Month: April 2022

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole( cas:73590-85-9 ) is researched.Category: ethers-buliding-blocks.Webster, Lorraine K.; Jones, D. Brian; Mihaly, George W.; Morgan, Denis J.; Smallwood, Richard A. published the article 《Effect of hypoxia on oxidative and reductive pathways of omeprazole metabolism by the isolated perfused rat liver》 about this compound( cas:73590-85-9 ) in Biochemical Pharmacology. Keywords: hypoxia omeprazole metabolism liver; oxidation reduction omeprazole liver hypoxia. Let’s learn more about this compound (cas:73590-85-9).

The effect of hypoxia on the elimination of H168-68 (omeprazole)(I) [73590-58-6] a potent inhibitor of gastric acid secretion, was studied in the isolated perfused rat liver. During normal oxygenation, a 10 mg bolus dose was eliminated rapidly (half-life (T1/2)-β = 8.0 min), while under hypoxic conditions T1/2β was increased to 81.6 min. Upon reoxygenation, T1/2β returned to 9.6 min. During hypoxia, perfusate concentrations of an oxidative metabolite (I-sulfone [88546-55-8]) were reduced by 68%, while those of the reductively-generated I-sulfide [73590-85-9] increased 4-fold. With reoxygenation, both formation and elimination of the sulfone were increased, whereas, which had accumulated during the hypoxic period, was eliminated rapidly. These findings were duplicated in steady-state experiments, in which omeprazole clearance during hypoxia fell by at least 70%, and sulfide concentrations in perfusate rose from undetectable levels to 200 ng/mL (at least a 10-fold increase). Sulfone concentrations did not change with hypoxia, consistent with a reduction in both its formation and elimination rates. Thus, the hepatic elimination of omeprazole is severely retarded by hypoxia, but this effect is promptly reversed by reoxygenation. The increased formation of the reductive metabolite during hypoxia is not of sufficient magnitude to sustain the normal hepatic elimination of omeprazole.

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Ether – Wikipedia,
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Synthetic Route of C10H14N2O. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about Synthesis of cycloalkylcarbamoyl substituted ketoconazole derivatives as antifungal agents. Author is Ryu, Seong-Ryuall.

In an effort to prepare new antifungal agents, two new title derivatives I (R = cyclopropyl, cyclohexyl) were synthesized by the reaction of substituted piperazine II with N-cycloalkylcarbamoyl derivatives ClCH2CONHR.

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SDS of cas: 56621-48-8. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about Discovery of novel pyrazole derivatives as a potent anti-inflammatory agent in RAW264.7 cells via inhibition of NF-kB for possible benefit against SARS-CoV-2. Author is Masih, Anup; Agnihotri, Amol K.; Srivastava, Jitendra K.; Pandey, Nidhi; Bhat, Hans R.; Singh, Udaya P..

Due to unavailability of a specific drug/vaccine to attenuate severe acute respiratory syndrome coronavirus 2, the current strategy to combat the infection has been largely dependent upon the use of anti-inflammatory drugs to control cytokines storm responsible for respiratory depression. Thus, in this study, we discovered novel pyrazole analogs as a potent nuclear factor kappa B (NF-κB) inhibitor. The compounds were assessed for NF-κB transcriptional inhibitory activity in RAW264.7 cells after stimulation with lipopolysaccharides (LPS), revealing Compound 6c as the most potent analog among the tested series. The effect of Compound 6c was further investigated on the levels of interleukin-1β, tumor necrosis factor-α, and interleukin-6 in LPS-stimulated RAW267.4 cells by enzyme immunoassay, where it causes a significant reduction in the level of these cytokines. In Western blot anal., Compound 6c also causes the inhibition of inhibitor kappa B-α and NF-κB. It was found to be snugly fitted into the inner grove of the active site of NF-κB by forming H-bonds and a nonbonded interaction with Asn28 in a docking anal.

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Malleron, Jean Luc; Comte, Marie Therese; Gueremy, Claude; Peyronel, Jean Francis; Truchon, Alain; Blanchard, Jean Charles; Doble, Adam; Piot, Odile; Zundel, Jean Luc published the article 《Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists》. Keywords: naphtosultam preparation receptor binding; antagonist 5HT2 naphtosultam; naphthoisothiazole dioxide aminoalkyl.They researched the compound: 4-(Piperazin-1-yl)phenol( cas:56621-48-8 ).HPLC of Formula: 56621-48-8. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:56621-48-8) here.

A series of 2-(aminoalkyl)naphtho[1,8-cd]isothiazole 1,1-dioxides I (R = aminoalkyl) was synthesized from I (R = H) and examined in various receptor binding tests. Most compounds demonstrated high affinity for the 5-HT2 receptor with moderate to high selectivity. A member of this series, compound I [R = 3-[4-(p-fluorophenyl)piperazino]propyl] (RP 62203), displays high 5-HT2 receptor affinity (Ki = 0.26 nM), which is resp. more than 100 and 1000 times higher than its affinity for α1 (Ki = 38 nM) and D2 (Ki >1000 nM) receptors. This compound is a potent orally effective and long lasting 5-HT2 antagonist in the mescaline-induced head-twitches test in mice and rats.

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Reference of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole, is researched, Molecular C17H19N3O2S, CAS is 73590-85-9, about A validated stability indicating ultra performance liquid chromatographic method for determination of impurities in Esomeprazole magnesium gastro resistant tablets. Author is Nalwade, Santaji Uttam; Reddy, Vangala Ranga; Rao, Dantu Durga; Morisetti, Nagendra kumar.

A novel gradient reversed-phase ultra performance liquid chromatog. method has been developed for quant. determination of Esomeprazole magnesium and its seven impurities in pharmaceutical dosage forms. Chromatog. separation has been achieved on an Acquity BEH C18, 50 mm × 2.1 mm, 1.7 μm with buffered mobile phase consisting solvent A (0.04 M (M) glycine (pH 9.0) buffer) and solvent B (mixture of acetonitrile and Milli-Q water in the ratio 90: 10 (volume/volume); resp.) delivered at flow rate of 0.21 mL min-1 and the detection wavelength 305 nm. Resolution of Esomeprazole magnesium and all the seven potential impurities has been achieved greater than 2.0 for all pairs of compounds The drug was subjected to the stress conditions of oxidative, acid, base, hydrolytic, thermal and photolytic degradation Esomeprazole magnesium was found to degrade significantly in oxidative and acid hydrolysis stress conditions and stable in base, hydrolytic and photolytic degradation conditions. The degradation products were well resolved from main peak and its impurities, thus proved the stability indicating power of the method. The stress samples were assayed against a reference standard and the mass balance was found to be close to 99.1%. So this method was also suitable for Assay determination of Esomeprazole magnesium in pharmaceutical dosage forms. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness.

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Ether – Wikipedia,
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Lindberg, Per; Nordberg, Peter; Alminger, Tomas; Braendstroem, Arne; Wallmark, Bjoern published an article about the compound: 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole( cas:73590-85-9,SMILESS:CC1=CN=C(CSC2=NC3=CC(OC)=CC=C3N2)C(C)=C1OC ).Product Details of 73590-85-9. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:73590-85-9) through the article.

The very potent gastric antisecretory agent omeprazole (I) [73590-58-6], presently under clin. evaluation, has been shown to act via inhibition of the gastric H+, K+-ATPase, the enzyme responsible for pumping of protons into the stomach. I needs acid activation to become an active inhibitor. A tetracyclic sulfenamide (II) was isolated from the acid decomposition of I. This sulfenamide, or, alternatively, the corresponding sulfenic acid, an unstable, probable intermediate in the sulfenamide formation, is the active inhibitor formed in vivo from omeprazole.

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Synthetic Route of C10H14N2O. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about Conformational analysis of 1-arylpiperazines and 4-arylpiperidines. Author is Dijkstra, Gerard D. H..

A conformational anal. of 1-arylpiperazines and 4-arylpiperidines is presented using mol.-mechanics and semi-empirical calculations Electronic effects of substituents on the aryl ring determine the conformational behavior of 1-arylpiperazines. Steric effects play a minor role. Electron-withdrawing substituents on the aryl moiety increase the conjugation between the anilino nitrogen lone pair and the π electrons of the aryl group and direct the orientation between the aryl and heterocycle towards the same plane. Electron-releasing substituents have the opposite effect and reduce the energy difference between a coplanar and perpendicular orientation between the rings. 4-Arylpiperidines prefer a perpendicular orientation between the rings.

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Ether – Wikipedia,
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SDS of cas: 56621-48-8. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about 9α-Hydroxy-12-{[4-(4-hydroxyphenyl)piperazin-1-yl]methyl}-4,8-dimethyl-3,14-dioxatricyclo[9.3.0.02,4]tetradec-7-en-13-one.

The title compound, C25H34N2O5, was synthesized from 9α-hydroxyparthenolide (9α-hydroxy-4,8-dimethyl-12-methylen-3,14-dioxa-tricyclo[9.3.0.02,4]tetradec-7-en-13-one), which in turn was isolated from the CHCl3 extract of the aerial parts of Anvillea radiata. Crystallog. data and at. coordinates are given. The mol. comprises a ten-membered ring fused to a five-membered ring with an addnl. epoxy ring system fused to the ten-membered ring. The five-membered ring also carries a 4-hydroxyphenyl-piperazin-1-ylmethyl substituent. The ten-membered ring adopts an approx. chair-chair conformation, while the piperazine ring displays a chair conformation and the five-membered ring shows an envelope conformation with the C atom closest to the hydroxy group forming the flap. Two C atoms in the Ph ring and the O atom of the hydroxyl group are disordered over two sites, with an occupancy ratio of 0.53(5):0.47(5). An intramol. O-H···N H-bond stabilizes the mol. conformation. In the crystal, C-H···O H bonds link the mols. into zigzag chains running along the a-axis direction.

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Category: ethers-buliding-blocks. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic. Author is Pace, Jennifer R.; DeBerardinis, Albert M.; Sail, Vibhavari; Tacheva-Grigorova, Silvia K.; Chan, Kelly A.; Tran, Raymond; Raccuia, Daniel S.; Wechsler-Reya, Robert J.; Hadden, M. Kyle.

Itraconazole (ITZ) is an FDA-approved member of the triazole class of antifungal agents. Two recent drug repurposing screens identified ITZ as a promising anticancer chemotherapeutic that inhibits both the angiogenesis and hedgehog (Hh) signaling pathways. We have synthesized and evaluated first- and second-generation ITZ analogs for their anti-Hh and antiangiogenic activities to probe more fully the structural requirements for these anticancer properties. Our overall results suggest that the triazole functionality is required for ITZ-mediated inhibition of angiogenesis but that it is not essential for inhibition of Hh signaling. The synthesis and evaluation of stereochem. defined des-triazole ITZ analogs also provides key information as to the optimal configuration around the dioxolane ring of the ITZ scaffold. Finally, the results from our studies suggest that two distinct cellular mechanisms of action govern the anticancer properties of the ITZ scaffold.

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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Application In Synthesis of 4-(Piperazin-1-yl)phenol. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about Electrochemical oxidation of 4-(piperazin-1-yl)phenols in the presence of indole derivatives: The unique regioselectivity in the synthesis of highly conjugated bisindolyl-p-quinone derivatives. Author is Amani, Amene; Khazalpour, Sadegh; Nematollahi, Davood.

The electrochem. oxidation of 4-(piperazin-1-yl)phenols were studied in the presence of indole derivatives as nucleophiles in H2O/MeCN mixture by cyclic voltammetry and controlled-potential coulometry. The reaction mechanism is believed to be oxidation of 4-(piperazin-1-yl)phenols, Michael addition reaction, oxidation of the formed adduct, another Michael addition reaction, oxidation of new adduct and hydrolysis (ECECEC). Bisindolyl-p-quinones were synthesized through the regioselective addition of indoles to electrochem. generated quinone imines in good yields at C electrode in a divided cell.

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Ether – Wikipedia,
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