Month: October 2022

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 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 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 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 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 April 30, 2009, Barlaam, Bernard Christophe; Bower, Justin Fairfield; Delouvrie, Benedicte; Fairley, Gary; Harris, Craig Steven; Lambert, Christine; Ouvry, Gilles; Winter, Jon James Gordon published a patent.Related Products of 1211568-27-2 The title of the patent was Pyridine and pyrazine derivatives as Axl and/or c-Met receptor enzyme inhibitors and their preparation, pharmaceutical compositions and use in the treatment of tumors. And the patent contained the following:

The invention concerns pyridine a nd pyrazine derivatives of formula I or a pharmaceutically-acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of tumors. Compounds of formula I wherein W is CH and N; J is O and S; each G1, G2, G3 and G4 is CH and N, proved that no more than two of G1,G2, G3 and R4 is N; A is (un)substituted Ph, (un)substituted 5- to 6-membered monocyclic heteroaryl; and (un)substituted 8- to 10-membered bicyclic ring; each R3 is independently H, halo, CN, amino, sulfamoyl, CF3, C1-8 alkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 2-aminophenol with 2-amino-5-bromopyridine-3-carboxylic acid; the resulting 3-(benzoxazol-2-yl)-5-bromopyridin-2-amine underwent cross-coupling with 4-(dimethylaminomethyl)phenylboronic acid to give compound II. All the invention compounds were evaluated for their Axl and c-Met receptor tyrosine kinase inhibitory activity. From the Axl tyrosine kinase assay, it was determined that compound II exhibited 99.8 % inhibition at 1 μM concentration The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to pyridine preparation axl cmet tyrosine kinase inhibitor treatment tumor, pyrazine preparation axl cmet tyrosine kinase inhibitor treatment tumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1211568-27-2

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

On June 30, 2007, He, Qiu Qin; Li, Ke; Cao, Yong Bing; Dong, Huan Wen; Zhao, Li Hua; Liu, Chao Mei; Sheng, Chun Quan published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Design, synthesis and molecular docking studies of novel triazole antifungal compounds. And the article contained the following:

Based on the active site of Candida albicans lanosterol 14α-demethylase (CACYP51), novel triazole compounds structurally different from the current triazole drugs were designed and synthesized. In vitro antifungal activities showed that compounds I (R = R1 = Me; R = CMe3, CN, NO2, R1 = H) exhibited strong activities. In addition, the first three also displayed certain activities against fluconazole-resistant fungi. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to triazolylpropanol benzylpiperazinylphenoxy derivative preparation antifungal activity, mol docking triazolylpropanol derivative lanosterol demethylase, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On September 17, 1998, Tanoury, Gerald J.; Senanayake, Chris H.; Hett, Robert; Kuhn, Amy M.; Kessler, Donald W.; Wald, Stephen A. published an article.Electric Literature of 67914-60-7 The title of the article was Pd-catalyzed aminations of aryltriazolones: effective synthesis of hydroxyitraconazole enantiomers. And the article contained the following:

A palladium-catalyzed amination of triazolone I by piperazine II was used as the key step in an efficient synthesis of highly enantiomerically pure hydroxyitraconazole (III). II (>99% ee) was prepared by reaction of an achiral phenol precursor with the corresponding dioxolyl tosylate (>99% ee). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Electric Literature of 67914-60-7

The Article related to hydroxyitraconazole asym preparation, amination aryltriazolone palladium, triazolone aryl amination palladium, heck coupling vs palladium catalyzed amination, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 67914-60-7

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

On December 31, 1990, Chapman, David R.; Bauer, Ludwig; Waller, Donald P.; Zaneveld, Lourens J. D. published an article.Recommanded Product: 67914-60-7 The title of the article was Synthesis of diastereomeric ketoconazole analogs. And the article contained the following:

Syntheses of trans-isomers of ketoconazole (I) and the corresponding des-acetyl, 1-Me, 1-formyl and 1-methanesulfonyl analogs were investigated. These isomers, along with the corresponding cis-diastereomers were characterized by their carbon-13 NMR spectra. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 67914-60-7

The Article related to ketoconazole diastereomer, imidazolylmethyldioxolanylmethoxyphenylpiperazine, piperazinophenol imidazolylmethyldioxolanylmethanesulfonate reaction, nmr ketoconazole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 67914-60-7

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

On June 30, 2005, Liu, Yong; Wang, Jingkang; Yin, Qiuxiang published an article.Electric Literature of 86393-32-0 The title of the article was Determination of the space group for ciprofloxacin hydrochloride monohydrate crystals. And the article contained the following:

Ciprofloxacin hydrochloride monohydrate (CPFX) crystals were obtained exptl. The deaquation, melting, decomposing apex temperatures and water content of ciprofloxacin hydrochloride monohydrate crystals were measured by DSC and TG techniques resp. The data of X-ray powder diffraction (XRPD) of these crystals were collected exptl. The indexing results by the software Cerius2 were obtained. The results showed that the crystal of ciprofloxacin hydrochloride monohydrate belonged to monoclinic, and the unit cell parameters a, b, c and β were 12.93×10-10 m, 19.56×10-10 m, 7.07×10-10 m, and 91.10° resp. Based on the indexing results and the extinction principle, the space group for ciprofloxacin hydrochloride monohydrate crystals produced in crystallization experiment was P21/c. 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).Electric Literature of 86393-32-0

The Article related to ciprofloxacin hydrochloride monohydrate x ray powder diffraction space group, unit cell parameter, Crystallography and Liquid Crystals: Crystallographic Methods and Apparatus For Structure Determination and other aspects.Electric Literature of 86393-32-0

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