Category: ethers-buliding-blocks

Quality Control of 4-(Piperazin-1-yl)phenol. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about Platinum(II) dithiocarbamate complexes [Pt(S2CNR2)Cl(PAr3)] as anticancer and DNA-damaging agents. Author is Kashif Amir, Muhammad; Hogarth, Graeme; Khan, Zaibunisa; Imran, Muhammad; Zia-ur-Rehman.

Following the fortunate discovery of cisplatin as an anticancer drug the search for new effective Pt-containing analogs with high potency but reduced side effects and resistance is of great importance. Herein, we report four new monofunctional platinum(II) dithiocarbamate complexes, [Pt(S2CNR2)Cl(PAr3)], and their activity against selected cancer cell lines. DFT-optimized structures reveal steric hindrance, similar to phenanthriplatin, from an axial C-H site of the triarylphosphine. High activity against selected cancer cell lines, MCF-7 > LU > Hepa-IcIc7, can be attributed to the axial protection offered by the aromatic C-H moiety, together with the lipophilicity and formation of bulkier and more hydrophobic DNA adducts. DNA binding, denaturing and plasmid cleavage studies demonstrate their potential to cleave DNA via electrostatic or covalent interactions. DFT and exptl. studies show the ability to replace chloride with different nucleophiles; substitution with smaller nucleophiles being fast while with larger nucleophiles is slow.

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

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Pharmaceutical Research called Structure-Function Analysis of Phenylpiperazine Derivatives as Intestinal Permeation Enhancers, Author is Fein, Katherine C.; Lamson, Nicholas G.; Whitehead, Kathryn A., which mentions a compound: 56621-48-8, SMILESS is OC1=CC=C(N2CCNCC2)C=C1, Molecular C10H14N2O, Formula: C10H14N2O.

Purpose: A major obstacle preventing oral administration of macromol. therapeutics is poor absorption across the intestinal epithelium into the bloodstream. One strategy to improve transport across this barrier is the use of chem. permeation enhancers. Several mol. families with permeation enhancing potential have been identified previously, including piperazines. In particular, 1-phenylpiperazine has been shown to enhance transepithelial transport with minimal cytotoxicity compared to similarly effective mols. To better understand how the chem. of 1-phenylpiperazine affects its utility as an intestinal permeation enhancer, this study examined a small library of 13 derivatives of 1-phenylpiperazine. Methods: The efficacy and cytotoxicity of 13 phenylpiperazine compounds were assessed in a Caco-2 model of the intestinal epithelium. Efficacy was measured using the paracellular diffusion marker calcein as well as by immunostaining and confocal imaging of Caco-2 monolayers. Results: Of the 13 derivatives, two enhanced the permeability of the fluorescent marker calcein over 100-fold. It was found that hydroxyl or primary amine substitutions on the Ph ring significantly increased toxicity, while aliphatic substitutions resulted in efficacy and toxicity profiles comparable to 1-phenylpiperazine. Conclusions: Several potent derivatives, including 1-methyl-4-phenylpiperazine and 1-(4-methylphenyl)piperazine, displayed lower toxicity than 1-phenylpiperazine, suggesting promise in future applications.

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Ether – Wikipedia,
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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-(Piperazin-1-yl)phenol(SMILESS: OC1=CC=C(N2CCNCC2)C=C1,cas:56621-48-8) is researched.Quality Control of Trimethylphosphineoxide. The article 《Synthesis and pharmacological evaluation of new 1-[3-(4-arylpiperazin-1-yl)-2-hydroxypropyl]-pyrrolidin-2-one derivatives with anti-arrhythmic, hypotensive, and α-adrenolytic activity》 in relation to this compound, is published in Archiv der Pharmazie (Weinheim, Germany). Let’s take a look at the latest research on this compound (cas:56621-48-8).

A series of novel arylpiperazines bearing a pyrrolidin-2-one fragment was synthesized and evaluated for the binding affinity of the α1- and α2-adrenoceptors (AR) and for the antiarrhythmic and hypotensive activities of the compounds The most potent and selective compound 1-[2-hydroxy-3-[4-[(2-hydroxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one 8 binds with pKi = 6.71 for α1-AR. Derivative 8 (I) was also the most active in the prophylactic antiarrhythmic test in adrenaline-induced arrhythmia in anesthetized rats. Its ED50 value equals 1.9 mg/kg (i.v.). Compounds with substituents such as a fluorine atom 4, a Me 5, or a hydroxyl 8 group, or two substituents such as fluorine/chlorine atoms and methoxy groups in the Ph ring, significantly decreased the systolic and diastolic pressure in normotensive anesthetized rats at a dosages of 5-10 mg/kg (i.v.). It was found that the presence of the piperazine ring and a hydroxy group in the second position of the Pr chain are critical structural features in determining the affinity of the compounds tested.

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Ether – Wikipedia,
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Recommanded Product: 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole. 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: 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole, is researched, Molecular C17H19N3O2S, CAS is 73590-85-9, about Baeyer-Villiger Monooxygenase-Mediated Synthesis of Esomeprazole As an Alternative for Kagan Sulfoxidation. Author is Bong, Yong Koy; Song, Shiwei; Nazor, Jovana; Vogel, Michael; Widegren, Magnus; Smith, Derek; Collier, Steven J.; Wilson, Rob; Palanivel, S. M.; Narayanaswamy, Karthik; Mijts, Ben; Clay, Michael D.; Fong, Ryan; Colbeck, Jeff; Appaswami, Amritha; Muley, Sheela; Zhu, Jun; Zhang, Xiyun; Liang, Jack; Entwistle, David.

A wild-type Baeyer-Villiger monooxygenase was engineered to overcome numerous liabilities to mediate a com. oxidation of pyrmetazole to esomeprazole, using air as the terminal oxidant in an almost exclusively aqueous reaction matrix. The developed enzyme and process compares favorably to the incumbent Kagan inspired chemocatalytic oxidation, as esomeprazole was isolated in 87% yield, in >99% purity, with an enantiomeric excess of >99%.

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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 Studies on the Human Metabolism and the Toxicologic Detection of the Cough Suppressant Dropropizine in Urine Using Gas Chromatography-Mass Spectrometry. Author is Staack, Roland F.; Theobald, Denis S.; Maurer, Hans H..

Studies are described on the metabolism and the toxicol. anal. of the nonopioid cough suppressant dropropizine [R,S-3-(4-phenyl-1-piperazinyl)1,2-propandiol, DRO] in human urine using gas chromatog.-mass spectrometry (GC-MS). The metabolism studies showed that DRO was metabolized in humans mainly by hydroxylation of the aromatic ring, by N-dealkylation of the parent drug and of the hydroxyl-metabolite to the corresponding N-phenylpiperazines, and by degradation of the piperazine moiety. The authors’ systematic toxicol. anal. (STA) procedure using full-scan GC-MS after acid hydrolysis, liquid-liquid extraction, and microwave-assisted acetylation allowed the unambiguous detection of DRO and its above-mentioned metabolites in human urine up to about 32 h after intake of a single common therapeutic dose. The target analytes were found to be the parent compound DRO (earlier phase of excretion) and the hydroxylated metabolite para-hydroxy-DRO (later phase of excretion). Both allowed unambiguous detection of an intake of DRO and also differentiation from other phenylpiperazine derivatives

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

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 56621-48-8, is researched, Molecular C10H14N2O, about Electrochemical Synthesis of a New Derivative of 1,4-Dihydroxybenzene: Embedded Nucleophile in the Structure of Electrophile, the main research direction is electrosynthesis derivative dihydroxybenzene embedded nucleophile structure electrophile.COA of Formula: C10H14N2O.

The electrochem. oxidation of 4-(Piperazin-1-yl)phenols (1a,b) was studied in the H2O, MeCN and nitromethan by cyclic voltammetry and controlled-potential coulometry. P-quinone-imines generated of oxidation 4-(Piperazin-1-yl)phenols after the hydrolysis reaction participate in Michael-addition reactions with released piperazine of hydrolysis reaction of p-quinone imines. The present work led to the development of a facile and environmentally friendly electrochem. method for the synthesis of a new derivative of 1,4-dihydroxybenzene under green conditions. The effect of H2O as a solute on the electrochem. response of 4-(Piperazin-1-yl)phenols (1a,b) was examined in the MeCN (AN) and nitromethane (NM) solvent.

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

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Itraconazole Side Chain Analogues: Structure-Activity Relationship Studies for Inhibition of Endothelial Cell Proliferation, Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) Glycosylation, and Hedgehog Signaling, Author is Shi, Wei; Nacev, Benjamin A.; Aftab, Blake T.; Head, Sarah; Rudin, Charles M.; Liu, Jun O., which mentions a compound: 56621-48-8, SMILESS is OC1=CC=C(N2CCNCC2)C=C1, Molecular C10H14N2O, Application In Synthesis of 4-(Piperazin-1-yl)phenol.

Itraconazole is an antifungal drug that was recently found to possess potent antiangiogenic activity and anti-hedgehog (Hh) pathway activity. To search for analogs of itraconazole with greater potency and to understand the structure-activity relationship in both antiangiogenic and Hh targeting activity, 25 itraconazole side chain analogs were synthesized and assayed for inhibition of endothelial cell proliferation and Gli1 transcription in a medulloblastoma (MB) culture. Through this anal., we have identified analogs with increased potency for inhibiting endothelial cell proliferation and the Hh pathway, as well as VEGFR2 glycosylation that was recently found to be inhibited by itraconazole. An SAR anal. of these activities revealed that potent activity of the analogs against VEGFR2 glycosylation was generally driven by side chains of at least four carbons in composition with branching at the α or β position. SAR trends for targeting the Hh pathway were divergent from those related to HUVEC proliferation or VEGFR2 glycosylation. These results also suggest that modification of the sec-Bu side chain can lead to enhancement of the biol. activity of itraconazole.

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

Recommanded Product: 56621-48-8. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. 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

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Domino Reaction of Arylglyoxals with Pyrazol-5-amines: Selective Access to Pyrazolo-Fused 1,7-Naphthyridines, 1,3-Diazocanes, and Pyrroles, published in 2014-06-06, which mentions a compound: 118430-78-7, mainly applied to domino heterocyclization arylglyoxal pyrazolamine pyrazolo naphthyridine diazocane pyrrole, HPLC of Formula: 118430-78-7.

New multicomponent domino reactions of arylglyoxals with pyrazol-5-amines have been established, providing selective access to unprecedented pyrazolo-fused 1,7-naphthyridines, 1,3-diazocanes, and pyrroles (up to 52 examples). The unreported dipyrazolo-fused 1,7-naphthyridines were regioselectively synthesized through a special double [3 + 2 + 1] heteroannulation accompanied by direct C-C formation between two electrophilic sites of arylglyoxals [e.g., PhCOCH(OH)2 + 1,3-dimethyl-5-pyrazolamine in presence of TsOH → I (70%)]. The unusual [3 + 3 + 1 + 1] cyclization resulted in 20 examples of novel dipyrazolo-fused 1,3-diazocanes [e.g., PhCOCH(OH)2 + 1-methyl-3-phenyl-5-pyrazolamine in presence of TsOH → II (71%)], whereas pyrrolo[2,3-c]pyrazoles were obtained in good yields by varying arylglyoxals and pyrazol-5-amines in the ratio 1:2 [e.g., PhCOCH(OH)2 + 1-phenyl-3-methyl-5-pyrazolamine in presence of TsOH → III (78%)]. Mechanisms of formation of these three new types of heterocycles are also proposed.

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

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole, is researched, Molecular C17H19N3O2S, CAS is 73590-85-9, about Oxygen dependence of omeprazole clearance and sulfone and sulfide metabolite formation in the isolated perfused rat liver, the main research direction is omeprazole metabolism liver oxygen dependence.Related Products of 73590-85-9.

This study, in the isolated perfused rat liver, examined the O dependence of the hepatic elimination of omeprazole, a drug which undergoes extensive oxidative metabolism in the rat. The relationship between hepatic O supply and the production of omeprazole’s oxidative sulfone and reductive sulfide metabolites was also examined Rat livers were perfused with a perfusate containing 5 μg omeprazole/mL in a single-pass design. Omeprazole clearance and the formation clearance of the 2 metabolites were measured in each liver during normal oxygenation, at different levels of hypoxia and after reoxygenation. There was a linear relationship between omeprazole clearance and O delivery over the whole range studied. Production of the sulfone was similarly O-dependent whereas the sulfide was detectable only after a significant reduction in oxygenation. In further experiments the O dependence of omeprazole clearance was not altered when the concentration of drug was lowered to 1 μg/mL. This study shows that O delivery is a critical determinant of the rate of oxidative drug metabolism in the isolated liver and supports the contention that reductions in hepatic O supply may alter the hepatic disposition of oxidatively metabolized drugs in vivo.

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