The piperazines are a broad class of chemical compounds, many with important pharmacological properties, which contain a core piperazine functional group. 103-76-4, formula is C6H14N2O, Name is N-(2-Hydroxyethyl)piperazine. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Synthetic Route of 103-76-4.
Lei, Hongrui;Cao, Zhi;Wu, Huinan;Li, Tong;Wang, Xinyu;Chen, Yuxiang;Ma, Enlong;Sun, Lixin;Zhai, Xin research published 《 Structural and PK-guided identification of indole-based non-acidic autotaxin (ATX) inhibitors exhibiting high in vivo anti-fibrosis efficacy in rodent model》, the research content is summarized as follows. In recent decades, pharmacol. targeting of the autotaxin (ATX)/lysophosphatidic acid (LPA) axis accounted for excellent disease management benefits. Herein, to extend the scope of structure-activity relationships (SARs), fifteen indole-based carbamate derivatives I [R = 4-Me, 3,4-difluoro, 2,3-dichloro; R1 = pyrrolidin-1-yl, (4-methyl-1-piperidyl), (4-methylpiperazin-1-yl); R2 = H, CH3, etc] were prepared to evaluate the ATX inhibitory potency. Among them, compound I [R = 3,5-dichloro; R1 = morpholino; R2 = H] bearing morpholine moiety was identified as the optimal ATX inhibitor (0.41 nM), superior to the pos. control GLPG1690 (2.90 nM). To resolve the intractable issue of poor pharmacokinetic (PK) property, urea moiety was introduced as a surrogate of carbamate which furnished compounds II [R3 = morpholino, (4-hydroxy-1-piperidyl), [2-(hydroxymethyl)pyrrolidin-1-yl]; R4 = H, 4-Cl, 4-F, etc]. The dedicated modification identified the diethanolamine entity II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] with satisfactory water solubility and PK profiles with a min. sacrifice of ATX inhibition (2.17 nM). The most promising candidate II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] was evaluated for anti-fibrosis effect in a bleomycin challenged mice lung fibrosis model. Upon treatment with II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)], the in vivo ATX activity in both lung homogenate and broncheoalveolar fluid (BALF) sample was significantly down-regulated. Furthermore, the gene expression of pro-fibrotic cytokines transforming growth factor-β (TGF-β), interleukin- 6 (IL-6) and tumor necrosis factor-α (TNF-α) in lung tissue was reduced to normal level. Collectively, the promising biol. effects may advocate potential application of II [R3 = [bis(2-hydroxyethyl)amino]; R4 = (3-chloro-4-methoxy-phenyl)] in fibrosis relevant diseases.
103-76-4, 1-(2-Hydroxyethyl)piperazine is a useful research compound. Its molecular formula is C6H14N2O and its molecular weight is 130.19 g/mol. The purity is usually 95%.
1-(2-Hydroxyethyl)piperazine is a chemical solvent that is used for the absorption of amines and other compounds. It has been shown to have a high affinity for acidic substances, which may be due to its ability to form hydrogen bonds with them. 1-(2-Hydroxyethyl)piperazine is also used in sample preparation for the analysis of amines and other compounds in fruit extracts. The solubility of 1-(2-Hydroxyethyl)piperazine depends on the experimental conditions, including pH, temperature, and pressure. FT-IR spectroscopy has been used to measure the vibrational modes of 1-(2-Hydroxyethyl)piperazine molecules. The IR spectrum revealed that this compound contains a hydroxyl group and two fatty acid chains with one or more hydroxyl groups at their terminal end. The nmr spectrum showed that 1-(2-Hydroxyethyl)piperazine contains an NH proton as well as, Synthetic Route of 103-76-4
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics