《Design, synthesis and biological evaluation of novel pleuromutilin derivatives containing piperazine and 1,2,3-triazole linker》 was written by Zhang, Guang-Yu; Zhang, Zhe; Li, Kang; Liu, Jie; Li, Bo; Jin, Zhen; Liu, Ya-Hong; Tang, You-Zhi. HPLC of Formula: 109-01-3 And the article was included in Bioorganic Chemistry in 2020. The article conveys some information:
A series of novel pleuromutilin derivatives containing piperazine ring, 1,2,3-triazoles and secondary amines on side chain of C14 e.g., I were synthesized under mild conditions via click reaction. The in vitro antibacterial activities of synthesized derivatives against four strains of Staphylococcus aureus (MRSA ATCC 43300, ATCC 29213,144 and AD3) and one strain of Escherichia coli (ATCC 25922) were evaluated by broth dilution method. Among these derivatives, 22-[2-(4-((4-nitrophenyl piperazine)methyl)-1,2,3-triazol-1-yl)-1-(piperazine-1-yl) ethyl-1-one] deoxy pleuromutilin I showed most prominent in vitro antibacterial effect against MRSA (MIC = 1μg/mL). Furthermore, compound I displayed more rapid bactericidal kinetic than tiamulin time-kill studies and possessed a longer PAE than tiamulin against MRSA in vitro. In addition, in vivo antibacterial activities of compound I against MRSA were further evaluated employing thigh infection model. And compound I (-8.89 log10 CFU/mL) displayed superior activities than tiamulin. Compound I was further evaluated in CYP450 inhibition assay and the results showed that it exhibited low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6 and CYP3A4 enzymes. The PK properties of compound I were then measured. The half-life (t1/2), clearance rate (Cl) and area under the plasma concentration time curve (AUC0→∞) of compound I were 0.74 h, 0.29 L/h/kg and 46.28μg·h/mL, resp.1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 109-01-3) was used in this study.
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..HPLC of Formula: 109-01-3
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics