Month: November 2022

Daneshyar, Anahita published the artcileElectrochemical synthesis of a new phosphonium betaine. Kinetic evaluation and antibacterial susceptibility, Quality Control of 67914-60-7, the publication is Electrochimica Acta (2019), 134893, database is CAplus.

Cyclic voltammetry, controlled-potential coulometry, chronoamperometry, chronocoulometry and chronopotentiometry methods were used for the electrochem. study of 1-acetyl-4-(4-hydroxyphenyl)piperazine (APIP) in the presence of PPh₃ (TPP) as a nucleophile. Electrochem. generated APIP_ox can serve as a Michael acceptor for nucleophilic attack by TPP to yield a new phosphonium betaine (APTP). The authors prepared a new product in good yield and purity by reaction of TPP with APIP_ox in an undivided cell equipped with C anode. Based on an EC mechanism, the observed homogeneous rate constant (k_obs) of the Michael addition reaction of APIP_ox with TPP were estimated by comparing the exptl. cyclic voltammograms with the digital simulated results. Also, electrochem. oxidation of APIP was studied both exptl. and theor. to provide insight into the influence of natural charge and thermodn. stability parameters on the type of chem. reaction which follows APIP_ox. The synthesized compound was evaluated for in vitro antibacterial.

Electrochimica Acta published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Quality Control of 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Beiginejad, Hadi published the artcileEfficient factors on the hydrolysis reaction rate of some para-aminophenol derivatives in acidic pHs, Application of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Journal of the Electrochemical Society (2013), 160(8), H469-H473, database is CAplus.

Electrochem. oxidation of some p-aminophenol derivatives (1-5) in acidic solutions was studied both exptl. and theor. to provide insight into the influence of some factors on the hydrolysis reaction rate. The result of this work shows that the electrogenerated p-quinoneimines participate in the hydrolysis reaction and are converted to the p-benzoquinone. The hydrolysis reaction rate strongly depends on the structure of the p-aminophenols and solution’s pH. The observed homogeneous rate constants of hydrolysis (k^obs_hyd) of p-quinoneimines were determined using digital simulation technique. The effect of different parameters such as: change of Gibbs free energy (ΔG) of the electrochem. oxidation of para-aminophenol derivatives (1-5), charge of reaction site, N-C₄ bond order (Wiberg Bond Indexes, WBIs) and the nature of substituted group, on the hydrolysis rate constant were also studied. All calculations were performed using D. Functional Theory (DFT) both BP86 and B3LYP levels of theory and 6-311G (p,d) basis set. The N-C₄ bond order and charge on the reaction site play significant roles in hydrolysis reaction’s rate.

Journal of the Electrochemical Society published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Application of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Amani, Ameneh published the artcileOne-pot electrochemical synthesis of highly symmetric and conjugated coumarin derivative, Synthetic Route of 67914-60-7, the publication is Journal of the Iranian Chemical Society (2018), 15(12), 2669-2674, database is CAplus.

A facile and one pot electrochem. synthesis of disubstituted hydroquinone generated from the electrochem. oxidation of 4-1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone in the presence of 4-hydroxy-6,7-dimethylcoumarin was reported. The results revealed that p-quinone imine derived from oxidation of 4-1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone participated in Michael addition reactions with 4-hydroxy-6,7-dimethylcoumarin and followed by a hydrolysis reaction attain to the highly sym. and conjugated coumarin derivative A new product in good yield was derived based on controlled potential electrochem. oxidation at carbon electrode in a divided cell.

Journal of the Iranian Chemical Society published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Synthetic Route of 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Amani, Amene published the artcileElectrochemical synthesis of new coumarin derivatives of potential biological significance, Quality Control of 67914-60-7, the publication is Journal of Electroanalytical Chemistry (2012), 11-15, database is CAplus.

Electrochem. synthesis of some new coumarin derivatives was carried out via the electrochem. oxidation of 1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone (1) in the presence of 4-hydroxycoumarin and 4-hydroxy-6-methylcoumarin (2a,b). Electrogenerated p-quinone imine, participated in Michael type reaction with 2a,b and after hydrolysis reaction is converted to the corresponding coumarin derivatives This method provides a 1-pot procedure for the synthesis of new coumarin derivatives of potential biol. significance.

Journal of Electroanalytical Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Quality Control of 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Amani, Amene published the artcileElectrochemical Synthesis Based on the Oxidation of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone in the Presence of Nucleophiles, Category: piperazines, the publication is Journal of Organic Chemistry (2012), 77(24), 11302-11306, database is CAplus and MEDLINE.

Electrochem. oxidation of piperazinylphenol I (R = R¹ = H) with 2-benzoxazolethiol or 2-benzothiazolethiol yielded the bis(benzoxazolethiyl)phenol I (R = R¹ = 2-benzoxazolylthio) and bis(benzothiazolethiyl)phenol I (R = R¹ = 2-benzothiazolylthio) in 87% and 93% yields, resp. Further electrochem. oxidation of I (R = R¹ = 2-benzothiazolylthio) in the presence of p-toluenesulfinic acid (TsH) gave (tosyl)(benzothiazolylthio)quinone II (Ts = 4-MeC₆H₄SO₂); attempted direct electrochem. synthesis of II from I (R = R¹ = H), 2-benzothiazolethiol, and TsH, from I (R = R¹ = 2-benzothiazolylthio) and TsH in the absence of elec. potential, and from I (R = Ts; R¹ = H) and 2-benzothiazolethiol were not successful. Cyclic voltammetric measurements during the reactions of I (R = H, 2-benzothiazolylthio, Ts; R¹ = H, 2-benzothiazolylthio) were used to delineate the mechanisms of formation of I (R = R¹ = 2-benzothiazolylthio) and II.

Journal of Organic Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Kondo, Takashi published the artcileDesign and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group, Related Products of piperazines, the publication is Bioorganic & Medicinal Chemistry (2008), 16(4), 1613-1631, database is CAplus and MEDLINE.

A series of (4β-substituted)-L-prolylpyrrolidine analogs lacking the electrophilic nitrile function were synthesized and their dipeptidyl peptidase IV (DPP-IV) inhibitory activity and duration of ex vivo activity were evaluated. Structural optimization of the analog (I), which was found by high-speed analog synthesis, was carried out to improve the potency and duration of action. A representative compound (II) was evaluated to assess its effect on the plasma glucose level after the oGTT (oral glucose tolerance test) in normal rats. Structure-activity relationships (SAR) are also presented.

Bioorganic & Medicinal Chemistry published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Related Products of piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Palazzolo, Isabella published the artcileB2 attenuates polyglutamine-expanded androgen receptor toxicity in cell and fly models of spinal and bulbar muscular atrophy, Name: (4-Chlorophenyl)(4-(8-nitroquinolin-5-yl)piperazin-1-yl)methanone, the publication is Journal of Neuroscience Research (2010), 88(10), 2207-2216, database is CAplus and MEDLINE.

Expanded polyglutamine tracts cause neurodegeneration through a toxic gain-of-function mechanism. Generation of inclusions is a common feature of polyglutamine diseases and other protein misfolding disorders. Inclusion formation is likely to be a defensive response of the cell to the presence of unfolded protein. Recently, the compound B2 has been shown to increase inclusion formation and decrease toxicity of polyglutamine-expanded huntingtin in cultured cells. We explored the effect of B2 on spinal and bulbar muscular atrophy (SBMA). SBMA is caused by expansion of polyglutamine in the androgen receptor (AR) and is characterized by the loss of motor neurons in the brainstem and spinal cord. We found that B2 increases the deposition of mutant AR into nuclear inclusions, without altering the ligand-induced aggregation, expression, or subcellular distribution of the mutant protein. The effect of B2 on inclusions was associated with a decrease in AR transactivation function. We show that B2 reduces mutant AR toxicity in cell and fly models of SBMA, further supporting the idea that accumulation of polyglutamine-expanded protein into inclusions is protective. Our findings suggest B2 as a novel approach to therapy for SBMA. © 2010 Wiley-Liss, Inc.

Journal of Neuroscience Research published new progress about 115687-05-3. 115687-05-3 belongs to piperazines, auxiliary class Epigenetics,Sirtuin, name is (4-Chlorophenyl)(4-(8-nitroquinolin-5-yl)piperazin-1-yl)methanone, and the molecular formula is C20H17ClN4O3, Name: (4-Chlorophenyl)(4-(8-nitroquinolin-5-yl)piperazin-1-yl)methanone.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Kamata, Ryo published the artcileAgonistic effects of diverse xenobiotics on the constitutive androstane receptor as detected in a recombinant yeast-cell assay, Application of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Toxicology In Vitro (2018), 335-349, database is CAplus and MEDLINE.

The constitutive androstane receptor (CAR) is a nuclear receptor and transcription factor regulating proteins involved in xenobiotic metabolism Agonist activation of the CAR can trigger metabolic activation and toxification as well as detoxification and clearance; accordingly, xenobiotic substances acting as CAR ligands may pose a threat to human and animal health. The authors used yeast cells transduced with the human CAR and the response pathway to measure the CAR-agonistic activities of 549 synthetic or natural compounds: 216 of the tested compounds exhibited CAR-agonistic effects. Eighty-four percent of CAR-activating compounds were aromatic compounds, and >65% of these active compounds were aromatic hydrocarbons, bisphenols, monoalkyl phenols, phthalates, styrene dimers, di-Ph ethers, organochlorines, and organophosphates. The ten most potent compounds were 4-tert-octylphenol (4tOP; reference substance), 4-nonylphenol, diethylstilbestrol, benzyl Bu phthalate, 2-(4-hydroxyphenyl)-2,4,4-trimethylchroman, o,p’-DDT, methoxychlor, di-Pr phthalate, hexestrol, and octachlorostyrene. The activities of these nine non-reference compounds exceeded 10% of the 4tOP activity. Anal. of para-monoalkyl phenols suggests that branching of the alkyl group and chlorination at the ortho position raises potency. This study provides critical information for identifying the potential of CAR-mediated toxic hazards and for understanding the relevant mechanism.

Toxicology In Vitro published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Application of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Nadaf, Afra Quasar A. published the artcileSynthesis of 6-[4-(4-Propoxyphenyl)piperazin-1-yl]-9H-purine Derivatives as Antimycobacterial and Antifungal Agents: In Vitro Evaluation and In Silico Study, Related Products of piperazines, the publication is Chemistry & Biodiversity (2020), 17(5), e2000053, database is CAplus and MEDLINE.

A series of novel alkyl substituted purines were synthesized. 6-[4-(4-Propoxyphenyl)piperazin-1-yl]-9H-purine was used as the key starting material, which was synthesized via a multistep protocol and finally subjected for N-alkylation with various alkyl halides with an aim to get prospective antimicrobial agents. The structures of the novel compounds were established by substantiating them through spectral techniques like 1H-NMR, 13C-NMR, FT-IR and EI-MS. They were explored for antitubercular activity against Mycobacterium tuberculosis H37RV. Furthermore, they were checked for their antimicrobial activity concerning bacterial and fungal strains. The title compounds exhibited considerable antimicrobial activity without any significant toxicity. In silico studies depicted their good binding profile against Mycobacterium tuberculosis enoyl reductase (InhA; PDB ID: 4TZK) and Candida albicans dihydrofolate reductase (PDB ID: 1AI9). The title compounds obeyed Lipinski’s parameters and have exhibited good drug-like properties.

Chemistry & Biodiversity published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Related Products of piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Yadav, M. R. published the artcileDesign and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α₁– and AII-receptors antagonism, SDS of cas: 178928-58-0, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(13), 3959-3966, database is CAplus and MEDLINE.

Multiple-targeted ligands can have certain advantages for the management of hypertension which has multiple controls. Mols. with dual bioactivities are available in literature for treating metabolic disorders like diabetes, hypertension and hypercholesterolemia. After scrutinizing the SAR of prazosin-type α₁-blockers and AII-antagonists it was planned to develop dual α₁– and AII-antagonists. Five series of quinazoline derivatives were synthesized and evaluated as dual α₁– and AII-antagonists on rat aortic strips for the blockade of known α₁– and AII-agonist mediated contractions. Many compounds showed balanced activity on both the receptors but compound (22) was the most active derivative having higher antagonistic activity on both the receptors. In the in vivo experiments the chosen compound (22) was slightly less active than prazosin but was equipotent to losartan. These findings shed a new light on the structural requirements for both α₁– and AII-receptor antagonists.

Bioorganic & Medicinal Chemistry Letters published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C44H28ClFeN4, SDS of cas: 178928-58-0.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics