, SMILES is ClC1=CC=C([C@H](N2CCNCC2)C3=CC=CC=C3)C=C1, belongs to piperazines compound. In a article, author is Guo, Shaochen, introduce new discover of the category.

In vitro and in vivo antimicrobial activities of a novel piperazine-containing benzothiazinones candidate TZY-5-84 against Mycobacterium tuberculosis

A piperazine-containing benzothiazinones lead compound PBTZ169, served as DprE1 inhibitor, displays nanomolar bactericidal activity against Mycobacteria tuberculosis. Here, we systematically evaluate anti-tuberculosis activity of one of PBTZ169 analogues, TZY-5-84, in vitro and in vivo. The MIC value of TZY-5-84 against M. tuberculosis H37Rv ranged from 0.014 to 0.015 mg/L, lower than those of INH, RFP and BDQ. Five susceptible and thirteen drug-resistant clinical isolates were also susceptive to TZY-5-84. It had anti-tuberculosis activity against intracellular bacilli in infected macrophage model. It exhibited its activity in time-dependent manner and against intracellular bacilli in infected macrophage cells. However, the MIC of TZY-5-84 against three laboratory PBTZ169-induced resistant isolates increased four-fold increment compared to that of H37Rv. No antagonism was observed in any combination between TZY-5-84 and seven commonly used anti-tuberculosis drugs in an in vitro checkerboard assay. In murine infection model, TZY-5-84 at lower dosage (12.5 mg/kg) was found to be comparatively efficacious as PBTZ169 at 25 mg/kg. Our research suggests TZY-5-84 can be a promising preclinical candidate for further study on TB treatment.

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Reference:
Piperazine – Wikipedia,
,Piperazines – an overview | ScienceDirect Topics