Tag: M.W=100-200

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Syntheses and radiofluorination of two derivatives of 5-cyano-indole as selective ligands for the dopamine subtype-4 receptor, published in 2006-01-31, which mentions a compound: 56621-48-8, Name is 4-(Piperazin-1-yl)phenol, Molecular C10H14N2O, Application In Synthesis of 4-(Piperazin-1-yl)phenol.

Two fluoroethoxy derivatives, namely 2-{4-[2-(2-fluoroethoxy)phenyl]piperazin-1-ylmethyl}indole-5-carbonitrile (I) and 2-{4-[4-(2-fluoroethoxy)phenyl]piperazin-1-ylmethyl}indole-5-carbonitrile (II) were synthesized as analogs of the selective D4 receptor ligand 2-[4-(4-fluorophenyl)piperazin-1-ylmethyl]indole-5-carbonitrile (FAUC 316). In vitro characterization using CHO-cells expressing different dopamine receptor subtypes gave Ki = 2.1 and 9.9 nM of I and II, resp., for the dopamine D4 subtype and displayed a 420-fold D4-selectivity over D2 receptors for II. Candidate II revealed substantially reduced α1 and serotoninergic binding affinities in comparison to I. To provide potential PET imaging probes for the dopamine D4 receptor, 18F-labeling conditions using [18F]fluoroethyl tosylate were optimized and led to radiochem. yields of 81 ± 5% (18F-I) and 47 ± 4% (18F-II) (n = 3, decay-corrected, referred to labeling agent), resp. Thus, 18F-fluoroethylation favorably at the para position of the phenylpiperazine moiety of the 5-cyanoindole framework proved to be tolerated by D4 receptors and could also be applied to alternative scaffolds to develop D4 radioligand candidates for PET with improved D4 receptor affinity and selectivity.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Quantitative structure-hepatotoxicity assessment of series arylpiperazine-N1-substituted theobromine derivatives, published in 2020-02-29, which mentions a compound: 56621-48-8, Name is 4-(Piperazin-1-yl)phenol, Molecular C10H14N2O, Product Details of 56621-48-8.

In this work series new theobromines, compounds I [R = benzyl, 4-hydroxyphenyl, bis(4-fluorophenyl)methyl, etc.; n = 3,4] with established antioxidant and antiproliferative activities were evaluated for their hepatotoxic effects on cellular and sub-cellular level. On isolated rat hepatocytes, compounds I [R = 4-hydroxyphenyl, n = 3,4] expressed lowest toxicity, while compounds I [R = bis(4-fluorophenyl)methyl, n = 3,4] showed highest toxicity. Compounds I [R = bis(4-fluorophenyl)methyl, n = 3,4] showed the most evident pro-oxidant effect in a lipid peroxidation model on rat liver microsomes, followed by compounds I [R = 4-fluorophenyl, n = 3,4], while the other compounds didn’t reveal statistically significant pro-oxidant effects. The performed quant. structure-toxicity relationship (QSTR) anal. show that increased lipophilicity of the tested compounds pos. correlates to their hepatotoxicity. Opposite, the presence in the structure of highly pos. H-atoms and strongly neg. oxygen, possibly originating from hydrogen bond donor groups, are associated with reduced hepatotoxicity.

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Reference of 4-(Piperazin-1-yl)phenol. 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 Acaricidal properties of piperazine and its derivatives against house-dust and stored-food mites. Author is Lee, Chi-Hoon; Kim, Hyung-Wook; Lee, Hoi-Seon.

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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Recommanded Product: 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 Electrochemical oxidation of acetaminophen and 4-(piperazin-1-yl)phenols in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone.

A facile and 1-pot electrochem. method for the synthesis of mono and disubstituted 1,4-benzoquinones generated from the electrochem. oxidation of 1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone (1a), 4-(piperazin-1-yl)phenol (1b) and acetaminophen (8) in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone (3) as nucleophile is reported. The electrochem. generated electrophiles derived from the oxidation of 1a, 1b and 8 participate in Michael-addition reactions with 3. The authors report the synthesis of mono and diquinolone substituted of 1,4-benzoquinone in good yields based on controlled potential condition at C electrode in a divided cell.

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Staack, R. F.; Theobald, D. S.; Paul, L. D.; Springer, D.; Kraemer, T.; Maurer, H. H. published an article about the compound: 4-(Piperazin-1-yl)phenol( cas:56621-48-8,SMILESS:OC1=CC=C(N2CCNCC2)C=C1 ).SDS of cas: 56621-48-8. 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.

The in vivo metabolism of 1-(4-methoxyphenyl)piperazine (MeOPP), a novel designer drug, was studied in male Wistar rats. MeOPP was mainly O-demethylated to 1-(4-hydroxyphenyl)piperazine (4-HO-PP) in addition to degradation of the piperazine moiety. O-demethylation, the major metabolic step, was studied with cDNA-expressed human hepatic cytochrome P 450 (CYP) enzymes in pooled human liver microsomes (pHLM) and in single donor human liver microsomes with CYP2D6 poor metabolizer genotype (PM HLM). CYP2D6 catalyzed O-demethylation with apparent Km and Vmax values of 48.34 μM and 5.44 pmol min-1 pmol-1 CYP, resp. pHLM catalyzed the monitored reaction with an apparent Km = 204.80 μM and Vmax = 127.50 pmol min-1 mg-1 protein. The CYP2D6-specific chem. inhibitor quinidine (1 and 3 μM) significantly inhibited 4-HO-PP formation by 71.9% and by 98.5%, resp., in incubation mixtures with pHLM and 200 μM MeOPP. O-demethylation was significantly lower in PM HLM compared with pHLM (70.6%). These data suggest that polymorphically expressed CYP2D6 is the enzyme mainly responsible for MeOPP O-demethylation.

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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 Synthesis and bioevaluation of 4,5,6,7-tetrahydrobenzo[d]isoxazole derivatives as melanogenesis inhibitors, published in 2014-02-20, which mentions a compound: 56621-48-8, mainly applied to arylpiperazinyl tetrahydrobenzoisoxazolyl methanone preparation melanogenesis inhibitor SAR; tetrahydrobenzoisoxalyl carboxylic acid chloride preparation arylpiperazine amide coupling, Recommanded Product: 4-(Piperazin-1-yl)phenol.

A series of 4,5,6,7-tetrahydrobenzo[d]isoxazole derivatives I [R1 = H, tert-butyl; R2 = 4-OH, 4-OMe, 2-OMe, 4-CF3, 4-F] was prepared via amide coupling of arylpiperazines with corresponding 4,5,6,7-tetrahydrobenzo[d]isoxazole carboxylic acid chlorides. Addnl., 4,5,6,7-tetrahydrobenzo[d]isoxazole derivative I [R1 = H; R2 = 4-OEt] was synthesized by O-alkylation of compound I [R1 = H; R2 = 4-OH] using iodoethane. The synthesized compounds were tested for their melanogenesis inhibiting activity through potential down-regulation of tyrosinase expression. Among the tested compounds, compounds I [R1 = H; R2 = 4-OMe, 2-OMe, 4-CF3] displayed better melanogenesis inhibiting activity than well-known compounds Arbutin and Kojic acid, without intrinsic cytotoxicity.

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Reference of 4-(Piperazin-1-yl)phenol. 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 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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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.Reference of 4-(Piperazin-1-yl)phenol. The article 《Structure-Function Analysis of Phenylpiperazine Derivatives as Intestinal Permeation Enhancers》 in relation to this compound, is published in Pharmaceutical Research. Let’s take a look at the latest research on this compound (cas:56621-48-8).

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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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.Velingkar, V. S.; Ahire, D. C.; Koihe, N. S.; Shidore, M. S. researched the compound: 4-(Piperazin-1-yl)phenol( cas:56621-48-8 ).Computed Properties of C10H14N2O.They published the article 《Synthesis of substituted 2-aminobenzothiazoles as non-acidic antiinflammatory agents》 about this compound( cas:56621-48-8 ) in Indian Journal of Heterocyclic Chemistry. Keywords: benzothiazolyl chloroacetamide reaction amine; benzothiazole aminoacetamide preparation antiinflammatory activity. We’ll tell you more about this compound (cas:56621-48-8).

The title compounds were synthesized and characterized by spectral anal. (IR, 1H NMR, mass spectroscopy). The effect of the synthesized compounds on inflammation, using the carrageenan induced mouse paw edema model was studied. In general, the compounds were found to be potent antiinflammatory agents. Antiinflammatory activity was influenced by some structural characteristics of the synthesized compounds

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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 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.Name: 4-(Piperazin-1-yl)phenol.

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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