Month: February 2023

[Cariprazine for acute and maintenance treatment of schizophrenia]. was written by Spoelstra, S K;Visser, L;Knegtering, H. And the article was included in Tijdschrift voor psychiatrie in 2019.Reference of 839712-12-8 This article mentions the following:

BACKGROUND: Since 2018, cariprazine has been available for the treatment of schizophrenia on the Dutch and Belgian markets.<br/> AIM: To give an overview of the indications, effectiveness and side effects of cariprazine. To make an inventory of the advantages and disadvantages of this new antipsychotic drug.<br/> METHOD: A clinically oriented literature review of published clinical studies and pharmacodynamic and -kinetic publications.<br/> RESULTS: Cariprazine is unique because of its preferential D3 receptor partial agonist affinity and has, in theory, a beneficial effect on negative symptoms. The antipsychotic has two active metabolites: desmethylcariprazine and didesmethylcariprazine. The long half-life of cariprazine indicates that, in theory, the drug should not be given daily. Cariprazine is metabolized by cyp3a4 and to a lesser extent by cyp2d6 enzymes. Extrapyramidal symptoms and akathisia are relatively frequent side effects. In contrast, metabolic side effects and weight gain have been reported rarely.<br/> CONCLUSION: Cariprazine can be an effective treatment option for schizophrenia. The final positioning of this antipsychotic drug will have to be based on future research. 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: 839712-12-8Reference of 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. 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).Reference of 839712-12-8

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

A simple and efficient synthesis of calcium channel blocker flunarizine was written by Narsaiah, A. Venkat;Kumar, J. Kranthi. And the article was included in Organic Chemistry: An Indian Journal in 2011.Quality Control of 4,4-Difluorobenzhydrylpiperazine This article mentions the following:

T-type calcium channel blocker and anti-ischemic drug 1-[bis(4-fluorophenyl)methyl]-4-cinnamylpiperazine synthesis was carried out in four steps with an average of 70% yield. This route is very convenient and can be applied for large scale preparation of Flunarizine with high yields. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Quality Control of 4,4-Difluorobenzhydrylpiperazine).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.Quality Control of 4,4-Difluorobenzhydrylpiperazine

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

Phenotypic Screening Combined with Machine Learning for Efficient Identification of Breast Cancer-Selective Therapeutic Targets was written by Gautam, Prson;Jaiswal, Alok;Aittokallio, Tero;Al-Ali, Hassan;Wennerberg, Krister. And the article was included in Cell Chemical Biology in 2019.Name: rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide This article mentions the following:

The lack of functional understanding of most mutations in cancer, combined with the non-druggability of most proteins, challenge genomics-based identification of oncol. drug targets. We implemented a machine-learning-based approach (idTRAX), which relates cell-based screening of small-mol. compounds to their kinase inhibition data, to directly identify effective and readily druggable targets. We applied idTRAX to triple-neg. breast cancer cell lines and efficiently identified cancer-selective targets. For example, we found that inhibiting AKT selectively kills MFM-223 and CAL148 cells, while inhibiting FGFR2 only kills MFM-223. Since the effects of catalytically inhibiting a protein can diverge from those of reducing its levels, targets identified by idTRAX frequently differ from those identified through gene knockout/knockdown methods. This is critical if the purpose is to identify targets specifically for small-mol. drug development, whereby idTRAX may produce fewer false-positives. The rapid nature of the approach suggests that it may be applicable in personalizing therapy. In the experiment, the researchers used many compounds, for example, rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3Name: rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide).

rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Name: rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide

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

Conjugated push-pull salts derived from linear benzobisthiazole: preparation and optical properties was written by Cibova, Alexandra;Magdolen, Peter;Fueloepova, Andrea;Zahradnik, Pavol. And the article was included in Chemical Papers in 2013.SDS of cas: 27913-99-1 This article mentions the following:

A series of novel monomethylated salts derived from linear benzobisthiazole was prepared The push-pull attributes of these new compounds are represented by a quaternized azolium cycle as the acceptor part at one end of the structure and the dialkylamino- or diarylamino-substituted benzene ring as the donor part at the opposite end. Both moieties are connected by a conjugated linker consisting of one or two double bonds. Such dipolar structures are promising candidates for non-linear optical materials. The quantum-chem. indexes describing linear and non-linear optical properties were obtained from semi-empirical calculations The relationships between the chem. structure and non-linear optical properties of the cations studied were obtained. Effective conjugation was confirmed by measuring the optical properties in the UV-VIS region. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1SDS of cas: 27913-99-1).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.SDS of cas: 27913-99-1

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

Ribociclib inhibits P-gp-mediated multidrug resistance in human epidermoid carcinoma cells was written by Zhang, Lei;Ye, Biwei;Lin, Yunfeng;Li, Yi-Dong;Wang, Jing-Quan;Chen, Zhuo;Ping, Feng-Feng;Chen, Zhe-Sheng. And the article was included in Frontiers in Pharmacology in 2022.Synthetic Route of C23H30N8O This article mentions the following:

The efficacy of cancer chemotherapy can be attenuated or abrogated by multidrug resistance (MDR) in cancer cells. In this study, we determined the effect of the CDK4/6 inhibitor, ribociclib (or LEE011), on P-glycoprotein (P-gp)-mediated MDR in the human epidermoid carcinoma MDR cell line, KB-C2, which is widely used for studying P-gpmediated MDR in cancers. The incubation of KB-C2 cells with ribociclib (3-9μM) increased the efficacy of colchicine, a substrate for P-gp. The cell expression of P-gp was downregulated at both translation and transcription levels. Furthermore, ribociclib produced a 3.5-fold increase in the basal activity of P-gp ATPase, and the concentration required to increase basal activity by 50% (EC₅₀) was 0.04μM. Docking studies indicated that ribociclib interacted with the drug-substrate binding site of P-gp. The short-term and long-term intracellular accumulation of doxorubicin greatly increased in the KB-C2 cells cocultured with ribociclib, indicating ribociclib inhibited the drug efflux activity of P-gp. The results of our study indicate that LEE011 may be a potential agent for combined therapy of the cancers with P-gp mediated MDR. 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: 1211441-98-3Synthetic Route of C23H30N8O).

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. Simple N-substituted piperazines have been found in many drug molecules. 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.Synthetic Route of C23H30N8O

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

Comparative efficacy and tolerability of pharmacological treatments for the treatment of acute bipolar depression: A systematic review and network meta-analysis was written by Bahji, Anees;Ermacora, Dylan;Stephenson, Callum;Hawken, Emily R.;Vazquez, Gustavo. And the article was included in Journal of Affective Disorders in 2020.Category: piperazines This article mentions the following:

We investigated the comparative efficacy and tolerability of pharmacol. treatment strategies for the treatment of acute bipolar depression. A systematic review and network meta-anal. was conducted by searching eight registries for published and unpublished, double-blind, randomized controlled trials of pharmacotherapies for the acute treatment of bipolar depression. PRISMA guidelines were used for abstracting data, while the Cochrane Risk of Bias Tool was used to assess data quality. Data extraction was done independently by two reviewers, with discrepancies resolved by consensus. Data were pooled using a random-effects model. Primary outcomes were efficacy (response and remission rate) and acceptability (completion of treatment and dropouts due to adverse events). Summary odds ratios (ORs) were estimated using pairwise and network meta-anal. with random effects. Identified citations (4,404) included 50 trials comprising 11,448 participants. Escitalopram, phenelzine, moclobemide, carbamazepine, sertraline, lithium, paroxetine, aripiprazole, gabapentin and ziprasidone appear to be ineffective as compared to placebo in treatment of bipolar depression. Divalproex, olanzapine/fluoxetine, olanzapine, quetiapine, cariprazine, and lamotrigine, appear to be effective as compared to placebo in treatment of bipolar depression according to the network meta-anal. Aripiprazole showed higher discontinuation rates vs. placebo due to the appearance of any adverse event. Quetiapine was better than placebo at reducing treatment-emergent affective switches. For Bipolar I Disorder, cariprazine, fluoxetine, imipramine, lamotrigine, lurasidone, olanzapine-fluoxetine, and olanzapine were significantly better than placebo at response, while fluoxetine, imipramine, cariprazine, lurasidone, olanzapine-fluoxetine, and olanzapine were significantly better than placebo at remission. These results could serve evidence-based practice and inform patients, physicians, guideline developers, and policymakers on the relative benefits of the different antidepressants, antipsychotics, and mood-stabilizing agents for the treatment of bipolar depression.PROSPERO (CRD42019122172). 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: 839712-12-8Category: piperazines).

3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea (cas: 839712-12-8) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Category: piperazines

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

Neural induction with a dopaminergic phenotype from human pluripotent stem cells through a feeder-free floating aggregation culture was written by Morizane, Asuka;Doi, Daisuke;Takahashi, Jun. And the article was included in Methods in Molecular Biology (New York, NY, United States) in 2013.Application of 1062368-24-4 This article mentions the following:

Pluripotent stem cells are promising potential sources for cell replacement therapy and are useful research tools for exploring disease mechanisms. Neural cells are one of the cell types that have been most efficiently differentiated through several established protocols. This chapter describes the feeder-free floating aggregation culture system for the induction of dopaminergic neurons. This method is simple and highly efficient for the production of dopaminergic neurons. It has several advantages for application in clin. usage in comparison to the other protocols using either feeder cells or Matrigel. In the experiment, the researchers used many compounds, for example, 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4Application of 1062368-24-4).

4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline (cas: 1062368-24-4) 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. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application of 1062368-24-4

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

Clinical and analytical validation of FoundationOneCDx, a comprehensive genomic profiling assay for solid tumors was written by Milbury, Coren A.;Creeden, James;Yip, Wai-Ki;Smith, David L.;Pattani, Varun;Maxwell, Kristi;Sawchyn, Bethany;Gjoerup, Ole;Meng, Wei;Skoletsky, Joel;Concepcion, Alvin D.;Tang, Yanhua;Bai, Xiaobo;Dewal, Ninad;Ma, Pei;Bailey, Shannon T.;Thornton, James;Pavlick, Dean C.;Frampton, Garrett M.;Lieber, Daniel;White, Jared;Burns, Christine;Vietz, Christine. And the article was included in PLoS One in 2022.Category: piperazines This article mentions the following:

FoundationOneCDx (F1CDx) is a United States (US) Food and Drug Administration (FDA)-approved companion diagnostic test to identify patients who may benefit from treatment in accordance with the approved therapeutic product labeling for 28 drug therapies. F1CDx utilizes next-generation sequencing (NGS)-based comprehensive genomic profiling (CGP) technol. to examine 324 cancer genes in solid tumors. F1CDx reports known and likely pathogenic short variants (SVs), copy number alterations (CNAs), and select rearrangements, as well as complex biomarkers including tumor mutational burden (TMB) and microsatellite instability (MSI), in addition to genomic loss of heterozygosity (gLOH) in ovarian cancer. CGP services can reduce the complexity of biomarker testing, enabling precision medicine to improve treatment decision-making and outcomes for cancer patients, but only if test results are reliable, accurate, and validated clin. and anal. to the highest standard available. The analyses presented herein demonstrate the extensive anal. and clin. validation supporting the F1CDx initial and subsequent FDA approvals to ensure high sensitivity, specificity, and reliability of the data reported. The anal. validation included several in-depth evaluations of F1CDx assay performance including limit of detection (LoD), limit of blank (LoB), precision, and orthogonal concordance for SVs (including base substitutions [SUBs] and insertions/deletions [INDELs]), CNAs (including amplifications and homozygous deletions), genomic rearrangements, and select complex biomarkers. The assay validation of >30,000 test results comprises a considerable and increasing body of evidence that supports the clin. utility of F1CDx to match patients with solid tumors to targeted therapies or immunotherapies based on their tumor’s genomic alterations and biomarkers. F1CDx meets the clin. needs of providers and patients to receive guideline-based biomarker testing, helping them keep pace with a rapidly evolving field of medicine. In the experiment, the researchers used many compounds, for example, 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7Category: piperazines).

3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7) 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 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

Behavior of 4-(-2-hydroxyethyl)-1-piperazineethanesulphonic acid under electrospray ionization mass spectrometry conditions was written by Saraiva, Marco A.;Borges, Carlos M.;Florencio, M. Helena. And the article was included in European Journal of Mass Spectrometry in 2010.Related Products of 75277-39-3 This article mentions the following:

The authors’ previous experiments on electrospray ionization mass spectrometry (ESI-MS) anal. of reaction mixtures containing 4-(-2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES, zwitterionic organic buffering agent), a commonly used buffer, indicated that HEPES species did not significantly suppress analyte species, even in reaction mixture solutions with significant amounts of HEPES. With the purpose of investigating the behavior of HEPES under ESI-MS conditions, HEPES aqueous solutions and HEPES aqueous solutions containing analyte with high polarity properties and low polarity properties and with different acid/base chem., were therefore investigated. For electrosprayed aqueous solutions of HEPES with concentrations above 10^-5M, an enhanced formation of HEPES multimer ions, showing HEPES monomer ion formation, was observed This enhanced formation of HEPES multimer ions is much higher than those observed for other polar compounds, such as acetyl-arginine, acetyl-lysine and histidine. Information from solution behavior such as HEPES concentration, solution pH and instrumental factors, namely the capillary temperature, was related to information from mass spectra. The results obtained led us to conclude that the formation of HEPES ions is related to the initial solution composition The influence of analyte species on HEPES species formation, for electrosprayed HEPES solutions with analyte, was also investigated. The variations observed for HEPES monomer and multimer ion abundance, which were found to be consistent with those observed for analyte monomer ion abundance, were related to the type of analyte, i.e. to their acid/base nature. Strikingly, the variations observed between HEPES monomer and multimer ion abundance enable the discrimination of different influences of analyte species on HEPES species formation. The results obtained also provided an explanation for the observation that HEPES species do not significantly suppress analyte species ion signals when highly-concentrated HEPES solutions with analyte are electrosprayed. According to our results, the associated behavior between HEPES species seems to be preserved in the gas phase during electrospray ionization. This observation may provide some information that may be useful regarding the behavior involved in the gas-phase ion formation process from charged droplets during electrospray ionization or, at least, to differentiate between behaviors. In the experiment, the researchers used many compounds, for example, Sodium 2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate (cas: 75277-39-3Related Products of 75277-39-3).

Sodium 2-(4-(2-hydroxyethyl)piperazin-1-yl)ethanesulfonate (cas: 75277-39-3) 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 an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Related Products of 75277-39-3

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

Microwave-assisted synthesis of new 2-substituted phenyl-5-{N⁴-[bi-(4-fluoro phenyl)-methyl]-N¹-methylene} piperazine-1,3,4-oxadiazoles was written by Zhang, Zhen;Mo, Song;Zhang, Gang;Shao, Xue-bei;Li, Qing-han;Yang, Xue-jun;Chen, Feng. And the article was included in Xinan Minzu Daxue Xuebao, Ziran Kexueban in 2017.Application In Synthesis of 4,4-Difluorobenzhydrylpiperazine This article mentions the following:

Objective: Eight new 2-substituted phenyl-5-{N⁴-[bi-(4-fluorophenyl)-methyl]-N¹-methylene} piperazine-1,3,4-oxadiazoles 4a-4h were prepared starting from [bi-(4-fluorophenyl)-methyl]-piperazine under microwave irradiation with good yields. The technique of microwave irradiation proved to be an efficient, safe and environment-friendly technique with significant decreases in reaction time, comparably moderate yields, and easy manipulation. Furthermore, this method can be applied to the synthesis of many other oxadiazoles with more potential functional qualities. The structures of the eight compounds were determined by IR, MS and 1H NMR data. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9Application In Synthesis of 4,4-Difluorobenzhydrylpiperazine).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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).Application In Synthesis of 4,4-Difluorobenzhydrylpiperazine

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