Month: March 2021

Electric Literature of 147081-29-6, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 147081-29-6, Name is (S)-tert-Butyl 3-methylpiperazine-1-carboxylate, SMILES is O=C(N1C[C@H](C)NCC1)OC(C)(C)C, belongs to piperazines compound. In a article, author is Manouchehrizadeh, Elham, introduce new discover of the category.

Design, Synthesis, Molecular Docking and Biological Activity of New Piperidine and Piperazine Derivatives of Dichloroacetate as Potential Anticancer Agents

Dichloroacetate (DCA) is a small anticancer agent acting through inhibition of pyruvate dehydrogenase kinases (PDKs) and preventing proliferation of tumor growth. In this study, a series of new piperidine and piperazine derivatives of DCA were designed and subjected to molecular docking analysis. Based on the docking results, nine compounds with a lowest binding energy and better interaction with PDK isoenzymes were selected and synthesized. The cytotoxic activities of the synthesized compounds were evaluated against HT-29 and MCF7 human cancer cell lines. These compounds showed moderate potency and much higher anticancer activity than DCA. The most active compound of the series (f1) showed IC50 value of 7.79 mu M against HT-29 cell line.

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

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 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, molecular formula is C23H32N6O5S. In an article, author is Mouhoubi, Seloua,once mentioned of 139755-85-4, Name: 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.

Thermodynamic modeling of CO2 absorption in aqueous solutions of N,N-diethylethanolamine (DEEA) and N-methyl-1,3-propanediamine (MAPA) and their mixtures for carbon capture process simulation

Carbone capture by absorption-regeneration technology is a well-known process. However, the development and utilization of new solvents remains crucial to lower its energy consumption. Therefore, an accurate thermodynamic modeling is essential for the process simulation and optimization. This work focuses on the thermodynamic modeling of CO2 absorption in aqueous solutions of N,N-diethylethanolamine (DEEA), N-methyl-1,3-propanediamine (MAPA) and their mixtures using electrolyte NRTL model. A novel thermodynamic modeling of DEEA-H2O-CO2, MAPA-H2O-CO(2 )and DEEA-MAPA-H2O-CO2 systems was developed. The modeling was carried out by considering the pure vapor pressures, excess enthalpies, dielectric constants, physical solubilities of CO2, partial and total pressures experimental data. The predicted and correlated data such as vapor-liquid equilibrium (VLE) and heat of CO2 absorption were compared favorably to experimental data from the literature. Liquid-liquid phase separation of a specific mixture of these two amines was also highlighted. Subsequently, the developed model could be used for further simulations at large scale considering that successful validation was performed at pilot scale. (C) 2020 Institution of Chemical Engineers. Published by Elsevier B.V. All rights reserved.

Interested yet? Keep reading other articles of 139755-85-4, you can contact me at any time and look forward to more communication. Name: 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.

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

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 130307-08-3, Name is 1-(4-Bromophenyl)-4-methylpiperazine, molecular formula is C11H15BrN2. In an article, author is Falsini, Matteo,once mentioned of 130307-08-3, Category: piperazines.

New 8-amino-1,2,4-triazolo[4,3-a]pyrazin-3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A(2A) adenosine receptor antagonists

In this work, further structural investigations on the 8-amino-2-phenyl-6-aryl-1,2,4-triazolo[4,3-a]pyrazin-3-one series were carried out to achieve potent and selective human A(2A) adenosine receptor (AR) antagonists. Different ether and amide moieties were attached at the para-position of the 6-phenyl ring, thus leading to compounds 1-9 and 10-18, respectively. Most of these moieties contained terminal basic rings (pyrrolidine, morpholine, piperidine and substituted piperazines) which were thought to confer good physicochemical and drug-like properties. Compounds 11-16, bearing the amide linker, possessed high affinity and selectivity for the hA(2A) AR (K-i = 3.6-11.8 nM). Also derivatives 1-9, featuring an ether linker, preferentially targeted the hA(2A) AR but with lower affinity, compared to those of the relative amide compounds. Docking studies, carried out at the hA(2A) AR binding site, highlighted some crucial ligand-receptor interactions, particularly those provided by the appended substituent whose nature deeply affected hA(2A) AR affinity.

Interested yet? Keep reading other articles of 130307-08-3, you can contact me at any time and look forward to more communication. Category: piperazines.

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

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 5308-25-8, Name is 1-Ethylpiperazine, molecular formula is C6H14N2, belongs to piperazines compound, is a common compound. In a patnet, author is Giancola, JoLynn B., once mentioned the new application about 5308-25-8, Recommanded Product: 1-Ethylpiperazine.

Structure-activity relationships for a series of (Bis(4-fluorophenyl) methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability

Despite considerable efforts to develop medications to treat psychostimulant use disorders, none have proven effective, leaving an underserved patient population and unanswered questions as to what mechanism(s) of action should be targeted for developing pharmacotherapies. Atypical dopamine transporter (DAT) inhibitors, based on (+/-)modafinil, have shown therapeutic potential in preclinical models of psychostimulant abuse. However, metabolic instability among other limitations to piperazine analogues 1-3 have impeded further development. Herein, bioisosteric substitutions of the piperazine ring were explored with a series of aminopiperidines (A) and piperidine amines (B) wherein compounds with either a terminal tertiary amine or amide were synthesized. Several lead compounds showed high to moderate DAT affinities and metabolic stability in rat liver microsomes. Aminopiperidines 7 (DAT K-i = 50.6 nM), 21b (DAT K-i = 77.2 nM) and 33 (DAT K(i)Elsevier = 30.0 nM) produced only minimal stimulation of ambulatory activity in mice, compared to cocaine, suggesting an atypical DAT inhibitor profile. (C) 2020 Elsevier Masson SAS. All rights reserved.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 5308-25-8. The above is the message from the blog manager. Recommanded Product: 1-Ethylpiperazine.

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

Electric Literature of 147081-29-6, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 147081-29-6, Name is (S)-tert-Butyl 3-methylpiperazine-1-carboxylate, SMILES is O=C(N1C[C@H](C)NCC1)OC(C)(C)C, belongs to piperazines compound. In a article, author is Cao, Xue-Li, introduce new discover of the category.

High-permeability and anti-fouling nanofiltration membranes decorated by asymmetric organic phosphate

Aiming at the two challenging bottlenecks of trade-off effect and membrane fouling that limit the development of nanofiltration (NF) membranes, this work developed a high-performance NF membrane based on the modification by an asymmetric hydrophilic zoledronic acid (ZA). ZA plays multiple roles: (1) the self-restrictive diffusion effect of piperazine (PIP)/ZA obtained from the reaction of PIP and ZA resulted in smooth membrane surface; (2) the imidazolyl on ZA uninvolved in interfacial polymerization (IP) led to enlarged polyamide network pores and provided more solvent tunnels; (3) all groups of ZA improved the membrane hydrophilicity; (4) the electronegative phosphate groups made a significant contribution to the strong membrane surface electronegativity. As a result, the ZA-modified membrane exhibited nearly five times higher permeability than that of traditional NF membranes, accompanied by perfect selectivity of SO42- and Cl- as well as the outstanding anti-fouling property, indicating its enormous application prospect in water treatment.

Electric Literature of 147081-29-6, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 147081-29-6.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 106261-49-8, Name is 4-[(4-Methylpiperazin-1-yl)methyl]benzoic acid dihydrochloride, formurla is C13H20Cl2N2O2. In a document, author is Liu, Biming, introducing its new discovery. Application In Synthesis of 4-[(4-Methylpiperazin-1-yl)methyl]benzoic acid dihydrochloride.

Enhanced oxidative degradation of norfloxacin using peroxymonosulfate activated by oily sludge carbon-based nanoparticles CoFe2O4/OSC

In this study, oily sludge (OS) was pyrolyzed into an environmentally friendly OS carbon (OSC) material, which was used as the carrier of CoFe2O4 nanoparticles to prepare a heterogeneous catalyst CoFe2O4/OSC, and it was used to catalyze the degradation of norfloxacin (NFC) by peroxymonosulfate (PMS). X-ray diffraction (XRD) and transmission electron microscope (TEM) characterization results show that CoFe2O4/OSC had a spinel structure under high temperature pyrolysis conditions. The effects of initial pH, PMS dosage, catalyst dosage, and temperature on NFC degradation efficiency were also studied. Under a temperature of 25 degrees C, an initial pH of 7, a catalyst amount of 0.5 g/L, and a PMS dosage of 0.8 mM, the reaction rate constant reached 0.051 min(-1), and the degradation efficiency and total organic carbon of NFC reached 90.8% and 62%, respectively, within 60 min. Trace amounts of Co and Fe ions were leached from the system (both less than 30 mu g/L). After ten cycles, the degradation efficiency of NFC decreased to 69.8%. Radical quenching experiments, electron paramagnetic resonance, and X-ray fluorescence spectroscopy characterization proved that free-radical ((OH)-O-center dot, SO4 center dot-, and O-2(center dot-)) and nonradical (O-1(2)) active species were present in the system. Moreover, the CoFe2O4/OSC/PMS system involved the participation of two pairs of redox couples (Fe(II)/Fe(III) and Co(III)/Co(II)). Results from matrix-assisted laser desorption ionization time-of-flight mass spectrometry and ion chromatography proved that the main oxidation pathways of NFC were formed through the fragmentation of heterocycles, defluorination of benzene rings, decarboxylation reactions, and piperazine ring-opening process. At the same time, NFC was eventually oxidized to fluoride. This study provides potential for the resource utilization of OS and the application of sludge-type catalysts in PMS-activated oxidation systems.

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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. 300543-56-0, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine, molecular formula is C17H19ClN2, belongs to piperazines compound. In a document, author is Salaciak, Kinga, introduce the new discover, Product Details of 300543-56-0.

The antidepressant-like activity of chiral xanthone derivatives may be mediated by 5-HT1A receptor and beta-arrestin signalling

Background: Our previous studies showed that xanthone derivatives with N-(2-methoxyphenyl)piperazine fragment have an affinity to the 5-HT1A receptor and show antidepressant-like properties in rodents. In this study, we tested three xanthone derivatives, HBK-1 (R, S) and its enantiomers, in which we increased the distance between the piperazine and xanthone fragments by using a hydroxypropoxy linker. We hypothesized that this would increase the binding to the 5-HT1A receptor and consequently, pharmacological activity. Aims: We aimed to assess the in vitro and in vivo pharmacological activity of the xanthone derivatives. Methods: We evaluated the in vitro affinity for serotonin 5-HT1A and 5-HT2A receptors and serotonin transporter. We also determined the intrinsic activity at the 5-HT1A receptor. We investigated the antidepressant-like properties and safety after acute administration (dose range: 1.25-20 mg/kg) using the forced swim, tail suspension, locomotor activity, rotarod and chimney tests in mice. We also evaluated the basic pharmacokinetic parameters. Results: Our results indicated that the compounds showed a high affinity for the 5-HT1A receptor but very weak antagonistic properties in the Ca2+ mobilization assay; however, they showed significant agonistic properties in the beta-arrestin recruitment assay. In both behavioural tests the studied xanthone derivatives showed antidepressant-like activity. Pre-treatment with p-chlorophenylalanine or WAY-100635 abolished their antidepressant-like activity. None of the compounds caused motor impairments at antidepressant-like doses. The racemate penetrated the blood-brain barrier and had a relatively high bioavailability after intraperitoneal administration. Conclusions: Xanthone derivatives with N-(2-methoxyphenyl)piperazine fragment and hydroxypropoxy linker show increased binding to the 5-HT1A receptor and may represent an attractive putative treatment candidate for depression.

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 300543-56-0. Product Details of 300543-56-0.

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

In an article, author is Kettle, Jason G., once mentioned the application of 5308-25-8, Application In Synthesis of 1-Ethylpiperazine, Name is 1-Ethylpiperazine, molecular formula is C6H14N2, molecular weight is 114.1888, MDL number is MFCD00059912, category is piperazines. Now introduce a scientific discovery about this category.

Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS(G12C)

Attempts to directly drug the important oncogene KRAS have met with limited success despite numerous efforts across industry and academia. The KRAS(G12)C mutant represents an Achilles heel and has recently yielded to covalent targeting with small molecules that bind the mutant cysteine and create an allosteric pocket on GDP-bound RAS, locking it in an inactive state. A weak inhibitor at this site was optimized through conformational locking of a piperazine-quinazoline motif and linker modification. Subsequent introduction of a key methyl group to the piperazine resulted in enhancements in potency, permeability, clearance, and reactivity, leading to identification of a potent KRAS(G12C) inhibitor with high selectivity and excellent cross-species pharmacokinetic parameters and in vivo efficacy.

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

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, Application In Synthesis of 1-Ethylpiperazine5308-25-8, Name is 1-Ethylpiperazine, SMILES is CCN1CCNCC1, belongs to piperazines compound. In a article, author is Hu, Zhi, introduce new discover of the category.

Flame retardancy, thermal properties, and combustion behaviors of intumescent flame-retardant polypropylene containing (poly) piperazine pyrophosphate and melamine polyphosphate

A (poly) piperazine pyrophosphate (PIPP) was synthesized and its chemical structure was confirmed via Fourier transform infrared spectroscopy,H-1 nuclear magnetic resonance, and(31)P nuclear magnetic resonance. PIPP was used together with melamine polyphosphate (MPP) as an ammonium polyphosphate (APP)-free intumescent flame retardant (IFR) to prepare several flame-retardant polypropylene (FRPP) composites. The flame retardancy and burning behaviors of the composites were investigated via limiting oxygen index (LOI) determination, vertical burning tests (UL-94), and cone calorimeter tests. The thermal properties were investigated by means of thermogravimetric analysis under nitrogen and air atmosphere. Use of PIPP and MPP together yielded an increase in the LOI value, a UL-94 V-0 rating, and a decrease in both the values of PHRR and THR in cone calorimetric analysis. Visual observations and scanning electronic microscopy confirmed the occurrence of char formation, which acted as a heat and fire barrier in the condense phase.

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 5308-25-8. Application In Synthesis of 1-Ethylpiperazine.

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

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , Safety of 2,2′-(Piperazine-1,4-diyl)diethanesulfonic acid, 5625-37-6, Name is 2,2′-(Piperazine-1,4-diyl)diethanesulfonic acid, molecular formula is C8H18N2O6S2, belongs to piperazines compound. In a document, author is Konduri, Srihari, introduce the new discover.

Design and synthesis of purine connected piperazine derivatives as novel inhibitors of Mycobacterium tuberculosis

A series of novel purine linked piperazine derivatives were synthesized to identify new, potent inhibitors of Mycobacterium tuberculosis. The compounds were designed to target MurB disrupting the biosynthesis of the peptidoglycan and exert antiproliferative effects. The first series of purine-2,6-dione linked piperazine derivatives were synthesized using an advanced intermediate 1-(3,4-difluorobenzyl)-7-(but-2-ynyl)-3-methyl-8-(piperazin-1-yl)-1H-purine-2,6(3H,7H)-dione hydrochloride (6) which was coupled with varied carboxylic acid chloride derivatives. Following this piperazine linked derivatives were also synthesized from 6 using diverse isocyanate partners. The anti-mycobacterial activity of the analogues was tested against Mycobacterium tuberculosis H37Rv which revealed a cluster of six analogues (11, 24, 27, 32, 33 and 34), possessed promising activity. In comparison, a set of these new compounds possessed greater potencies relative to current drugs used in the clinic such as Ethambutol. These results were also correlated with computational molecular docking analysis, providing models for strong interactions of the inhibitors with MurB providing a template for the future development of preclinical agents against Mycobacterium tuberculosis.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 5625-37-6. Safety of 2,2′-(Piperazine-1,4-diyl)diethanesulfonic acid.

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