Category: piperazines

On April 11, 2013, Letavic, Michael A.; Lord, Brian; Bischoff, Francois; Hawryluk, Natalie A.; Pieters, Serge; Rech, Jason C.; Sales, Zachary; Velter, Adriana I.; Ao, Hong; Bonaventure, Pascal; Contreras, Victor; Jiang, Xiaohui; Morton, Kirsten L.; Scott, Brian; Wang, Qi; Wickenden, Alan D.; Carruthers, Nicholas I.; Bhattacharya, Anindya published an article.Related Products of 1428327-31-4 The title of the article was Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists. And the article contained the following:

The synthesis and preclin. characterization of two novel, brain penetrating P2X7 compounds will be described. Both compounds are shown to be high potency P2X7 antagonists in human, rat, and mouse cell lines and both were shown to have high brain concentrations and robust receptor occupancy in rat. Compound I is of particular interest as a probe compound for the preclin. assessment of P2X7 blockade in animal models of neuro-inflammation. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Related Products of 1428327-31-4

The Article related to brain penetrating p2x7 antagonist nicotinamide isoquinolinecarboxamide derivative, p2x7, depression, neuro-inflammation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1428327-31-4

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

On May 31, 2020, Chow, Amanda; McCrea, Liam; Kimball, Elizabeth; Schaub, Julie; Quigley, Harry; Pitha, Ian published an article.Product Details of 380843-75-4 The title of the article was Dasatinib inhibits peripapillary scleral myofibroblast differentiation. And the article contained the following:

Scleral fibroblast activation occurs in glaucomatous and myopic eyes. Here we perform an unbiased screen to identify kinase inhibitors that reduce fibroblast activation to diverse stimuli in vitro and to in vivo intraocular pressure (IOP) elevation. Primary cultures of peripapillary scleral (PPS) fibroblasts from two human donors were screened using a library of 80 kinase inhibitors to identify compounds that inhibit TGFbeta-induced extracellular matrix (ECM) synthesis. Inhibition of myofibroblast differentiation was verified by alpha smooth muscle actin (aSMA) immunoblot and collagen contraction assay. Three kinase inhibitors were verified to reduce TGFbeta-induced aSMA expression and cellular contractility (rottlerin, PP2, tyrphostin 9). The effect of three Src inhibitors, bosutinib, dasatinib, and SU-6656, on myofibroblast differentiation was evaluated, with only dasatinib significantly inhibiting TGFbeta-induced ECM synthesis, aSMA expression, and cellular contractility at nanomolar dosages. Subconjunctival injection of dasatinib reduced IOP-induced scleral fibroblast proliferation compared to control (4.9 ± 11.1 ng/sclera with 0.1 muM vs. 88.7 ± 38.6 ng/sclera in control, P < 0.0001). Dasatinib inhibits scleral myofibroblast differentiation and there is pharmacol. evidence that this inhibition is not solely due to Src-kinase inhibition. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Product Details of 380843-75-4

The Article related to glaucoma peripapillary scleral myofibroblast differentiation dasatinib, fibroblast, fibrosis, glaucoma, kinase inhibitor, peripapillary sclera, scleral remodeling, src kinase and other aspects.Product Details of 380843-75-4

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

On July 24, 1992, Rotstein, David M.; Kertesz, Denis J.; Walker, Keith A. M.; Swinney, David C. published an article.COA of Formula: C12H16N2O2 The title of the article was Stereoisomers of ketoconazole: preparation and biological activity. And the article contained the following:

The four stereoisomers of the antifungal agent ketoconazole, (2S,4R)-, (2R,4R)-, (2R,4S)-, and (2S,4S)-(imidazolylmethyl)phenyl{[(acetylpiperazinyl)phenoxy]methyl}dioxolanes I, were prepared and evaluated for their selectivity in inhibiting a number of cytochrome P 450 enzymes. Thus, (bromomethyl)phenyldioxolanes II condensed with 4-(N-acetylpiperazino)phenol and imidazole to give I. II were prepared by bromination of 2′,4′-dichloroacetophenone followed by reaction with (S)- and (R)-solketal tosylate. Large differences in selectivity among the isomers were observed for inhibition of the cytochromes P 450 involved in steroid biosynthesis, whereas little difference was observed for inhibition of those associated with hepatic drug metabolism The cis-(2S,4R) and trans-(2R,4R) isomers are equipotent in inhibiting corticoid 11β-hydroxylase and much more effective than their antipodes. Little selectivity was observed for inhibition of cholesterol side chain cleavage or xenobiotic hydroxylases. These data indicate that the affinity of azoles for cytochrome P 450 enzymes involved in steroid synthesis is high dependent on the stereochem. of the entire mol., whereas binding to drug metabolizing enzymes is a less selective process. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).COA of Formula: C12H16N2O2

The Article related to ketoconazole stereoisomer preparation cytochrome p450 inhibition, imidazolylmethylphenylacetylpiperazinylphenoxymethyldioxolane preparation cytochrome p450 enzyme inhibition and other aspects.COA of Formula: C12H16N2O2

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

On September 30, 2021, Kikuya, Megumi; Furuichi, Kenta; Hirao, Takuya; Endo, Satoshi; Toyooka, Naoki; Ito, Kousei; Aoki, Shigeki published an article.Computed Properties of 380843-75-4 The title of the article was Aldo-keto reductase inhibitors increase the anticancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia. And the article contained the following:

Tyrosine kinase inhibitors (TKIs) are widely utilized in clin. practice to treat carcinomas, but secondary tumor resistance during chronic treatment can be problematic. AKR1B1 and AKR1B10 of the aldo-keto reductase (AKR) superfamily are highly expressed in cancer cells and are believed to be involved in drug resistance. The aim of this study was to understand how TKI treatment of chronic myelogenous leukemia (CML) cells changes their glucose metabolism and if inhibition of AKRs can sensitize CML cells to TKIs. K562 cells were treated with the TKIs imatinib, nilotinib, or bosutinib, and the effects on glucose metabolism, cell death, glutathione levels, and AKR levels were assessed. To assess glucose dependence, cells were cultured in normal and low-glucose media. Pretreatment with AKR inhibitors, including epalrestat, were used to determine AKR-dependence. Treatment with TKIs increased intracellular glucose, AKR1B1/10 levels, glutathione oxidation, and nuclear translocation of nuclear factor erythroid 2-related factor 2, but with minimal cell death. These effects were dependent on intracellular glucose accumulation. Pretreatment with epalrestat, or a selective inhibitor of AKR1B10, exacerbated TKI-induced cell death, suggesting that especially AKR1B10 was involved in protection against TKIs. Thus, by disrupting cell protective mechanisms, AKR inhibitors may render CML more susceptible to TKI treatments. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Computed Properties of 380843-75-4

The Article related to anticancer aldoketo reductase tyrosine kinase inhibitor chronic myelogenous leukemia, akr1b1/10, chronic myelogenous leukemia, epalrestat, glucose, tyrosine kinase inhibitor and other aspects.Computed Properties of 380843-75-4

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

On October 31, 2021, Baggio, Diva; Tan, Sean; Porch, Kylie; Shortt, Jake; Ko, Brian published an article.Application of 380843-75-4 The title of the article was Prediction of cardiovascular events in patients with chronic myeloid leukaemia using baseline risk factors and coronary artery calcium scoring. And the article contained the following:

A standardised method for cardiovascular risk stratification in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors is lacking. We report an algorithm for risk stratification applicable to all patients commencing tyrosine kinase inhibitor therapy based on age, prior cardiovascular disease and Framingham Risk Score, incorporating coronary artery calcium scoring in patients at intermediate Framingham Risk Score risk. Of 88 patients retrospectively studied, major adverse cardiovascular event rates in our study-defined low-, intermediate- and high-risk categories were 0%, 10% and 19% resp. Of nine patients down-classified from intermediate to low risk on the basis of coronary artery calcium scoring, none went on to experience a major adverse cardiovascular event. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Application of 380843-75-4

The Article related to chronic myeloid leukemia coronary artery calcium algorithm bosutinib, calcium scoring, cardio-oncology, chronic myeloid leukaemia, coronary artery, tyrosine kinase inhibitor and other aspects.Application of 380843-75-4

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

On June 12, 1974, Jeanmart, Claude; Leger, Andre; Messer, Mayer N. published a patent.Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride The title of the patent was [1,4]Dithiino[2,3-c]pyrrole derivatives. And the patent contained the following:

Dithiinopyrrolyl esters I (R =substituted 2-pyridyl, 2-naphthyridinyl, phenyl, 6-methoxy-3-pyridazinyl, 7-chloro-2-quinolyl, R1 = Me; R1 = Et, CHMe2, allyl, CH2CH2OH, R = 5-chloro-2-pyridyl) (25 compounds) were prepared by esterifying the alcs. II (R2 = OH, R3 = H), prepared by treating III with RNH2 and reducing II (R2R3 = O). Thus, 35. g III was treated with 24 g 2-amino-5-chloropyridine to give 51 g II (R = 5-chloro-2-pyridyl, R2R3 = O), which was reduced with KBH4 to 49.8 g II (R2 = OH, R3 = H). Esterification of 15 g of the alc. with 24.4 g 1-(chlorocarbonyl)-4-methylpiperazine gave 15.6 g I (R = 5-chloro-2-pyridyl, R1 = Me). I were tranquilizing, anticonvulsant, and muscle relaxant at 5-100 mg/kg orally in mice. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride

The Article related to dithiinopyrrolyl ester, anticonvulsant dithiinopyrrolyl ester, muscle relaxant dithiinopyrrolyl ester, tranquilizer dithiinopyrrolyl ester, piperazine dithiinopyrrolyl ester and other aspects.Recommanded Product: 4-Ethyl-piperazine-1-carbonyl chloride

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

On March 31, 2005, Rizk, N. M. H.; El-Kosasy, A. M. published an article.SDS of cas: 86393-32-0 The title of the article was Novel ciprofloxacin ion membrane sensors based on β-cyclodextrin. And the article contained the following:

Ciprofloxacin (CF) is sensitively detected in pharmaceuticals and human serum by potentiometric method. The proposed method based on the use of β-cyclodextrin (βCD) as ionophore, o-nitrophenyl octyl ether as plasticizer and potassium tetraphenyl-fluoromethylborate as a cationic additive, in polyvinyl chloride (PVC) matrix for the fabrication and construction of ciprofloxacin sensors. The conventional and microsized coated wire types are prepared, characterized compared and applied. The proposed sensors exhibit linear response in the range of 1×10-1-1×10-4 M ciprofloxacin with cationic slopes of 30.2±0.5 and 29.3±0.6 mV decade-1 at 25° over the pH range 4-6 for conventional and microsized coated wire, resp. Ciprofloxacin electrodes show reasonable selectivity towards some related compounds, amino acids, common organic and inorganic cations. The investigated procedures are successfully applied to the determination of ciprofloxacin in bulk powder, pharmaceutical products and human serum. Results with mean accuracy 99.8±0.6 % and 99.6±0.7 % for the nominal concentrations were obtained for conventional and microsized coated wire, resp., which compare well with data obtained using spectrophotometric (UV-Vis) method. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).SDS of cas: 86393-32-0

The Article related to ciprofloxacin sensor beta cyclodextrin ionophore potassium tetraphenyl fluoromethylborate, cationic additive pharmaceutical preparation nitrophenyl octyl ether plasticizer and other aspects.SDS of cas: 86393-32-0

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

On December 31, 2021, Nielsen, Soeren Saxmose; Bicout, Dominique Joseph; Calistri, Paolo; Canali, Elisabetta; Drewe, Julian Ashley; Garin-Bastuji, Bruno; Gonzales Rojas, Jose Luis; Gortazar Schmidt, Christian; Herskin, Mette; Michel, Virginie; Miranda Chueca, Miguel Angel; Padalino, Barbara; Pasquali, Paolo; Roberts, Helen Clare; Spoolder, Hans; Stahl, Karl; Velarde, Antonio; Viltrop, Arvo; Winckler, Christoph; Dewulf, Jeroen; Guardabassi, Luca; Hilbert, Friederike; Mader, Rodolphe; Baldinelli, Francesca; Alvarez, Julio published an article.Application of 86393-32-0 The title of the article was Assessment of animal diseases caused by bacteria resistant to antimicrobials: sheep and goats. And the article contained the following:

In this opinion, the antimicrobial-resistant bacteria responsible for transmissible diseases that constitute a threat to the health of sheep and goats have been assessed. The assessment has been performed following a methodol. based on information collected by an extensive literature review and expert judgement. Details of the methodol. used for this assessment are explained in a sep. opinion. A global state of play on antimicrobial resistance in clin. isolates of Staphylococcus aureus, Escherichia coli (non-VTEC), Pseudomonas aeruginosa, Dichelobacter nodosus, Moraxella ovis, Mannheimia haemolytica, Pasteurella multocida, Mycoplasma ovipneumoniae, Mycoplasma agalactiae, Trueperella pyogenes, Streptococcus uberis, Bibersteinia trehalosi, Campylobacter fetus, Mycoplasma mycoides subsp. capri, Mycoplasma capricolum subsp. capricolum, Fusobacterium necrophorum is provided. Among those bacteria, EFSA identified E. coli with > 66% certainty as being the most relevant antimicrobial-resistant bacteria in sheep and goat in the EU based on the available evidence. The animal health impact of these most relevant bacteria, as well as their eligibility for being listed and categorized within the animal health law framework will be assessed in sep. scientific opinions. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Application of 86393-32-0

The Article related to animal diseases caused bacteria resistant antimicrobial sheep goat, animal health law, antimicrobial resistance, extensive literature review, goats, sheep, small ruminants and other aspects.Application of 86393-32-0

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

On June 30, 2020, Bruemmendorf, Tim H.; Gambacorti-Passerini, Carlo; Bushmakin, Andrew G.; Cappelleri, Joseph C.; Viqueira, Andrea; Reisman, Arlene; Isfort, Susanne; Mamolo, Carla published an article.Formula: C26H29Cl2N5O3 The title of the article was Relationship between molecular response and quality of life with bosutinib or imatinib for chronic myeloid leukemia. And the article contained the following:

Abstract: Patients with newly diagnosed chronic phase chronic myeloid leukemia (CP CML) can be effectively treated with tyrosine kinase inhibitors (TKIs) and achieve a lifespan similar to the general population. The success of TKIs, however, requires long-term and sometimes lifelong treatment; thus, patient-assessed health-related quality of life (HRQoL) has become an increasingly important parameter for treatment selection. Bosutinib is a TKI approved for CP CML in newly diagnosed adults and in those resistant or intolerant to prior therapy. In the Bosutinib Trial in First-Line Chronic Myelogenous Leukemia Treatment (BFORE), bosutinib demonstrated a significantly higher major mol. response rate compared with imatinib, with maintenance of HRQoL (measured by the Functional Assessment of Cancer Therapy-Leukemia (FACT-Leu) questionnaire), after 12 mo of first-line treatment. We examined relationships between mol. response (MR) and HRQoL. MR values were represented by a log-reduction scale (MRLR; a continuous variable). A repeated-measures longitudinal model was used to estimate the relationships between MRLR as a predictor and each FACT-Leu domain as an outcome. Effect sizes were calculated to determine strength of effects and allow comparisons across domains. The majority of FACT-Leu domains (with the exception of social well-being and phys. well-being) demonstrated a significant relationship with MRLR (p < 0.05). Our results showed variable impact of clin. improvement on different dimensions of HRQoL. For patients who achieved MR5, emotional well-being and leukemia-specific domains showed the greatest improvement, with medium differences in effect sizes, whereas social well-being and phys. well-being had the weakest relationship with MR. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Formula: C26H29Cl2N5O3

The Article related to bosutinib imatinib antileukemic agent diagnosis chronic myeloid leukemia, bosutinib, chronic myeloid leukemia, health-related quality of life, imatinib, molecular response and other aspects.Formula: C26H29Cl2N5O3

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

On October 2, 2015, Salahifar, Eslam; Nematollahi, Davood; Bayat, Mehdi; Mahyari, Amir; Amiri Rudbari, Hadi published an article.Formula: C12H16N2O2 The title of the article was Regioselective Green Electrochemical Approach to the Synthesis of Nitroacetaminophen Derivatives. And the article contained the following:

A regioselective green synthesis of nitroacetaminophen derivatives e. g., I, was carried out by electrochem. oxidation of acetaminophen, N-(2-hydroxyphenyl)acetamide, and 1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone in the presence of nitrite ion as a nucleophile. The present work has led to the development of a reagentless green and facile electrochem. method for the synthesis of some nitroacetaminophen derivatives The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to nitroacetaminophen derivative regioselective synthesis green chem, acetaminophen hydroxyphenylacetamide hydroxyphenylpiperazinylethanone electrochem oxidation nitrite ion and other aspects.Formula: C12H16N2O2

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