Tag: 200-300

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

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

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

On March 12, 2020, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Crews, Craig M.; Jaime-Figueroa, Saul; Dong, Hanqing; Qian, Yimin; Zimmerman, Kurt published a patent.Formula: C15H29N3O2 The title of the patent was Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides. And the patent contained the following:

The present disclosure relates to bifunctional compounds, ULM- L-PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the resp. E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Formula: C15H29N3O2

The Article related to polycyclic targeted protein kinase raf, Pharmaceuticals: Pharmaceutics and other aspects.Formula: C15H29N3O2

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

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

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

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

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

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

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

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

On January 17, 2022, Lodha, Kamlesh K.; Wavhal, Deepak S.; Bhalekar, Sujit B.; Meshram, Rohan J.; Shinde, Vaishali S. published an article.Computed Properties of 67914-60-7 The title of the article was Exploring new tetrahydrothienopyridine derivatives as platelet agglutination inhibitors: synthesis, biological evaluation and In silico study. And the article contained the following:

The P2Y12 receptor is the major target for antithrombic drugs which plays a key role in platelet activation. New derivatives of 4,5,6,7-tetrahydrothieno[3,2-c]pyridine (THP) were designed targeting P2Y12 receptor. An efficient route was developed for synthesis of THP derivatives and subsequently evaluated for their antiplatelet agglutination activity. Amongst the synthesized THP derivatives (4 a-4 g), the compounds 4 a and 4 g displayed significant activity (with 88.25 and 70.17 % inhibition) as compared to other analogs and comparable with that of the reference drugs, aspirin and prasugrel. Data extracted from computational chem. techniques such as mol. docking, provided the structural rationale for the observed platelet agglutination inhibition by the newly synthesized tetrahydrothienopyridine analogs. We proposed the involvement of residues such as Cys-194 in the formation of the covalent adduct with the active metabolite of tetrahydrothienopyridine derivatives This study also put forward the possibility of the existence of an alternate pathway for metabolizing the tetrahydrothienopyridine compounds The structural data presented in this study is expected to accelerate the research on developing a tetrahydrothienopyridine scaffold as an effective antithrombotic therapeutic modality. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Computed Properties of 67914-60-7

The Article related to platelet agglutination tetrahydrothienopyridine screening antiplatelet, Placeholder for records without volume info and other aspects.Computed Properties of 67914-60-7

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

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

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

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

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