67914-60-7 | Page 7 of 20 | Heterocyclic Building Blocks-piperazine

Zhao, Lihua’s team published research in Zhongguo Yaowu Huaxue Zazhi in 18 | CAS: 67914-60-7

Zhongguo Yaowu Huaxue Zazhi 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 C2H4ClNO, Category: piperazines.

Zhao, Lihua published the artcileDesign, synthesis and antitumor activity of thalidomide derivatives, Category: piperazines, the publication is Zhongguo Yaowu Huaxue Zazhi (2008), 18(1), 16-22, database is CAplus.

The antitumor activity of thalidomide derivatives [i.e., 2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione derivatives] was studied. A method for the synthesis of the title compounds is reported here. According to the structure of thalidomide, starting from β-D-glucosamine hydrochloride, twenty compounds were designed and synthesized. Product structures were determined by NMR, IR, MS. The target compounds were evaluated for their anticancer activity. The survival of 4T1 cells was determined Compounds substituted by a 3,4,6-tri-O-acetyl glucopyranoside have better antitumor activity than thalidomide dose.

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

Huang, Jian-Dong’s team published research in Wuji Huaxue Xuebao in 22 | CAS: 67914-60-7

Wuji Huaxue Xuebao 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, Computed Properties of 67914-60-7.

Huang, Jian-Dong published the artcileTetra-(acetyl piperazine phenoxy) phthalocyaninato zinc complexes and their proteins conjugates: synthesis, characterisation and photodynamic activities, Computed Properties of 67914-60-7, the publication is Wuji Huaxue Xuebao (2006), 22(3), 435-442, database is CAplus.

Two zinc phthalocyanines, tetra-α-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C₈₀H₇₂N₁₆O₈Zn) and tetra-β-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C₈₀H₇₂N₁₆O₈Zn), have been synthesized and characterized with ¹H NMR, MS, IR and elemental anal. The electronic absorption spectra of two complexes in common organic solvents (N,N-DMF, THF, n-octanol) were typical for nonaggregated phthalocyanines, showing a Q band at 693∼698 nm for 1 and 681 ∼ 682 nm for 2. This indicates that the Q band of zinc phthalocyanine with the substituted groups located in the α position is largely red shifted than that in the β position. The spectral features of complexes 1 and 2 in aqueous media suggest the α-substituted groups are more effective than β-substituted groups to hinder the aggregation of phthalocyanine mol. The interactions between two complexes with serum albumin and transferrin (BSA, HSA and apoTf) were investigated by absorption and fluorescence spectroscopy. The binding constants were found to be (1 ∼ 20) × 10⁵ mol^-1·L. By comparison, β-substituted 2 had stronger combining ability with albumin than that of α-substituted 1. The non-covalent conjugates (1-BSA, 2-BSA, 1-HSA, 1-apoTf and 1-FeTf) with the molar ratio of about 1 : 1 have also been prepared The photodynamic activities of two complexes and their bioconjugates against MCF-7 mammary tumor cells were examined The result shows that the photocytotoxicities of conjugates are higher than that of complexes 1 ∼ 2 and follows the order 1-BSA > 1-FeTf > 1-HSA, 1-apoTf > 2-BSA > 1>2.

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

Yang, Jiqiu’s team published research in Yiyao Gongye in | CAS: 67914-60-7

Yiyao Gongye 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 C24H12, Application In Synthesis of 67914-60-7.

Yang, Jiqiu published the artcileSynthesis of an antifungal drug ketoconazole, Application In Synthesis of 67914-60-7, the publication is Yiyao Gongye (1984), 1-4, database is CAplus.

The title compound [I, R = p-(4-acetylpiperazin-1-yl)phenyl] was prepared by condensation of I (R = MeSO₂) with piperazine II which was prepared starting from piperazine.

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

Chen, Yonghao’s team published research in Zhongguo Yiyao Gongye Zazhi in 39 | CAS: 67914-60-7

Zhongguo Yiyao Gongye Zazhi 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, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

Chen, Yonghao published the artcileSynthesis of ketoconazole by phase-transfer catalysis, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Zhongguo Yiyao Gongye Zazhi (2008), 39(8), 564-566, database is CAplus.

Antifungal drug ketoconazole was synthesized by utilization of phase-transfer catalysis from [2-bromomethyl-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl]methanol via acylation, N-alkylation with imidazole and hydrolysis, formation the active ester with methanesulfonyl chloride, and then condensation with the side chain 1-acetyl-4-(4-hydroxyphenyl)piperazine. The overall yield was about 30%.

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

Bruncko, Milan et al. published their research in Journal of Medicinal Chemistry in 2015 |CAS: 67914-60-7

The Article related to erratum structure antitumor neoplasm, Pharmacology: Structure-Activity and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

On May 14, 2015, Bruncko, Milan; Wang, Le; Sheppard, George S.; Phillips, Darren C.; Tahir, Stephen K.; Xue, John; Erickson, Scott; Fidanze, Steve; Fry, Elizabeth; Hasvold, Lisa; Jenkins, Gary J.; Jin, Sha; Judge, Russell A.; Kovar, Peter J.; Madar, David; Nimmer, Paul; Park, Chang; Petros, Andrew M.; Rosenberg, Saul H.; Smith, Morey L.; Song, Xiaohong; Sun, Chaohong; Tao, Zhi-Fu; Wang, Xilu; Xiao, Yu; Zhang, Haichao; Tse, Chris; Leverson, Joel D.; Elmore, Steven W.; Souers, Andrew J. published an article.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity [Erratum to document cited in CA162:393666]. And the article contained the following:

On pages 2183, the authors scrambled MCL-1 helix numbering in three locations and mislabeled an amino acid in one place; the corrections are given. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to erratum structure antitumor neoplasm, Pharmacology: Structure-Activity and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Bruncko, Milan et al. published their research in Journal of Medicinal Chemistry in 2015 |CAS: 67914-60-7

The Article related to structure antitumor neoplasm, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

On March 12, 2015, Bruncko, Milan; Wang, Le; Sheppard, George S.; Phillips, Darren C.; Tahir, Stephen K.; Xue, John; Erickson, Scott; Fidanze, Steve; Fry, Elizabeth; Hasvold, Lisa; Jenkins, Gary J.; Jin, Sha; Judge, Russell A.; Kovar, Peter J.; Madar, David; Nimmer, Paul; Park, Chang; Petros, Andrew M.; Rosenberg, Saul H.; Smith, Morey L.; Song, Xiaohong; Sun, Chaohong; Tao, Zhi-Fu; Wang, Xilu; Xiao, Yu; Zhang, Haichao; Tse, Chris; Leverson, Joel D.; Elmore, Steven W.; Souers, Andrew J. published an article.Application In Synthesis of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity. And the article contained the following:

Myeloid cell leukemia 1 (MCL-1) is a BCL-2 family protein that has been implicated in the progression and survival of multiple tumor types. Herein the authors report a series of MCL-1 inhibitors that emanated from a high throughput screening (HTS) hit and progressed via iterative cycles of structure-guided design. Advanced compounds from this series exhibited subnanomolar affinity for MCL-1 and excellent selectivity over other BCL-2 family proteins as well as multiple kinases and GPCRs. In a MCL-1 dependent human tumor cell line, administration of compound I rapidly induced caspase activation with associated loss in cell viability. The small mols. described herein thus comprise effective tools for studying MCL-1 biol. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Application In Synthesis of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to structure antitumor neoplasm, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Jiang, Xiong-Jie et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2006 |CAS: 67914-60-7

The Article related to phthalocyanine albumin conjugate photodynamic therapy, Pharmaceuticals: Pharmaceutics and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

On May 1, 2006, Jiang, Xiong-Jie; Huang, Jian-Dong; Zhu, Yu-Jiao; Tang, Fen-Xiang; Ng, Dennis K. P.; Sun, Jian-Cheng published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Preparation and in vitro photodynamic activities of novel axially substituted silicon (IV) phthalocyanines and their bovine serum albumin conjugates. And the article contained the following:

Two novel axially substituted phthalocyanines, namely bis(4-(4-acetylpiperazine)phenoxy)phthalocyaninatosilicon (IV) (1) and its N-methylated derivative 2, have been synthesized. The dicationic phthalocyanine 2 is non-aggregated in water and exhibits good photophys. properties. The non-covalent BSA conjugates of these compounds have also been prepared Compound 2 and the conjugate 2-BSA show extremely high photodynamic activities toward B16 melanoma cancer cell lines. The corresponding 50% growth-inhibitory (IC50) ratios are 33 and 38 nM, resp. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to phthalocyanine albumin conjugate photodynamic therapy, Pharmaceuticals: Pharmaceutics and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Yoneyama, Hiroshi et al. published their research in Shinkin to Shinkinsho in 1984 |CAS: 67914-60-7

The Article related to ketoconazole analog microbicide, bactericide ketoconazole derivative, fungicide ketoconazole derivative, Microbial Biochemistry: Other and other aspects.HPLC of Formula: 67914-60-7

Yoneyama, Hiroshi; Kobayashi, Satoshi; Okachi, Ryo published an article in 1984, the title of the article was Studies on antimicrobial activity of ketoconazole (KW-1414). VI. In vitro antifungal and antibacterial activity of ketoconazole (KW-1414) and its analogs.HPLC of Formula: 67914-60-7 And the article contains the following content:

Antifungal activities of structural analogs and metabolites of the synthetic antifungal agent ketoconazole (KCZ; KW-1414) (I) were investigated. R-39519 (desacetyl derivative) and R-44319 (trans isomer) had less antifungal activity against Candida species and dermatophytes than did I. HLI-151 (oxidized derivative) had no antifungal activity against any of the yeasts or fungi. Two known physiol. metabolites of I, R-43568 and T-1141, also showed no antifungal activity. I, R-39519, R-43568, and T-1141 showed no antibacterial activity against 12 strains of Lactobacillus species which are normal flora of the vagina. In blood of human volunteers administered orally 200 mg of I, no antifungal activity was detected except for I by bioautog. seeded with Kluyveromyces fragilis. In human urine of the same volunteers, no antifungal activity was detected by the bioautog. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).HPLC of Formula: 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Hu, Feng et al. published their research in European Journal of Medicinal Chemistry in 2021 |CAS: 67914-60-7

The Article related to fluorine 18 labeled radiotracer pet imaging dreadd receptor, (18)f, chemogenetics, dreadd, pet, sar, hm3dq, hm4di, Placeholder for records without volume info and other aspects.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

On March 5, 2021, Hu, Feng; Morris, Patrick J.; Bonaventura, Jordi; Fan, Hong; Mathews, William B.; Holt, Daniel P.; Lam, Sherry; Boehm, Matthew; Dannals, Robert F.; Pomper, Martin G.; Michaelides, Michael; Horti, Andrew G. published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was 18F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography. And the article contained the following:

Designer Receptors Exclusively Activated by Designer Drugs (DREADD) are a preclin. chemogenetic approach with clin. potential for various disorders. In vivo visualization of DREADDs has been achieved with positron emission tomog. (PET) using 11C radiotracers. The objective of this study was to develop DREADD radiotracers labeled with 18F for a longer isotope half-life. A series of non-radioactive fluorinated analogs of clozapine with a wide range of in vitro binding affinities for the hM3Dq and hM4Di DREADD receptors has been synthesized for PET. Compound [18F]7b was radiolabeled via a modified 18F-deoxyfluorination protocol with a com. ruthenium reagent. [18F]7b demonstrated encouraging PET imaging properties in a DREADD hM3Dq transgenic mouse model, whereas the radiotracer uptake in the wild type mouse brain was low. [18F]7b is a promising long-lived alternative to the DREADD radiotracers [11C]clozapine ([11C]CLZ) and [11C]deschloroclozapine ([11C]DCZ). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Beiginejad, Hadi et al. published their research in Monatshefte fuer Chemie |CAS: 67914-60-7

The Article related to electrophile isulfur nucleophile electrochem oxidation reaction mechanism, Placeholder for records without volume info and other aspects.SDS of cas: 67914-60-7

Beiginejad, Hadi; Rafiee, Zeinab published an article in , the title of the article was Dependence of mechanisms to thermodynamics in the electrochemical study of different electrophiles in the presence of some sulfur nucleophiles.SDS of cas: 67914-60-7 And the article contains the following content:

Abstract: Electrochem. study of different electrophiles in the presence of p-toluenesulfinic acid and 2-mercaptobenzothiazole as sulfur nucleophiles was investigated. Mechanistic study of the electrochem. reactions indicates that the electrochem. oxidation of some species in the presence of the sulfur groups has different mechanisms, but some other species in the presence of both sulfur nucleophiles have the same mechanism. To explain the reason for this difference, the computational study was used. Thermodn. investigation shows that when ΔGtot of the electrochem. oxidation of products are less than that of initial species, the electrochem. produced species can be oxidized during controlled-potential coulometry. The results of this work indicate that the computational study can be used to justify the reaction mechanisms. Cyclic voltammetry, linear sweep voltammetry, and controlled-potential coulometry were used to obtain the exptl. results. Also, by the use of BP86 level of theory and 6-31 + G(d,p) basis set, the theor. data were obtained. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).SDS of cas: 67914-60-7

The Article related to electrophile isulfur nucleophile electrochem oxidation reaction mechanism, Placeholder for records without volume info and other aspects.SDS of cas: 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics