Tag: M.W=100-200

Masih, Anup; Agnihotri, Amol K.; Srivastava, Jitendra K.; Pandey, Nidhi; Bhat, Hans R.; Singh, Udaya P. published the article 《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》. Keywords: pyrazole derivative antiinflammatory severe acute resipiratory syndrome coronavirus docking; NF-ĸB; SARS-CoV-2; docking; inflammation; pyrazole.They researched the compound: 4-(Piperazin-1-yl)phenol( cas:56621-48-8 ).Product Details of 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.

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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Safety of 4-(Piperazin-1-yl)phenol. 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 Synthesis of cycloalkylcarbamoyl substituted ketoconazole derivatives as antifungal agents.

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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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 Development of 1,3,4-Thiadiazole and Piperazine Fused Hybrid Quinazoline Derivatives as Dynamic Antimycobacterial Agents. Author is Patel, Amit B.; Rohit, Jignesh V..

Novel series of 1,3,4-thiadiazole and piperazine substituted quinazoline derivatives I [R = H, Cl, CF3, etc] were designed, synthesized, and tested in vitro for antimycobacterial activity. The synthetic procedure involved Suzuki C-C cross-coupling on a quinazoline ring and subsequently by the formation of 1,3,4-thiadiazole based piperazines. Many synthesized analogs were observed active against Mycobacterium H37Rv strain in preliminary anal. using the BACTEC MGIT method. A secondary antimycobacterial assay using the Lowenstein-Jensen MIC method indicates that I [R = bromo, trifluoromethyl, hydroxy] groups substituted analogs was showed strong efficacy in the range of 3.12-6.25 μg/mL. Active compounds were also tested for their cytotoxic activity against Human cervical (HeLa) cells at their MICs. The synthesized analogs were analyzed by IR, 1H NMR, 13 C NMR, MS, and elemental anal. for their structure determination

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Ether – Wikipedia,
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Recommanded Product: 56621-48-8. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about Different nematic phases and a switchable SmCP phase formed by homologues of a new class of asymmetric bent-core mesogens. Author is Schroeder, Martin W.; Diele, Siegmar; Pelzl, Gerhard; Dunemann, Ulrike; Kresse, Horst; Weissflog, Wolfgang.

Ten homologues of a class of asym. bent-shaped liquid crystal compounds were synthesized by reaction of 4-(4-alkyloxy-benzoyloxy)benzoyl chlorides with N-(4-hydroxyphenyl)piperazine. The mesophase structure and transitions of the compounds were studied by polarizing microscopy, x-ray diffraction, dielec. and electro-optical measurements. The long-chain members of the series C8-C16 exhibit the switchable polar antiferroelec. smectic phase ( SmCP). The short-chain members, C4-C8, form a nematic phase. The homologues C5 and C6 show a transition from nematic to a low-temperature phase which is indicated by a sharp peak in the DSC trace. Whereas the texture of the phase points to a nematic-smectic transition, the x-ray studies definitely prove a structure without any long range (or quasi long range) positional order in the low-temperature phase. A mol. model is described which exhibits structural features similar to those of a nematic phase, which can be regarded as the precursor of the following columnar phase (B1 phase).

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

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 Different nematic phases and a switchable SmCP phase formed by homologues of a new class of asymmetric bent-core mesogens. Author is Schroeder, Martin W.; Diele, Siegmar; Pelzl, Gerhard; Dunemann, Ulrike; Kresse, Horst; Weissflog, Wolfgang.

Ten homologues of a class of asym. bent-shaped liquid crystal compounds were synthesized by reaction of 4-(4-alkyloxy-benzoyloxy)benzoyl chlorides with N-(4-hydroxyphenyl)piperazine. The mesophase structure and transitions of the compounds were studied by polarizing microscopy, x-ray diffraction, dielec. and electro-optical measurements. The long-chain members of the series C8-C16 exhibit the switchable polar antiferroelec. smectic phase ( SmCP). The short-chain members, C4-C8, form a nematic phase. The homologues C5 and C6 show a transition from nematic to a low-temperature phase which is indicated by a sharp peak in the DSC trace. Whereas the texture of the phase points to a nematic-smectic transition, the x-ray studies definitely prove a structure without any long range (or quasi long range) positional order in the low-temperature phase. A mol. model is described which exhibits structural features similar to those of a nematic phase, which can be regarded as the precursor of the following columnar phase (B1 phase).

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Ether – Wikipedia,
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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 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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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. 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.Electric Literature of C10H14N2O.

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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Recommanded Product: 56621-48-8. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 4-(Piperazin-1-yl)phenol, is researched, Molecular C10H14N2O, CAS is 56621-48-8, about Synthesis of novel WAY 100635 derivatives containing a norbornene group and radiofluorination of [18F]AH1.MZ as a serotonin 5-HT1A receptor antagonist for molecular imaging. Author is Herth, Matthias M.; Kramer, Vasko; Roesch, Frank.

5-HT1A receptors are involved in a variety of psychiatric disorders and in vivo mol. imaging of the 5-HT1A status represents an important approach to analyze and treat these disorders. We report herein the synthesis of three new fluoroethylated 5-HT1A ligands (AH1.MZ, AH2.MZ and AH3.MZ) as arylpiperazine derivatives containing a norbornene group. AH1.MZ (Ki = 4.2 nM) and AH2.MZ (Ki = 30 nM) showed reasonable in vitro affinities to the 5-HT1A receptor, whereas AH3.MZ appeared to be non-affine toward the 5-HT1A receptor. The receptor profile of AH1.MZ and AH2.MZ showed selectivity within the 5-HT system. 18F-labeling via [18F]FETos to [18F]AH1.MZ was carried out in radiochem. yields of > 70%. The final formulation of injectable solutions including [18F]FETos synthon synthesis, radiosynthesis and semipreparative high-performance liquid chromatog. (HPLC) separation took no longer than 130 min and provided [18F]AH1.MZ with a purity of >98% as indicated by anal. HPLC analyses.

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Lee, Chi-Hoon; Kim, Hyung-Wook; Lee, Hoi-Seon published an article about the compound: 4-(Piperazin-1-yl)phenol( cas:56621-48-8,SMILESS:OC1=CC=C(N2CCNCC2)C=C1 ).Safety of 4-(Piperazin-1-yl)phenol. 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:56621-48-8) through the article.

Piperazine derivatives possess pharmacol. properties, yet the acaricidal activity of these compounds has not been investigated. This study was conducted to evaluate the color alteration and acaricidal activity of piperazine derivatives against Dermatophagoides spp. and Tyrophagus putrescentiae using filter paper and fumigant methods. In a fumigant bioassay, 1-phenylpiperazine (7.83 μg/cm2) against D. farinae was found to be 4.7-fold more toxic than DEET (36.84 μg/cm2), followed by benzyl benzoate (9.72 μg/cm2), piperazine (11.41 μg/cm2), 1-ethoxycarbonylpiperazine (20.14 μg/cm2), and 1-(2-methoxyphenyl)piperazine (22.14 μg/cm2). In a filter paper bioassay, 1-(2-methoxyphenyl)piperazine (3.65 μg/cm2) was 5.7-fold more toxic than DEET (20.64 μg/cm2), followed by 1-ethoxycarbonylpiperazine (4.02 μg/cm2), 1-phenylpiperazine (4.75 μg/cm2), benzyl benzoate (7.83 μg/cm2), and piperazine (10.59 μg/cm2). Similar results have been exhibited with piperazine derivatives against D. pteronyssinus. However, no activity against T. putrescentiae was observed for piperazine derivatives, except for piperazine. These results indicate that piperazine derivatives may be suitable as vapor-phase acaricide fumigants owing to their high volatility, acaricidal activity and safety. 1-Phenylpiperazine was found to be an excellent mite indicator based on the color change it induced. Taken together, these findings indicate that piperazine derivatives may be used to replace existing problematical acaricides owing to their activity and ability to act as a mite indicator.

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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, European Journal of Medicinal Chemistry called A novel class of ethacrynic acid derivatives as promising drug-like potent generation of anticancer agents with established mechanism of action, Author is Mignani, Serge; El Brahmi, Nabil; El Kazzouli, Said; Eloy, Laure; Courilleau, Delphine; Caron, Joachim; Bousmina, Mosto M.; Caminade, Anne-Marie; Cresteil, Thierry; Majoral, Jean-Pierre, which mentions a compound: 56621-48-8, SMILESS is OC1=CC=C(N2CCNCC2)C=C1, Molecular C10H14N2O, Electric Literature of C10H14N2O.

The well-known diuretic Ethacrynic acid (EA, Edecrin), showing low anti-proliferative activities, was chem. modified at different positions. The new EA derivatives have been tested in vitro in anti-proliferative assays on both tumor KB (epidermal carcinoma) and leukemia HL60 (promyelocytic) cells suitable targets for anticancer activity. Reduction of the α-β double bond of EA completely abolished anti-cancer activities, whereas introduction of either 2-(4-substituted phenyl)ethanamine (series A) or 4-(4-substituted phenyl)piperazine (series B) moieties generated compounds showing moderate to strong anti-proliferative activities against human cancer cell lines. Several substitutions on the Ph of these two moieties are tolerated. The mechanism of action of the EA derivatives prepared in this study is more complex than the inhibition of glutathione S-transferase π ascribed as unique effect to EA and might help to overcome tumor resistances.

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