Category: piperazines

Synthetic Route of 16153-81-4, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 16153-81-4, Name is 4-(4-Methylpiperazin-1-yl)phenylamine, SMILES is NC1=CC=C(N2CCN(C)CC2)C=C1, belongs to piperazines compound. In a article, author is Muresan-Pop, M., introduce new discover of the category.

Structural characterization of 5-fluorouracil & piperazine new solid forms and evaluation of their antitumor activity

A salt (FP-S) and two co-crystals (FP-C1 and FP-C2) of fluorouracil (FU) with piperazine (PZ) were investigated in terms of bioavailability and their effect on endothelial cells. From structural point of view, the best stability was observed for FP-C2 sample obtained by storage of FP-C1 sample under extreme conditions of temperature and humidity. This result was explained by the strong intermolecular interactions between 5-fluorouracil, piperazine and water, as denoted by the crystallographic analysis of FP-C2 form. Dissolution measurements in water indicate that the most soluble form is the salt, with a dissolution rate about 3 times greater than for the fluorouracil pure compound, while the solubility for co-crystals decreases compared to FU. Toxicity and antitumoral effect of the synthesized compounds were checked on three different cell lines: normal cells (HUVEC endothelial cells) and tumor cells (DLD-1 and HT29, both colorectal adenocarcinoma) and cytotoxicity by the MTT assay and cell proliferation assay. It has been found that the FP-C1 exerts a selective cytotoxic effect on HT29 cells and FP-C2 on DLD-1 cells in contrast to normal endothelial cell line resistance. For FU and FP-S salt, the effect on normal and tumoral cells is similar. The comparative study of the three fluorouracil forms shows that the best antitumor selective response was obtained for the co-crystal forms. (C) 2020 Elsevier B.V. All rights reserved.

Synthetic Route of 16153-81-4, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 16153-81-4 is helpful to your research.

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

In an article, author is Noorbasha, Khaleel, once mentioned the application of 130307-08-3, Name is 1-(4-Bromophenyl)-4-methylpiperazine, molecular formula is C11H15BrN2, molecular weight is 255.1542, MDL number is MFCD09029689, category is piperazines. Now introduce a scientific discovery about this category, Quality Control of 1-(4-Bromophenyl)-4-methylpiperazine.

Determination of residual solvents in paclitaxel by headspace gas chromatography

Background: A simple and sensitive gas chromatographic method was developed and validated for the simultaneous determination of methanol, ethanol, acetone, isopropyl alcohol, dichloromethane, N-hexane, ethyl acetate, tetrahydrofuran, and N,N-diisopropyl ethyl amine in Paclitaxel. A chromatographic separation was done on DB-624 column, 30m length x0.53mm ID, and film thickness 3 mu m, using a flame ionization detector (FID) with gradient column oven temperature program. The injection was carried out in split mode, with a split ratio of 5:1. A mixture of N-methyl-2-pyrrolidinone (contains 1% piperazine) and water in the ratio of 80:20 (v/v) was selected as a diluent to obtain good sensitivity along with the recovery. Results: The developed gas chromatographic method offers symmetric peak shape, good resolution of more than 2.0 between the solvent peaks, and the relative standard deviation for replicate injections of all the solvents were found to be not more than 15.0% with reasonable retention time for all the solvents. The limit of detection for methanol, ethanol, acetone, isopropyl alcohol, dichloromethane, N-hexane, ethyl acetate, tetrahydrofuran, and N,N-diisopropyl ethyl amine was found to be 304.69ppm, 497.98ppm, 498.99ppm, 504.49ppm, 61.81ppm, 30.07ppm, 505ppm, 73.05ppm, and 2.09ppm, respectively. Limit of quantitation of methanol, ethanol, acetone, isopropyl alcohol, dichloromethane, N-hexane, ethyl acetate, tetrahydrofuran, and N,N-diisopropyl ethyl amine was found to be 89.62ppm, 146.47ppm, 146.76ppm, 148.38ppm, 18.18ppm, 8.84ppm, 148.53ppm, 21.49ppm, and 0.62ppm, respectively. Precision was found to be satisfactory. Linear in the range of LOQ to 150% level for all the solvents, and accuracy along with robustness, is performed, and acceptable results were obtained. Conclusion: The proposed method was demonstrated to be simple, sensitive, specific, linear, precise, accurate, and robust, hence can be used to determine the residual organic solvents in Paclitaxel drug substance and drug product.

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

109-01-3, Name is 1-Methylpiperazine, molecular formula is C5H12N2, belongs to piperazines compound, is a common compound. In a patnet, author is Kurutos, Atanas, once mentioned the new application about 109-01-3, Safety of 1-Methylpiperazine.

Near-infrared pH responsive heptamethine cyanine platforms: Modulating the proton acceptor

In this report, we wish to present the rational design, synthesis, and study of optical characteristics of near-infrared (NIR) molecular probes emitting over 800 nm. The title pH sensing platforms consist of a piperazine moiety serving as a hydronium ion receptor, coupled with a rigidified symmetric heptamethine backbone. The spectrally fine-tuned response of the fluorophores was studied in both organic solvents and aqueous buffer solutions, employing combined UV-Vis and steady state fluorimetric techniques. In parallel, computational approach and optical spectroscopy were employed aiming to ascribe the origin of spectral behavior of the amino-substituted heptamethines. Herein, we also investigated the halochromic effect of the differently substituted piperazines on the spectral properties of the NIR cyanine dyes. Under acidic conditions, the protonation of the piperazine moiety promoted a gradual bathochromic shift in the absorption spectra. The Delta lambda between the neutral and the protonated forms are indirectly related to the modifications applied to the proton acceptor. The calculated pK(a) values (5.13-7.06) were found to be dependent on the dye chemical structure. A good linear correlation was established between the pK(a) of the newly synthesized dyes and that of the reported piperazine moieties. This aspect allows the future expansion of the current facile strategy since sensing chromophores with predicted pH response could readily be designed based on pK(a) databases for substituted piperazine derivatives. A detailed literature study along with NMR and computational methods were found to be in agreement with our assumption, that both nitrogen atoms of the 1,4-disubstituted amine are involved in the sensing process. The covered pK(a) range allows us to recommend the title fluorophores as promising potential candidates for qualitative analysis of biological samples. A cytotoxicity study by the MTT assay showed that the NIR dyes are safe and applicable for bioanalytical purposes at dye concentrations up to 10 mu M. Fluorescence imaging and cellular applications, including staining and visualization of HeLa cervical cancer cells was successfully demonstrated.

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

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 130307-08-3, Name is 1-(4-Bromophenyl)-4-methylpiperazine, molecular formula is C11H15BrN2, belongs to piperazines compound. In a document, author is Vinarov, Zahari, introduce the new discover, Quality Control of 1-(4-Bromophenyl)-4-methylpiperazine.

Solubilization of itraconazole by surfactants and phospholipid-surfactant mixtures: interplay of amphiphile structure, pH and electrostatic interactions

Although surfactants are frequently used in enabling formulations of poorly water-soluble drugs, the link between their structure and drug solubilization capacity is still unclear. We studied the solubilization of the brick-dust molecule itraconazole by 16 surfactants and 3 phospholipid:surfactant mixtures. NMR spectroscopy was used to study in more details the drug-surfactant interactions. Very high solubility of itraconazole (up to 3.6 g/L) was measured in anionic surfactant micelles at pH = 3, due to electrostatic attraction between the oppositely charged (at this pH) drug and surfactant molecules. H-1 NMR spectroscopy showed that itraconazole is ionized at two sites (2+ charge) at these conditions: in the phenoxy-linked piperazine nitrogen and in the dioxolane-linked triazole ring. The increase of amphiphile hydrophobic chain length had a markedly different effect, depending on the amphiphile type: the solubilization capacity of single-chain surfactants increased, whereas a decrease was observed for double-chained surfactants (phosphatidylglycerols). The excellent correlation between the chain melting temperatures of phosphatidylglycerols and itraconazole solubilization illustrated the importance of hydrophobic chain mobility. This study provides rules for selection of itraconazole solubilizers among classical single-chain surfactants and phospholipids. The basic physics underpinning the described effects suggests that these rules should be transferrable to other brick-dust molecules.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 130307-08-3. Quality Control of 1-(4-Bromophenyl)-4-methylpiperazine.

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

Reference of 109-01-3, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 109-01-3, Name is 1-Methylpiperazine, SMILES is CN1CCNCC1, belongs to piperazines compound. In a article, author is Lee, Yi-Tzu, introduce new discover of the category.

AdeABC Efflux Pump Controlled by AdeRS Two Component System Conferring Resistance to Tigecycline, Omadacycline and Eravacycline in Clinical Carbapenem Resistant Acinetobacter nosocomialis

Carbapenem-resistant Acinetobacter nosocomialis (CRAn) is a significant public health concern. Tigecycline non-susceptible CRAn (Tn-CRAn) isolates have emerged worldwide. Tigecycline resistance is mainly related to the overexpression of AdeABC efflux pump controlled by AdeRS two-component system (TCS). Two novel tetracycline derivatives, omadacycline and eravacycline, may present a treatment option for CRAn. This study investigated the in vitro antimicrobial activity of tigecycline, omadacycline and eravacycline against clinical CRAn isolates and the contribution of efflux pumps in their resistance. Eighty-nine clinical CRAn isolates, including 57 Tn-CRAn isolates were evaluated for minimum inhibitory concentrations (MICs) by the broth microdilution. The relationship between the antimicrobial resistance and efflux pump expression was assessed by their responses to the efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine (NMP). The contribution of the AdeABC efflux pump in their resistance was determined by the complementation of the AdeRS two-component system in wild-type, adeRS operon and adeB gene knockout strains. Among the 89 isolates, omadacycline and eravacycline MICs were correlated closely with those of tigecycline. They demonstrated improved potency, based on MIC90 values, by showing a 4 to 8-fold greater potency than tigecycline. The synergetic effects of tigecycline, omadacycline and eravacycline with NMP were observed in 57 (100%), 13 (22.8%), and 51 (89.5%) of Tn-CRAn isolates, respectively. Further analysis showed that the laboratory strain carrying the Type 1 adeRS operon increased the tigecycline, omadacycline and eravacycline MICs by 4-8-folds, respectively. Eravacycline demonstrated improved potency over tigecycline against populations of CRAn, including Tn-CRAn isolates. The over-expression of AdeABC efflux pumps was directly activated by the AdeRS two-component system and simultaneously reduced the susceptibilities of tigecycline, eravacycline, and omadacycline. Omadacycline and eravacycline MICs were correlated closely with those of eravacycline.

Reference of 109-01-3, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 109-01-3 is helpful to your research.

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

Application 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 Lee, Jae Won, introduce new discover of the category.

Nitrogen-Bearing Carbon Nanoparticles by Pyrolytic Decomposition of Piperazine Citrate Macromolecules for Cellular Imaging

In this work, highly photoluminescent carbon nanoparticles (CNPs) are fabricated by pyrolytic decomposition of piperazine citrate at high pressure and high temperature. Piperazine serves as a hydrolytic, surface-passivating, and N-doping agent, facilitating the formation of a photopolymer. The as-synthesized CNPs, without any surface protection/passivation, exhibit excellent photoluminescence and a maximum quantum yield of 84%. The average particle size of the N-doped CNPs is 0.89 +/- 0.05 nm. In addition, the N-doped CNPs exhibit uniform diameters and nearly spherical shapes. The X-ray photoelectron spectroscopy results reveal that the CNPs are composed of carbon (64.4 wt%), oxygen (18.5 wt%), and nitrogen (17.1 wt%), indicating the presence of nitrogen-doped and carbon-rich moieties in the CNPs. Notably, the CNPs purified by the procedure developed in this work exhibit more stable luminescence properties than those purified with the conventional dialysis membrane. In addition, the potential application of the CNPs as fluorescent bioimaging probes, which offer a broad dosing window and exhibit multicolor emission, is investigated by directly culturing A549 cells with the CNPs. The results reveal that the CNPs exhibit not only exceptional optical stability, but also outstanding biocompatibility and cell labeling capability. After incubating the A549 cells with CNPs, the CNPs are confined in perinuclear vacuole-similar shapes with a granulated form in cytoplasm preserving the nucleus. Notably, no significant morphological deterioration such as nuclear contraction is detected.

Application 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. I hope my blog about 300543-56-0 is helpful to your research.

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

Chemistry, like all the natural sciences, begins with the direct observation of nature¡ª in this case, of matter.139755-85-4, Name is 5-(2-Ethoxy-5-((4-(2-hydroxyethyl)piperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one, SMILES is O=C1C(N(C)N=C2CCC)=C2N=C(C3=CC(S(=O)(N4CCN(CCO)CC4)=O)=CC=C3OCC)N1, belongs to piperazines compound. In a document, author is Lee, Yunje, introduce the new discover, Formula: C23H32N6O5S.

Operation of a Pilot-Scale CO2 Capture Process with a New Energy-Efficient Polyamine Solvent

A new blending recipe of a polyamine-based solvent for capturing post-combustion CO2 was proposed, and its performance and characteristics were investigated using a pilot-scale carbon capture process (PCCP). The proposed solvent is a blend of three types of amines and was designed to separate the solvent roles into those of a main amine, auxiliary amine, and reaction-rate-enhancing amine. Polyamine 3,3 ‘-iminobis (N, N-dimethylpropylamine) was selected as the main amine given its ability to capture large amounts of CO2. 2-Amino-2-methyl-1-propanol was used as the auxiliary amine, with piperazine added as the reaction-rate-enhancing amine. This solvent was tested in a PCCP that can handle 150 Nm(3)/h of flue gas. The proposed solvent was found to operate stably while consuming substantially lower reboiler duty than the monoethanolamine (MEA) 30 mass% solvent.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 139755-85-4 is helpful to your research. Formula: C23H32N6O5S.

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

Chemistry, like all the natural sciences, COA of Formula: C8H18N2O6S2, begins with the direct observation of nature¡ª in this case, of matter.5625-37-6, Name is 2,2′-(Piperazine-1,4-diyl)diethanesulfonic acid, SMILES is O=S(CCN1CCN(CCS(=O)(O)=O)CC1)(O)=O, belongs to piperazines compound. In a document, author is Fang, Heting, introduce the new discover.

Ciprofloxacin-degrading Paraclostridium sp. isolated from sulfate-reducing bacteria-enriched sludge: Optimization and mechanism

Ciprofloxacin (CIP), one of the most widely used fluoroquinolone antibiotics, is frequently detected in the effluents of wastewater treatment plants and aquatic environments. In this study, a CIP-degrading bacterial strain was isolated from the sulfate reducing bacteria (SRB)-enriched sludge, identified as Paraclostridium sp. (i.e., strain S2). The effects of critical operational parameters on CIP removal by the strain S2 were systematically studied and these parameters were optimized via response surface methodology to maximize CIP removal. Furthermore, the pathway and kinetics of CIP removal were investigated by varying the initial CIP concentrations (from 0.1 to 20 mg/L). The CIP removal was characterized by rapid sorption followed by biotransformation with a specific biotransformation rate of 1975.7 +/- 109.1 mu g/g-cell dry weight/h at an initial CIP concentration of 20 mg/L. Based on the main transformation products, several biotransformation pathways have been proposed including piperazine ring cleavage, OH/F substitution, decarboxylation, and hydroxylation as the major transformation reactions catalyzed by cytochrome P450 and dehydrogenases. Acute toxicity assessment apparently shows that CIP biotransformation by strain S2 resulted in the formation of less toxic intermediates. To the best of our knowledge, this is the very first study in which a key functional microbe, Paraclostridium sp., highly effective in CIP biotransformation, was isolated from SRB-enriched sludge. The findings of this study could facilitate in developing appropriate bioaugmentation strategy, and in designing and operating an SRB-based engineered process for treating CIP-laden wastewater. (C) 2021 Elsevier Ltd. All rights reserved.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 5625-37-6. COA of Formula: C8H18N2O6S2.

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

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 841-77-0, Name is 1-Benzhydrylpiperazine, SMILES is N1(C(C2=CC=CC=C2)C3=CC=CC=C3)CCNCC1, belongs to piperazines compound. In a document, author is Liu, Lixin, introduce the new discover, Recommanded Product: 1-Benzhydrylpiperazine.

Pharmaceutical salts/cocrystals of enoxacin with dicarboxylic acids: Enhancing in vitro antibacterial activity of enoxacin by improving the solubility and permeability

Base on improving the solubility and permeability of enoxacin (EX) to enhance the antibacterial activity in vitro, three new pharmaceutical salts/cocrystals of EX with oxalic acid (EX center dot 0.5(C2H2O4)center dot 2(H2O)), malonic acid ((HEX)center dot C3H3O4) and fumaric acid ((HEX)center dot C4H3O4) have been designed, synthesized and characterized. Comprehensive analysis structure and Hirshfeld surface reveal that the hydrogen bonds/CAHBs formed by the N atom in the piperazine ring from EX molecule with the carboxylic acid group in the coformer could form a stable crystal structure. It is universally acknowledged that improving the solubility of the EX (BCS class II) to make it a BCS class I drug would obtain a Bioequivalence of immunity to the drug trial. The solubilities of three pharmaceutical salts/cocrystals of EX with dicarboxylic acids are consistent with expectation that they are dramatically improved in pure water than pure enoxacin, and the solubility order of three pharmaceutical salts/ cocrystals of EX is consistent with coformers solubility. The permeabilities of three pharmaceutical salts/cocrystals of EX are improved compared with the pure enoxacin, and the variation tendency is consistent with the solubilities of three pharmaceutical salts/cocrystals of EX. In addition, the antibacterial activities in vitro of three pharmaceutical salts/cocrystals of EX are improved compared with the corresponding parent compound (EX), which change the order is consistent with the solubility and permeability. Simultaneously, the hygroscopic stabilities of three pharmaceutical salts/cocrystals are surpassing pure EX, and the hygroscopic stability of molecular cocrystal EX-OXA is better than ionic cocrystal EX-MLO and EX-FUM. This implies that preparation of the pharmaceutical salts/cocrystals of EX with oxalic acid, malonic acid and fumaric acid could not only enhance the antibacterial activity of EX, which base on improving the solubility and permeability of EX, but also improve the hygroscopic stability of EX.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 841-77-0 is helpful to your research. Recommanded Product: 1-Benzhydrylpiperazine.

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

Chemistry is an experimental science, Application In Synthesis of 1-(4-Bromophenyl)-4-methylpiperazine, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 130307-08-3, Name is 1-(4-Bromophenyl)-4-methylpiperazine, molecular formula is C11H15BrN2, belongs to piperazines compound. In a document, author is Liu, Zhenxing.

AIE-based nanoaggregate tracker: high-fidelity visualization of lysosomal movement and drug-escaping processes

High-fidelity imaging and long-term visualization of lysosomes are crucial for their functional evaluation, related disease detection and active drug screening. However, commercial aggregation-caused quenching probes are not conducive to precise lysosomal imaging because of their inherent drawbacks, like easy diffusion, short emission and small Stokes shift, let alone their long-term tracing due to rapid photobleaching. Herein we report a novel aggregation-induced emission (AIE)-based TCM-PI nanoaggregate tracker for direct visualization of lysosomes based on the building block of tricyano-methylene-pyridine (TCM), wherein introduced piperazine (PI) groups behave as targeting units to lysosomes upon protonation, and the self-assembled nanostructure contributes to fast endocytosis for enhanced targeting ability as well as extended retention time for long-term imaging. The piperazine-stabilized TCM-PI nanoaggregate shifts the emission maximum to 677 nm in an aqueous environment, and falls within the desirable NIR region with a large Stokes shift of 162 nm, thereby greatly reducing biological fluorescent background interference. In contrast with the commercially available LysoTracker Red, the essential AIE characteristic of high photostability can guarantee three-dimensional high-fidelity tracing with low photobleaching, and little diffusion from lysosomes, and especially overcome the AIE bottleneck to target specificity. Consequently, the AIE-based nanoaggregate tracker successfully achieves the high-fidelity and long-term tracing of lysosomal movement and even monitors the drug-escaping process from lysosomes to cell nuclei, which provides a potential tool to benefit drug screening.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 130307-08-3. Application In Synthesis of 1-(4-Bromophenyl)-4-methylpiperazine.

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