Marder, Stephen et al. published their research in European Neuropsychopharmacology in 2019 | CAS: 839712-12-8

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Synthetic Route of C21H32Cl2N4O

Efficacy of cariprazine across symptom domains in patients with acute exacerbation of schizophrenia: Pooled analyses from 3 phase II/III studies was written by Marder, Stephen;Fleischhacker, W. Wolfgang;Earley, Willie;Lu, Kaifeng;Zhong, Yan;Nemeth, Gyorgy;Laszlovszky, Istvan;Szalai, Erzsebet;Durgam, Suresh. And the article was included in European Neuropsychopharmacology in 2019.Synthetic Route of C21H32Cl2N4O This article mentions the following:

Schizophrenia affects various symptom domains, including pos. and neg. symptoms, mood, and cognition. Cariprazine, a dopamine D3/D2 receptor partial agonist and serotonin 5-HT1A receptor partial agonist, with preferential binding to D3 receptors, is approved for the treatment of adult patients with schizophrenia and mania associated with bipolar I disorder. Post hoc analyses evaluated mean change from baseline to week 6 in PANSS-derived symptom factors (pos. symptoms, neg. symptoms, disorganized thought, uncontrolled hostility/excitement, anxiety/depression) and PANSS single items for cariprazine vs. placebo. P values were not adjusted for multiple comparisons. At week 6, statistically significant differences vs. placebo were seen for cariprazine on all 5 PANSS factors (P < 0.01 all). Effects sizes ranged from 0.21 (anxiety/depression) to 0.47 (disorganized thought). Dose-response anal. from the fixed-dose studies found significant differences for all cariprazine doses (1.5, 3.0, 4.5, and 6.0 mg/d) vs. placebo in PANSS total score, and in neg. symptom and disorganized thought factor scores (P < 0.001). Differences between cariprazine and placebo were also statistically significant on 26 of 30 PANSS single items (P < 0.05). In these post hoc analyses, cariprazine was effective vs. placebo in improving all 5 PANSS factor domains, suggesting that it may have broad-spectrum efficacy in patients with acute schizophrenia. In the experiment, the researchers used many compounds, for example, 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8Synthetic Route of C21H32Cl2N4O).

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Synthetic Route of C21H32Cl2N4O

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

 

Gokmen, Zeliha et al. published their research in Journal of the Chemical Society of Pakistan in 2016 | CAS: 27469-60-9

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Category: piperazines

Preparation and spectral properties of novel N,S-substituted trichloronitrodienes was written by Gokmen, Zeliha;Hanay, Nur;Deniz, Nahide Gulsah. And the article was included in Journal of the Chemical Society of Pakistan in 2016.Category: piperazines This article mentions the following:

A series of piperazinyl(sulfanyl)trichloronitrodienes I [R1 = Et, cyclopentyl, 4-ClC6H4, 4-t-BuC6H4CH2; R2 = 2-tetrahydrofurylmethyl, 2-furylcarbonyl, bis(4-fluorophenyl)methyl, etc.] was synthesized via regioselective substitution of sulfide-containing nitrodienes II with piperazine derivatives The nitrodienes II were obtained by the reaction of polyhalo-3-nitrobutadiene with thiols. The structures of N,S-substituted trichloronitrodienes I were characterized by microanal., FT-IR, 1H NMR, 13C NMR and mass spectrometry. The high temperature NMR technique was used for determination of methylene protons of piperazine ring in the new compound I (R1 = 4-t-BuC6H4CH2; R2 = 2-furylcarbonyl). In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Category: piperazines).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Category: piperazines

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

 

Ukraintsev, V. B. et al. published their research in Russian Journal of General Chemistry (Translation of Zhurnal Obshchei Khimii) in 1997 | CAS: 142-64-3

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Name: Piperazine Dihydrochloride

Synthesis and transformations of the copper(II) N-(2-aminoethyl)aziridine and N-(2-haloethyl)ethylenediamine complexes was written by Ukraintsev, V. B.;Esikov, K. A.;Krasnov, B. A.;Potekhin, V. V.. And the article was included in Russian Journal of General Chemistry (Translation of Zhurnal Obshchei Khimii) in 1997.Name: Piperazine Dihydrochloride This article mentions the following:

The Cu(II) complexes with N-(2-aminoethyl)aziridine (L’) and N-(2-haloethyl)ethylenediamine (L”) with the mol. compositions [CuLX2] and [CuL2X2] (L = L’ or L”, X = Cl or Br) were synthesized. According to the IR spectra, [CuLX2] are coordination polymers consisting of tetrahedrally distorted hexacoordinated species. [CuLBr2] disproportionates in H2O to form [CuL2Br2]. Refluxing of [CuLX2] and [CuL2X2] in BuOH results in intraspheric transformation of their L ligands into piperazine. Reaction of all the obtained Cu(II) derivatives with formaldehyde initiates formation of the piperazine ring. In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Name: Piperazine Dihydrochloride).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Name: Piperazine Dihydrochloride

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

 

Ng, Yuen Lam Dora et al. published their research in Nature Communications in 2022 | CAS: 571190-30-2

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Computed Properties of C24H29N7O2

Proteomic profiling reveals CDK6 upregulation as a targetable resistance mechanism for lenalidomide in multiple myeloma was written by Ng, Yuen Lam Dora;Ramberger, Evelyn;Bohl, Stephan R.;Dolnik, Anna;Steinebach, Christian;Conrad, Theresia;Mueller, Sina;Popp, Oliver;Kull, Miriam;Haji, Mohamed;Guetschow, Michael;Doehner, Hartmut;Walther, Wolfgang;Keller, Ulrich;Bullinger, Lars;Mertins, Philipp;Kroenke, Jan. And the article was included in Nature Communications in 2022.Computed Properties of C24H29N7O2 This article mentions the following:

The immunomodulatory drugs (IMiDs) lenalidomide and pomalidomide are highly effective treatments for multiple myeloma. However, virtually all patients eventually relapse due to acquired drug resistance with resistance-causing genetic alterations being found only in a small subset of cases. To identify non-genetic mechanisms of drug resistance, we here perform integrated global quant. tandem mass tag (TMT)-based proteomic and phosphoproteomic analyses and RNA sequencing in five paired pre-treatment and relapse samples from multiple myeloma patients. These analyses reveal a CDK6-governed protein resistance signature that includes myeloma high-risk factors such as TRIP13 and RRM1. Overexpression of CDK6 in multiple myeloma cell lines reduces sensitivity to IMiDs while CDK6 inhibition by palbociclib or CDK6 degradation by proteolysis targeting chimeras (PROTACs) is highly synergistic with IMiDs in vitro and in vivo. This work identifies CDK6 upregulation as a druggable target in IMiD-resistant multiple myeloma and highlights the use of proteomic studies to uncover non-genetic resistance mechanisms in cancer. In the experiment, the researchers used many compounds, for example, 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2Computed Properties of C24H29N7O2).

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Computed Properties of C24H29N7O2

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

 

Shimizu, Masahiro et al. published their research in Scientific Reports in 2022 | CAS: 571190-30-2

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.SDS of cas: 571190-30-2

Enhanced O-GlcNAc modification induced by the RAS/MAPK/CDK1 pathway is required for SOX2 protein expression and generation of cancer stem cells was written by Shimizu, Masahiro;Shibuya, Hiroshi;Tanaka, Nobuyuki. And the article was included in Scientific Reports in 2022.SDS of cas: 571190-30-2 This article mentions the following:

Cancer stem cells (CSCs) have tumor initiation, self-renewal, and long-term tumor repopulation properties, and it is postulated that differentiated somatic cells can be reprogrammed to CSCs by oncogenic signals. We previously showed that oncogenic HRASV12 conferred tumor initiation capacity in tumor suppressor p53-deficient (p53-/-) primary mouse embryonic fibroblasts (MEFs) through transcription factor NF-κB-mediated enhancement of glucose uptake; however, the underlying mechanisms of RAS oncogene-induced CSC reprogramming have not been elucidated. Here, we found that the expression of the reprogramming factor SOX2 was induced by HRASV12 in p53-/- MEFs. Moreover, gene knockout studies revealed that SOX2 is an essential factor for the generation of CSCs by HRASV12 in mouse and human fibroblasts. We demonstrated that HRASV12-induced cyclin-dependent kinase 1 (CDK1) activity and subsequent enhancement of protein O-GlcNAcylation were required for SOX2 induction and CSC generation in these fibroblasts and cancer cell lines containing RAS mutations. Moreover, the CDK inhibitor dinaciclib and O-GlcNAcylation inhibitor OSMI1 reduced the number of CSCs derived from these cells. Taken together, our results reveal a signalling pathway and mechanism for CSC generation by oncogenic RAS and suggest the possibility that this signalling pathway is a therapeutic target for CSCs. In the experiment, the researchers used many compounds, for example, 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2SDS of cas: 571190-30-2).

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.SDS of cas: 571190-30-2

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

 

Jevtic, Ivana I. et al. published their research in Molecules in 2020 | CAS: 142-64-3

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.COA of Formula: C4H12Cl2N2

Newly synthesized fluorinated cinnamylpiperazines possessing low in vitro MAO-B binding was written by Jevtic, Ivana I.;Lai, Thu Hang;Penjisevic, Jelena Z.;Dukic-Stefanovic, Sladjana;Andric, Deana B.;Brust, Peter;Kostic-Rajacic, Sladjana V.;Teodoro, Rodrigo. And the article was included in Molecules in 2020.COA of Formula: C4H12Cl2N2 This article mentions the following:

Herein, the synthesis and pharmacol. evaluation of ten novel fluorinated cinnamylpiperazines I (R = 2-fluorophenyl, phenyl; R1 = (4-fluorophenyl)carbonyl, 2-fluoropyridin-3-yl, 6-fluoropyridin-2-yl, etc.)as potential monoamine oxidase B (MAO-B) ligands were reported. The designed derivatives I consist of either cinnamyl or 2-fluorocinnamyl moieties connected to 2-fluoropyridylpiperazines. The three-step synthesis starting from com. available tert-Bu piperazine-1-carboxylate afforded the final products I in overall yields between 9% and 29%. An in vitro competitive binding assay using l-[3H]Deprenyl as radioligand was developed and the MAO-B binding affinities of the synthesized derivatives I were assessed. Docking studies revealed that the compounds I were stabilized in both MAO-B entrance and substrate cavities, thus resembling the binding pose of l-Deprenyl. Although the results revealed that the novel fluorinated cinnamylpiperazines I do not possess sufficient MAO-B binding affinity to be eligible as positron emission tomog. (PET) agents, the herein developed binding assay and the insights gained within our docking studies will certainly pave the way for further development of MAO-B ligands. In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3COA of Formula: C4H12Cl2N2).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.COA of Formula: C4H12Cl2N2

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

 

Sano, Maria V. et al. published their research in Expert Review of Anticancer Therapy in 2022 | CAS: 1211441-98-3

7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 1211441-98-3

Ribociclib efficacy in special populations and analysis of patient-reported outcomes in the MONALEESA trials was written by Sano, Maria V.;Martorana, Federica;Lavenia, Giuseppe;Rossello, Rosalba;Prestifilippo, Angela;Sava, Serena;Ricciardi, Giuseppina R.;Vigneri, Paolo. And the article was included in Expert Review of Anticancer Therapy in 2022.Recommanded Product: 1211441-98-3 This article mentions the following:

Cyclin-dependent kinase 4/6 (CDK4/6) inhibitors abemaciclib, palbociclib, and ribociclib radically modified the treatment of hormone receptor-pos./human epidermal growth factor 2-neg. advanced breast cancer. Ribociclib efficacy was proved in the phase III MONALEESA-2, -3, and -7 trials. In the first-line setting, ribociclib plus endocrine therapy determined statistically significant improvements in progression-free (PFS) and overall survival (OS) in pre-menopausal (MONALEESA-7) and post-menopausal (MONALEESA-2) women. Likewise, ribociclib and fulvestrant induced a significant PFS and OS benefit in post-menopausal women previously treated with endocrine therapy (MONALEESA-3). Addnl., ribociclib did not affect patients health-related quality of life in all the MONALEESA trials. We reviewed the results of the available randomized phase III trials testing ribociclib and endocrine therapy in advanced breast cancer, focusing on different patient subgroups and then on health-related quality of life. The benefit of ribociclib is consistent across patient subgroups and is maintained in populations with unfavorable features, such as those with endocrine resistance or visceral metastases. Furthermore, the addition of ribociclib to endocrine therapy delays quality of life deterioration and improves pain scores. These results represent a pivotal improvement for the treatment of advanced breast cancer patients receiving CDK4/6 inhibitors. In the experiment, the researchers used many compounds, for example, 7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3Recommanded Product: 1211441-98-3).

7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (cas: 1211441-98-3) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 1211441-98-3

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

 

Wang, Yixia et al. published their research in European Food Research and Technology in 2022 | CAS: 113617-63-3

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.COA of Formula: C19H20F3N3O3

Determination of 12 quinolones in honey by vortex-assisted dispersive liquid liquid microextraction performed in syringe based on deep eutectic solvent combine with ultra performance liquid chromatography-mass spectrometry was written by Wang, Yixia;Zhao, Sijun;Yang, Linyan;Liu, Chang;Wang, Hongyu;Li, Daowen;Zhang, Wei;Li, Liuan;Song, Cuiping;Li, Cun. And the article was included in European Food Research and Technology in 2022.COA of Formula: C19H20F3N3O3 This article mentions the following:

A novel vortex-assisted dispersive liquid-liquid microextraction method based on deep eutectic solvent (VA-DLLME-DES) completed in syringe has been established to extract 12 quinolones from honey. This method is an improvement of traditional DLLME. In this work, the green DES prepared with heptanoic acid and thymol was used for extractant rather than traditional organic extraction solvent. Without centrifugation, the phases were separated in the way of removing aqueous phase by pushing the syringe and extractant phase was collected for ultra performance liquid chromatog.-mass spectrometry (UPLC-MS) anal. The stability of DES and some exptl. parameters (type, molar ratios and volume of extraction solvent, type and volume of dispersant, vortex time and effect of pH and NaCl) were evaluated. In the range of 2-100 ng/mL, the proposed method showed good linearities (r2 ranged from 0.996 to 0.999). The extraction recoveries were obtained in the range of 75.01%-117.05% and relative standard deviations were less than 13.83% for inter- (n = 6) and intra-day (n = 3) precisions. The limits of detection and quantification were 3 ng g-1 and 10 ng g-1, resp. The developed method with the advantages of simple operation, short extraction time and less consumption organic solvent provides a tech. idea for green, simple and time-saving sample preparation methods. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3COA of Formula: C19H20F3N3O3).

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.COA of Formula: C19H20F3N3O3

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

 

Bidard, Francois-Clement et al. published their research in Lancet Oncology in 2022 | CAS: 571190-30-2

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Recommanded Product: 571190-30-2

Switch to fulvestrant and palbociclib versus no switch in advanced breast cancer with rising ESR1 mutation during aromatase inhibitor and palbociclib therapy (PADA-1): a randomised, open-label, multicentre, phase 3 trial was written by Bidard, Francois-Clement;Hardy-Bessard, Anne-Claire;Dalenc, Florence;Bachelot, Thomas;Pierga, Jean-Yves;de la Motte Rouge, Thibault;Sabatier, Renaud;Dubot, Coraline;Frenel, Jean-Sebastien;Ferrero, Jean Marc;Ladoire, Sylvain;Levy, Christelle;Mouret-Reynier, Marie-Ange;Lortholary, Alain;Grenier, Julien;Chakiba, Camille;Stefani, Laetitia;Plaza, Jerome Edouard;Clatot, Florian;Teixeira, Luis;D′Hondt, Veronique;Vegas, Helene;Derbel, Olfa;Garnier-Tixidre, Claire;Canon, Jean-Luc;Pistilli, Barbara;Andre, Fabrice;Arnould, Laurent;Pradines, Anne;Bieche, Ivan;Callens, Celine;Lemonnier, Jerome;Berger, Frederique;Delaloge, Suzette. And the article was included in Lancet Oncology in 2022.Recommanded Product: 571190-30-2 This article mentions the following:

In advanced estrogen receptor-pos., HER2-neg. breast cancer, acquired resistance to aromatase inhibitors frequently stems from ESR1-mutated subclones, which might be sensitive to fulvestrant. The PADA-1 trial aimed to show the efficacy of an early change in therapy on the basis of a rising ESR1 mutation in blood (bESR1mut), while assessing the global safety of combination fulvestrant and palbociclib. We did a randomised, open-label, phase 3 trial in 83 hospitals in France. Women aged at least 18 years with estrogen receptor-pos., HER2-neg. advanced breast cancer and an Eastern Cooperative Oncol. Group performance status of 0-2 were recruited and monitored for rising bESR1mut during first-line aromatase inhibitor (2·5 mg letrozole, 1 mg anastrozole, or 25 mg exemestane, orally once per day, taken continuously) and palbociclib (125 mg orally once per day on days 1-21 of a 28-day cycle) therapy. Patients with newly present or increased bESR1mut in circulating tumor DNA and no synchronous disease progression were randomly assigned (1:1) to continue with the same therapy or to switch to fulvestrant (500 mg i.m. on day 1 of each 28-day cycle and on day 15 of cycle 1) and palbociclib (dosing unchanged). The randomisation sequence was generated within an interactive web response system using a minimisation method (with an 80% random factor); patients were stratified according to visceral involvement (present or absent) and the time from inclusion to bESR1mut detection (<12 mo or ≥12 mo). The co-primary endpoints were investigator-assessed progression-free survival from random assignment, analyzed in the intention-to-treat population (ie, all randomly assigned patients), and grade 3 or worse haematol. adverse events in all patients. The trial is registered with Clinicaltrials.gov (NCT03079011), and is now complete. From March 22, 2017, to Jan 31, 2019, 1017 patients were included, of whom 279 (27%) developed a rising bESR1mut and 172 (17%) were randomly assigned to treatment: 88 to switching to fulvestrant and palbociclib and 84 patients to continuing aromatase inhibitor and palbociclib. At database lock on July 31, 2021, randomly assigned patients had a median follow-up of 35·3 mo (IQR 29·2-41·4) from inclusion and 26·0 mo (13·8-34·3) from random assignment. Median progression-free survival from random assignment was 11·9 mo (95% CI 9·1-13·6) in the fulvestrant and palbociclib group vs. 5·7 mo (3·9-7·5) in the aromatase inhibitor and palbociclib group (stratified HR 0·61, 0·43-0·86; p=0·0040). The most frequent grade 3 or worse haematol. adverse events were neutropenia (715 [70·3%] of 1017 patients), lymphopenia (66 [6·5%]), and thrombocytopenia (20 [2·0%]). The most common grade 3 or worse adverse events in step 2 were neutropenia (35 [41·7%] of 84 patients in the aromatase inhibitor and palbociclib group vs 39 [44·3%] of 88 patients in the fulvestrant and palbociclib group) and lymphopenia (three [3·6%] vs four [4·5%]). 31 (3·1%) patients had grade 3 or worse serious adverse events related to treatment in the overall population. Three (1·7%) of 172 patients randomly assigned had one serious adverse event in step 2: one (1·2%) grade 4 neutropenia and one (1·2%) grade 3 fatigue among 84 patients in the aromatase inhibitor and palbociclib group, and one (1·1%) grade 4 neutropenia among 88 patients in the fulvestrant and palbociclib group. One death by pulmonary embolism in step 1 was declared as being treatment related. PADA-1 is the first prospective randomised trial showing that the early therapeutic targeting of bESR1mut results in significant clin. benefit. Addnl., the original design explored in PADA-1 might help with tackling acquired resistance with new drugs in future trials.Pfizer. In the experiment, the researchers used many compounds, for example, 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2Recommanded Product: 571190-30-2).

6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one (cas: 571190-30-2) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Recommanded Product: 571190-30-2

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

 

Ju, Chun-Rong et al. published their research in Transplant International in 2022 | CAS: 62893-19-0

(6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Computed Properties of C25H27N9O8S2

Metagenomic next-generation sequencing for diagnosing infections in lung transplant recipients: a retrospective study was written by Ju, Chun-Rong;Lian, Qiao-Yan;Guan, Wei-Jie;Chen, Ao;Zhang, Jian-Heng;Xu, Xin;Chen, Rong-Chang;Li, Shi-Yue;He, Jian-Xing. And the article was included in Transplant International in 2022.Computed Properties of C25H27N9O8S2 This article mentions the following:

Accurate identification of pathogens is essential for the diagnosis and control of infections. We aimed to compare the diagnostic performance of metagenomic next-generation sequencing (mNGS) and conventional detection methods (CDM) in lung transplant recipients (LTRs). We retrospectively analyzed 107 LTRs with suspected infection of pulmonary, blood, central nervous system or chest wall between March 2018 and Nov. 2020. Bronchoalveolar lavage fluid and other body fluids were subject to pathogen detection by both mNGS and CDM. Of the 163 specimens, 84 (51.5%) tested pos. for both mNGS and culture, 19 (11.7%) of which were completely consistent, 44 (27.0%) were partially congruent, and 21 (12.9%) were discordant (kappa = .215; p = .001). Compared with CDM, mNGS detected a higher diversity of pathogens. Moreover, the turn-around time was significantly shorter for mNGS compared with culture (2.7 ± .4 vs. 5.5 ± 1.6 days, p < .001). As an auxiliary method, treatment strategies were adjusted according to mNGS findings in 31 cases (29.0%), including eight patients with non-infectious diseases, who were finally cured. MNGS can identify pathogens with a shorter turn-around time and therefore provide a more accurate and timely diagnostic information to ascertaining pulmonary infections. mNGS might have a role in differentiating infectious from non-infectious lung diseases in LTRs. In the experiment, the researchers used many compounds, for example, (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0Computed Properties of C25H27N9O8S2).

(6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Computed Properties of C25H27N9O8S2

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