Category: piperazines

Volume changes in the proton ionization of amines in water. 1. Morpholines and piperazines was written by Cabani, S.;Mollica, V.;Lepori, L.;Lobo, S. T.. And the article was included in Journal of Physical Chemistry in 1977.Application In Synthesis of Piperazine Dihydrochloride This article mentions the following:

Apparent molar volumes, 桅v, at various concentrations in water at 25掳 of some cyclic bifunctional amines [morpholine, 4-methylmorpholine, piperazine, 1-methyl- and 1,4-dimethylpiperazine, 1,4-diazabicyclo[2.2.2]octane (triethylenediamine)] and their mono- and dihydrochlorides were determined The volume changes 螖V1掳 and 螖V2掳, involved in the 1st and 2nd proton ionizations from the protonated amines, were calculated from the limiting partial molar volumes V虆2掳. The volumes of ionization for the bifunctional cyclic amines were compared with those for the monofunctional amines ad the relationship between entropies and volumes of ionization was examined In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Application In Synthesis of Piperazine Dihydrochloride).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Application In Synthesis of Piperazine Dihydrochloride

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

A multi-residue method by supercritical fluid chromatography coupled with tandem mass spectrometry method for the analysis of chiral and non-chiral chemicals of emerging concern in environmental samples was written by Rice, Jack;Lubben, Anneke;Kasprzyk-Hordern, Barbara. And the article was included in Analytical and Bioanalytical Chemistry in 2020.Synthetic Route of C23H32N6O4S This article mentions the following:

Abstract: This manuscript presents the development, validation and application of a multi-residue supercritical fluid chromatog. coupled with tandem mass spectrometry method for the anal. of 140 chiral and non-chiral chems. of emerging concern in environmental samples, with 81 compounds being fully quant., 14 semi-quant. and 45 qual., validated according to European Medicine Agency (EMA) guidelines (European Medicines Agency 2019). One unified LC-MS method was used to analyze all analytes, which were split into three injection methods to ensure sufficient peak resolution The unified method provided an average of 113% accuracy and 4.5% precision across the analyte range. Limits of detection were in the range of 35 pg L^-1-0.7 渭g L^-1, in both river water and wastewater, with an average LOD of 33 ng L^-1. The method was combined with solid-phase extraction and applied in environmental samples, showing very good accuracy and precision, as well as excellent chromatog. resolution of a range of chiral enantiomers including beta-blockers, benzodiazepines and antidepressants. The method resulted in quantification of 75% of analytes in at least two matrixes, and 56% in the trio of environmental matrixes of river water, effluent wastewater and influent wastewater, enabling its use in monitoring compounds of environmental concern, from their sources of origin through to their discharge into the environment. In the experiment, the researchers used many compounds, for example, 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4Synthetic Route of C23H32N6O4S).

2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Synthetic Route of C23H32N6O4S

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

Reduction of 2,5-dioxopiperazines with lithium aluminum hydride was written by Langenbeck, Wolfgang;Augustin, Manfred;Boehm, Ralf;Hoffmann, Siegfried. And the article was included in Journal fuer Praktische Chemie (Leipzig) in 1964.Synthetic Route of C4H12Cl2N2 This article mentions the following:

2,5-Di-oxopiperazines added to excess LiAlH₄ in dry tetrahydrofuran, the mixture refluxed 165 hrs., the excess LiAlH₄ decomposed with dilute H₂SO₄, the solution extracted with Et₂O, the raffinate alkalinized with KOH and steam-distilled, the distillate acidified with HCl and evaporated, and the residue crystallized from EtOH or EtOH-Et₂O gave the piperazine hydrochlorides (substituents and % yield given): none, 40; 1,4-dimethyl, 62; 1,4-dibenzyl (free base m. 92掳), 57; 3,6-dimethyl, 55; 3,6-dimethyl, 38; 3,6-diisopropyl, 38; and 3,6-diisobutyl, 48 (250 hrs. reflux). In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Synthetic Route of C4H12Cl2N2).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C4H12Cl2N2

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

Homo-PROTAC mediated suicide of MDM2 to treat non-small cell lung cancer was written by He, Shipeng;Ma, Junhui;Fang, Yuxin;Liu, Ying;Wu, Shanchao;Dong, Guoqiang;Wang, Wei;Sheng, Chunquan. And the article was included in Acta Pharmaceutica Sinica B in 2021.Product Details of 548472-68-0 This article mentions the following:

The dose-related adverse effects of MDM2-P53 inhibitors have caused significant concern in the development of clin. safe anticancer agents. Herein we report an unprecedented homo-PROTAC strategy for more effective disruption of MDM2-P53 interaction. The design concept is inspired by the capacity of sub-stoichiometric catalytic PROTACs enabling to degrade an unwanted protein and the dual functions of MDM2 as an E3 ubiquitin ligase and a binding protein with tumor suppressor P53. The new homo-PROTACs are designed to induce self-degradation of MDM2. The results of the investigation have shown that PROTAC 11a efficiently dimerizes MDM2 with highly competitive binding activity and induces proteasome-dependent self-degradation of MDM2 in A549 non-small cell lung cancer cells. Furthermore, markedly, enantiomer 11a-1 exhibits potent in vivo antitumor activity in A549 xenograft nude mouse model, which is the first example of homo-PROTAC with in vivo therapeutic potency. This study demonstrates the potential of the homo-PROTAC as an alternative chem. tool for tumorigenic MDM2 knockdown, which could be developed into a safe therapy for cancer treatment. In the experiment, the researchers used many compounds, for example, 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0Product Details of 548472-68-0).

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Product Details of 548472-68-0

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

Synthesis, molecular docking and biological evaluation of metronidazole derivatives containing piperazine skeleton as potential antibacterial agents was written by Wang, She-Feng;Yin, Yong;Qiao, Fang;Wu, Xun;Sha, Shao;Zhang, Li;Zhu, Hai-Liang. And the article was included in Bioorganic & Medicinal Chemistry in 2014.Related Products of 27469-60-9 This article mentions the following:

Metronidazole has a broad-spectrum antibacterial activity. Hereby a series of novel metronidazole derivatives were designed and synthesized based on nitroimidazole scaffold in order to find some more potent antibacterial drugs. For these compounds which were reported for the first time, their antibacterial activities against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis and Staphylococcus aureus were tested. These compounds showed good antibacterial activities against Gram-pos. strains. One compound represented the most potent antibacterial activity against S. aureus ATCC 25923 with MIC of 0.003 渭g/mL and it showed the most potent activity against S. aureus TyrRS with IC₅₀ of 0.0024 渭M. Mol. docking of one compound into S. aureus tyrosyl-tRNA synthetase active site were also performed to determine the probable binding mode. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Related Products of 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Related Products of 27469-60-9

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

Occurrence and distribution of antibiotics in surface water was written by Liu, Jing;Deng, Wen-Jing;Ying, Guang-Guo;Tsang, Eric P. K.;Hong, Hua-Chang. And the article was included in Ecotoxicology in 2022.COA of Formula: C20H17F2N3O3 This article mentions the following:

The concentrations, distribution, and ecol. risks of 24 typical antibiotics in Hong Kong rivers and seawater were investigated using high-performance liquid chromatog. coupled with electrospray ionization tandem mass spectrometry (UHPLC-EI-MS/MS). The results showed that the select antibiotics were widely distributed in the study area. Among the target antibiotics, the detection rate of tetracyclines (TCs) was 100%, which indicated the widespread use of TCs in Hong Kong. The detection rates of sulfonamides (SAs) (57.1-100%), fluoroquinolones (FQs) (78.6-100%), roxithromycin (RTM) (50%) and novobiocin (NOV) (50%) were all above 50%. Compared with river water (7.9-114.26 ng/L, medium: 27.7 ng/L), concentrations of the most antibiotics in seawater (9.5-32.0 ng/L, medium: 13.3 ng/L) were lower; seawater concentrations were similar to those reported from other coastal cities, such as Guangzhou and Zhuhai in China, which implied that the source of marine antibiotic pollution may be the nearby rivers, and the vastness of the ocean causes environmental dilution of antibiotics. According to the ratio of the measured environmental concentration (MEC) to the predicted no-effect concentration (PNEC), ofloxacin (OFX) (average risk quotient: 1.94E-01) and ciprofloxacin (CFX) (average risk quotient: 3.53E-01) posed medium to high ecol. risk in most places, whereas other antibiotics posed lower risk. In Yuen Long, where there were many livestock farms nearby, the detected concentration of antibiotics was higher, indicating that livestock wastewater may be the major reason for the increase in antibiotic levels in this area. In general, the detected concentration of antibiotics in Hong Kong was lower than that in the United States, Japan, the United Kingdom, and coastal areas of China, but the long-term existence of low concentrations of antibiotics also poses great risks. According to the risk assessment, Hong Kong should pay more attention to the use of FQs (e.g., OFX and CFX) in the future. In the experiment, the researchers used many compounds, for example, 6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8COA of Formula: C20H17F2N3O3).

6-Fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 98105-99-8) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. COA of Formula: C20H17F2N3O3

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

Determination of 50 antibiotic residues in drone pupa powder by liquid chromatography-tandem mass spectrometry was written by Yang, Wenquan;Zhang, Xiaoyan;Yao, Qian;Zhou, Yangjuan;Hu, Yawen;Wang, Maohua;Tang, Maozhi. And the article was included in Sepu in 2019.HPLC of Formula: 113617-63-3 This article mentions the following:

A method was established for the determination of 50 antibiotic residues (macrolides, quinolones, sulfonamides, tetracyclines, nitroimidazoles, lincomycin and chloramphenicol) in drone pupa powder by liquid chromatog.-tandem mass spectrometry (LC-MS/MS). The samples were extracted with perchloric acid and lead acetate solution, and the protein was precipitated The extraction solution was adjusted to pH 8 using dipotassium hydrogen phosphate, and then the solution was purified by solid phase extraction (SPE) and analyzed by LC-MS/MS. The target compounds in the drone pupa powder were determined quant. and quant. by using multiple reaction monitoring and pos. ion or neg. ion modes. The recoveries of the 50 antibiotics were in the range of 70.2-118.3%, and the relative standard deviations (RSDs) were 1.8-13.6%. The method is simple and selective, and can be suitable for the anal. and confirmation of veterinary drug residues in drone pupa powder. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3HPLC of Formula: 113617-63-3).

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.HPLC of Formula: 113617-63-3

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

Cow manure simultaneously reshaped antibiotic and metal resistome in the earthworm gut tract by metagenomic analysis was written by Yang, Fengxia;Wang, Xiaolong;Tian, Xueli;Zhang, Zulin;Zhang, Kai;Zhang, Keqiang. And the article was included in Science of the Total Environment in 2023.Reference of 85721-33-1 This article mentions the following:

Earthworm conversion is an eco-friendly biol. process that converts livestock waste into a benign nutrient-rich organic fertilizer. However, little is known about the impacts of earthworm-converted livestock manure on the antibiotic resistome in the earthworm gut microbiota. Herein, lab-scale vermicomposting was performed to comprehensively evaluate the shift of antibiotic resistance genes (ARGs) in the earthworm gut-feeding on cow manure (CM)-by metagenomic anal. The effects of copper (Cu) as a food addictive were also evaluated. CM substantially enriched the antibiotic resistome in the foregut and midgut, while it decreased in the hindgut. A similar trend was observed for metal resistance genes (MRGs). Notably, Cu in the CM had little effect on composition of ARGs and MRGs in earthworm gut. The earthworm gut microbiome altered by CM was responsible for the shift of ARGs and MRGs. In wormcast, Cu (100 and 300 mg/kg) significantly increased the abundance of ARGs and MRGs. Our study provides valuable insight into the response of ARGs and MRGs to CM in earthworm gut, and underscores the need for the judicious use of heavy metals as feed additives in livestock and poultry farming. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1Reference of 85721-33-1).

1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Reference of 85721-33-1

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

Facilitation of delayed spontaneous alternation behavior in adult rats following early hydroxyzine treatment: differential sensitivity in late infancy was written by Isseroff, Ami. And the article was included in Psychopharmacology (Berlin, Germany) in 1980.Computed Properties of C21H29Cl3N2O2 This article mentions the following:

When tested in adulthood, male rats that had been treated daily with 50 mg/kg hydroxyzine-HCl (I) [2192-20-3] s.c. at 10-29 or 23-29 days of age were facilitated in performance of delayed spontaneous alternation relative to saline-injected rats. Treatment at 10-16 days of age did not produce significant facilitation in the delay task, nor were there any significant differences between groups in spontaneous alternation with no intertrial delay. The facilitative effect may be attributable to anomalies in areas, such as the limbic system, that continue to develop postnatally and mature in late infancy. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Computed Properties of C21H29Cl3N2O2).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Computed Properties of C21H29Cl3N2O2

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

Antimicrobial resistance in clinical Escherichia coli isolated from companion animals in Australia was written by Saputra, Sugiyono;Jordan, David;Mitchell, Tahlia;Wong, Hui San;Abraham, Rebecca J.;Kidsley, Amanda;Turnidge, John;Trott, Darren J.;Abraham, Sam. And the article was included in Veterinary Microbiology in 2017.Product Details of 113617-63-3 This article mentions the following:

Multidrug-resistant (MDR) Escherichia coli have become a major public health concern to both humans and animal health. While the frequency of antimicrobial resistance (AMR) in clin. E. coli is monitored regularly in human medicine, current frequency of AMR in companion animals remains unknown in Australia. In this study we conducted antimicrobial susceptibility testing (AST) and where possible, determined potential risk factors for MDR infection among 883 clin. Escherichia coli isolated from dogs (n = 514), cats (n = 341) and horses (n = 28). AST was undertaken for 15 antimicrobial agents according to the Clin. Laboratory Standards Institute (CLSI) guidelines and interpreted using epidemiol. cut-off values (ECOFFs) as well as CLSI veterinary and human clin. breakpoints. The AST revealed complete absence of resistance to carbapenems while resistance to amikacin was observed at a low level in isolates from dogs (1.6%) and cats (1.5%) compared to horses (10.7%). Among dog isolates, resistance to fluoroquinolones ranged from 9.1%-9.3% whereas among cat isolates, it ranged from 3.2%-5%. Among dog isolates, the proportion showing a 3rd generation cephalosporin (3GC) non-wild type phenotype was significantly higher (P < 0.05) in skin and soft tissue infection (SSTI, n = 122) isolates (17.2%-20.5%) compared to urinary tract infection (UTI, n = 392) isolates (9.9%-10.2%). The frequency of multidrug resistance was 18.1%, 11.7% and 42.9% in dog, cat and horse isolates, resp. Risk factor anal. revealed that MDR E. coli isolated from UTI were pos. associated with chronicity of infection and previous antimicrobial treatment. Dogs and cats with chronic UTI that had been previously treated with antimicrobials were eight times and six times more likely to be infected with MDR E. coli compared to dogs and cats with non-chronic UTI, and no history of antimicrobial treatment, resp. This study revealed that pre-existing disease condition and prior antimicrobial use were the major risks associated with UTI with MDR E. coli in companion animals. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3Product Details of 113617-63-3).

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Product Details of 113617-63-3

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