Category: piperazines

Isolation and characterisation of Pulsatilla Radix-utilising bacteria Pediococcus pentosaceus PR-1 from human faeces. was written by Liu, Yue;Sun, Xiaoxia;Zhang, Jincan;Gao, Feng;Yu, Leilei;Dong, Lina;Zhang, Gangli;Wu, Changxin. And the article was included in FEMS microbiology letters in 2022.Reference of 70458-96-7 The following contents are mentioned in the article:

Although probiotics have been isolated from different sources, few were isolated from traditional Chinese medicine. The current study firstly isolates Pulsatilla Radix-utilising Pediococcus pentosaceus PR-1 from human faeces. Subsequently, the tolerance of PR-1 to low pH, bile salts, simulated gastric juice and succus entericus, antioxidant activity, antimicrobial activity, cholesterol assimilation and antibiotics susceptibility were investigated. After 2 h of incubation at pH 2.0, over 80% of PR-1 survived. The cell viability of PR-1 at 2 h under 0.1% bile salt condition was 99.2%. The survival rate of PR-1 in gastric juice and succus entericus was 64.48% and 81.86%, respectively. Cell-free supernatant of PR-1 culture also showed antimicrobial activity against Escherichia coli, Staphylococcus aureus and Salmonella typhimurium. Besides, antioxidant activity of PR-1 CFS was significantly greater than cell pellet. PR-1 was shown to be resistant to kanamycin, streptomycin, vancomycin and norfloxacin and was able to lower the cholesterol level to 72.5±1.5%. In addition, PR-1 displayed γ-haemolysis and was non-pathogenic. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Reference of 70458-96-7).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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. 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 70458-96-7

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

Comprehensive survey and health risk assessment of antibiotic residues in freshwater fish in southeast China was written by Hua, Yongyou;Yao, Qinghua;Lin, Jian;Li, Xi;Yang, Yan. And the article was included in Journal of Food Composition and Analysis in 2022.Category: piperazines The following contents are mentioned in the article:

To assess the health risks from antibiotic residues in freshwater fish, this study analyzed residues of 65 antibiotics in 10 freshwater fish species sampled in southeast China. Eight antibiotics were detected by UPLC-MS/MS at an overall detection rate of 53.9 %, with 3.48 % of samples exceeding MRLs and 13.0 % suggesting the misuse of human antibiotics. Quinolones, particularly enrofloxacin, were the most frequently detected residues. Azithromycin, an antibiotic intended only for human use, was detected at a rate of 14.8 % at concentrations up to 453.1 μg/kg. Antibiotic residues varied in category and concentration across freshwater fish species. Residues were detected in benthic predatory fish at higher levels than in middle or upper omnivorous or herbivorous fish. Estimated daily intakes showed that the consumption of cultured fish from this region does not pose a serious risk to human health, the hazard index being less than one. However, these findings suggest that the abuse of antibiotics in aquaculture is still a problem, and more attention should be paid to their residues in fish to enhance food safety. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Category: piperazines).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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.Category: piperazines

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

High-throughput screening of 756 chemical contaminants in aquaculture products using liquid chromatography/quadrupole time-of-flight mass spectrometry was written by Bai, Mingkai;Tang, Ruixue;Li, Guorong;She, Wenhai;Chen, Gangjun;Shen, Hongmei;Zhu, Suqin;Zhang, Hongwei;Wu, Haohao. And the article was included in Food Chemistry: X in 2022.Related Products of 70458-96-7 The following contents are mentioned in the article:

A high-throughput screening method embracing 756 multiclass chem. contaminants in aquaculture products was developed using modified QuEChERS extraction coupled with liquid chromatog./quadrupole time-of-flight mass spectrometry. A mega-database with retention time/accurate mass data for 524 pesticides, 182 veterinary drugs, 32 persistent organic pollutants and 18 marine toxins was established for compound identification via retrospective library searching. In the four representative matrixes (muscle tissues of tilapia and grouper, and edible portions of oyster and scallop), all the database compounds showed acceptable recovery and repeatability with the screening detection limit and limit of quantification below 0.01 mg/kg for >90% of them. The matrix-matched calibration revealed acceptable quant. property of the method in terms of linear range, linearity, and matrix effect, and fish muscle samples showed stronger matrix effect than shellfish samples. Anal. of 64 real-life samples from aquaculture farms and retail markets evidenced applicability of the proposed method to high-throughput screening scenarios. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Related Products of 70458-96-7).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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 70458-96-7

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

Facile synthesis of surface functionalized Pd²⁺@P-CDP/COFs for highly sensitive detection of norfloxacin drug based on the host-guest interaction was written by Zhang, Cong;Fan, Limin;Ren, Jujie;Cui, Min;Li, Na;Zhao, Haiyan;Qu, Yihang;Ji, Xueping. And the article was included in Journal of Pharmaceutical and Biomedical Analysis in 2022.Product Details of 70458-96-7 The following contents are mentioned in the article:

In this work, β-cyclodextrin porous polymers (P-CDPs) functionalized novel covalent organic frameworks (P-CDPs/COFs) were synthesized by a simple and facile method. After combined with Pd²⁺ via electrostatic interaction, the Pd²⁺@P-CDPs/COFs nanocomposites were prepared and utilized as novel electrode materials to fabricate the non-enzyme electrochem. sensors for high-sensitivity detection of Norfloxacin (NF). Due to the host-guest recognition, excellent adsorption performance and catalytic performance of Pd²⁺@P-CDPs/COFs, the prepared sensor exhibited excellent electrochem. performance for detecting NF under the optimum conditions, which showed two linear ranges of 0.08-7.0 μM and 7.0-100.0 μM with a low detection limit of 0.031 μM (S/N = 3). Addnl., the obtained sensor has also been successfully applied to measure NF with satisfactory results in the real medicinal samples of NF eye-drops. Our findings paved the way for the development of COFs-based sensing platform in drug anal. and testing for human health, food security and the quality control of drugs. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Product Details of 70458-96-7).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Product Details of 70458-96-7

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

Development and validation of RP-HPLC method for the estimation of nintedanib esylate in bulk and its formulation was written by Patil, Rohan S.;Mahajan, Moreshwar P.. And the article was included in Research & Reviews: A Journal of Pharmaceutical Science in 2018.Synthetic Route of C33H39N5O7S The following contents are mentioned in the article:

A review. A simple, precise, reliable, rapid and reproducible reversed-phase high performance liquid chromatog. method (RP-HPLC) method has was developed and validated for the estimation of Nintedanib Esylate. Chromatog. was carried out with anal. technol. HPLC system consisted of UV-3000-M detector on C18 (4.6×250 mm, 5μ) column with a mobile phase composed of methanol:water (80:20 volume/volume) at a flow rate of 1 mL/min. The pH of the mobile phase was adjusted by 0.05% ortho phosphoric acid (pH-3). Detection was carried out using a UV detector at 287 nm. Parameters such as linearity, precision, accuracy, ruggedness, robustness, LOD and LOQ were studied as per the ICH Q2 (R1) guidelines. The retention time was found to be 4.67 min. The linearity range for Nintedanib esylate was 10-60μg/mL. The correlation coefficient was found to be 0.999. Developed method was found to be accurate, precise, selective and rapid for estimation of Nintedanib esylate in pharmaceutical dosage form. The proposed method can be useful in quality control of bulk manufacturing and pharmaceutical dosage form. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Synthetic Route of C33H39N5O7S).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Synthetic Route of C33H39N5O7S

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

Development and evaluation of cost effective formula of nintedanib esylate soft gelatin capsule and compare with prepared product similar to innovator was written by Gaikwad, Sonal S.;Singh, Meera C.. And the article was included in Research & Reviews: A Journal of Pharmaceutical Science in 2018.HPLC of Formula: 656247-18-6 The following contents are mentioned in the article:

Nintedanib esylate was invented by Boehringer Ingelheim Pharmaceuticals. Nintedanib esylate is an organosulfonate salt obtained by combination of Nintedanib with ethane sulfonic acid. It’s a kinase inhibitor used for the treatment of idiopathic pulmonary fibrosis and non-small cell lung cancer. Bioavailability and water solubility of Nintedanib esylate is very low and BCS class is not mentioned in the literature. Due to poor solubility of Nintedanib esylate at neutral conditions, the active substance cannot be formulated as solution and therefore innovator has prepared soft gelatin capsule with oil base i.e. suspended in a lipophilic fill mix. Innovator’s product (Ofev) is not available in India, so in this research, we first prepared innovator’s product (Derived on the basis of literature) and then prepared product similar to innovator’s product which is cost effective. For evaluation of product, in-vitro anal. data was compared with data available for innovator’s product literature. The product similar to innovator was successfully developed and compared with available literature. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6HPLC of Formula: 656247-18-6).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.HPLC of Formula: 656247-18-6

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

Reproductive toxicities of ofloxacin and norfloxacin on Caenorhabditis elegans with multi-generational oscillatory effects and trans-generational residual influences was written by Zhang, Jing;Zheng, Yungu;Yu, Zhenyang. And the article was included in Environmental Toxicology and Pharmacology in 2022.Safety of 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid The following contents are mentioned in the article:

The reproductive toxicities over generations are essential to assess the long-term impacts environmental fluoroquinolone antibiotics (FQs). In the present study, the multi-generational effects of ofloxacin (OFL) and norfloxacin (NOR) on reproduction were studied on Caenorhabditis elegans from 9 successive generations (F1-F9). Results showed that OFL showed no effects in F1, stimulation in F2 to F4, and inhibition F5 to F9. The effects of NOR also showed oscillation between stimulation and inhibition across generations. Further biochem. anal. demonstrated that the reproductive toxicities of OFL and NOR were more closely connected with total cholesterol (TCHO), progesterone (P) and testosterone (T), than major sperm protein (MSP) and vitellogenin (Vn). Moreover, OFL and NOR also showed significant trans-generational reproductive toxicities in T4 and T4′, the great-grand-daughter of F1 and F9. Differences between T4 and T4′ and between OFL and NOR, indicated influences of multi-generational exposure and urged more exploration on different mechanisms between FQs. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Safety of 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) belongs to piperazine derivatives. 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. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Safety of 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid

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

Pyrimidine-conjugated fluoroquinolones as new potential broad-spectrum antibacterial agents was written by Tan, Yi-Min;Li, Di;Li, Fen-Fen;Fawad Ansari, Mohammad;Fang, Bo;Zhou, Cheng-He. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2022.Product Details of 70458-96-7 The following contents are mentioned in the article:

Pyrimidine-conjugated fluoroquinolones were constructed to cope with the dreadful resistance. Most of the target pyrimidine derivatives effectively suppressed the growth of the tested strains, especially, 4-aminopyrimidinyl compound 1c showed a broad antibacterial spectrum and low cytotoxicity and exhibited superior antibacterial potency against Enterococcus faecalis with a low MIC of 0.25 μg/mL to norfloxacin and ciprofloxacin. The active compound 1c with fast bactericidal potency could inhibit the formation of biofilms and showed much lower trend for the development of drug-resistance than norfloxacin and ciprofloxacin. Further exploration revealed that compound 1c could prompt ROS accumulations in bacterial cells and interact with DNA to form a DNA-1c complex, thus facilitating bacterial death. ADME anal. indicated that compound 1c possessed favorable drug-likeness and promising pharmacokinetic properties. These results demonstrated that pyrimidine-conjugated fluoroquinolones held hope as potential antibacterial candidates and deserve further study. This study involved multiple reactions and reactants, such as 1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7Product Details of 70458-96-7).

1-Ethyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 70458-96-7) 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. 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.Product Details of 70458-96-7

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

Solubility measurement and thermodynamic properties of Nintedanib Esylate Hemihydrate in pure solvents was written by Ma, Jinju;Huang, Jingyi;Cao, Zidan;Sha, Jiao;Sun, Renren;He, Haixia;Wan, Yameng;Li, Yu;Li, Tao;Ren, Baozeng. And the article was included in Journal of Molecular Liquids in 2022.Category: piperazines The following contents are mentioned in the article:

The thermodn. property of NE crystallization in 10 pure solvents was studied, and the solid-liquid equilibrium solubility of NE in these ten solvents was determined by laser dynamic method. The result showed that the solubility was proportional to the temperature Five models including the modified Apleblat model, λh model, Polynomial model, Van’t Hoff model, and Yaws model were adopted to fit the solubility of the solute in a single solvent, and the result showed that the Polynomial model had a high fitting degree for the solubility of NE in the single solvent chosen. The activity coefficients, as well as thermodn. properties of the mixing, were obtained and studied. The effect of solvents themselves on the solubility order of Nintedanib Esylate was also studied by correlating to the solubility of Nintedanib Esylate through the KAT-LSER model. What is more, by adopting Mol. Dynamic simulation, it was proved that the Nintedanib Esylate solubility in different solvents could be largely influenced by the interaction of the solute mols. and solvent mols. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Category: piperazines).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. 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. 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.Category: piperazines

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

Nanostructured lipid carriers as oral delivery systems for improving oral bioavailability of nintedanib by promoting intestinal absorption was written by Zhu, Yunjing;Liang, Xue;Lu, Cong;Kong, Yihan;Tang, Xing;Zhang, Yu;Yin, Tian;Gou, Jingxin;Wang, Yanjiao;He, Haibing. And the article was included in International Journal of Pharmaceutics in 2020.HPLC of Formula: 656247-18-6 The following contents are mentioned in the article:

The aim of this study was to fabricate nanostructured lipid carriers, NLCs, of nintedanib (BIBF) to improve its oral bioavailability. Two types of NLCs loaded with BIBF (BIBF-NLCs-1 and BIBF-NLCs-2) were prepared by the melt-emulsification technique. BIBF-NLCs-1 and BIBF-NLCs-2 showed nanoscale particle sizes of 142.70 ± 0.85 nm and 7.99 ± 0.06 nm, and both were pos. zeta potential. Study on Caco-2 cells showed that BIBF-NLCs-1 exhibited distinct advantages at the cytol. level. The oral bioavailability of BIBF-NLCs-1 and BIBF-NLCs-2 was extremely improved 3.13-fold and 2.39-fold resp. compared with BIBF solution (BIBF-Sol). And in vivo anti-tumor efficiency study in mice bearing LLC lung tumor indicated that BIBF-NLCs-1 and BIBF-NLCs-2 had excellent tumor inhibition. Besides, the two NLCs did not increase the risk of liver damage and can even reduce the incidence of gastrointestinal irritation of BIBF to some extent. In summary, NLCs are a potential oral delivery system to improve the bioavailability of BIBF by promoting intestinal absorption. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6HPLC of Formula: 656247-18-6).

(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.HPLC of Formula: 656247-18-6

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