Category: piperazines

Synthesis of new hexahydropyrimido[1,2-a]azepine derivatives bearing functionalized aryl and heterocyclic moieties as anti-inflammatory agents was written by Hassanein, Hassanein H.;Abdel Rahman, Doaa E.;Fouad, Marwa A.;Ahmed, Rehab F.. And the article was included in Future Medicinal Chemistry in 2021.HPLC of Formula: 27913-99-1 This article mentions the following:

New hexahydropyrimido[1,2-a]azepine derivatives bearing functionalized aryl and heterocyclic moieties were synthesized as anti-inflammatory agents with better safety profiles. All synthesized compounds were assessed in vitro for their COX-1 and COX-2 inhibition activities. The most selective compounds, 2f, 5 and 6, were further evaluated for their in vivo anti-inflammatory activity and PGE2 inhibitory activity. To rationalize their selectivity, mol. docking within COX-1 and COX-2 binding sites was performed. Their physicochem. properties and drug-like nature profile were also calculated The good activity and selectivity of compounds 2f, 5 and 6 were rationalized using a mol. docking study and supported by in vivo studies. These promising findings are encouraging for performing future investigations of these derivatives In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1HPLC of Formula: 27913-99-1).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.HPLC of Formula: 27913-99-1

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

miR-217-5p regulates myogenesis in skeletal muscle stem cells by targeting FGFR2 was written by Zhu, Menghai;Chen, Gang;Yang, Yi;Yang, Jiantao;Qin, Bengang;Gu, Liqiang. And the article was included in Molecular Medicine Reports in 2020.Quality Control of rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide This article mentions the following:

MicroRNA-217-5p (miR-217-5p) has been implicated in cell proliferation; however, its role in skeletal muscle stem cells (SkMSCs) remains unknown. The present study aimed to explore the roles of miR-217-5p in the biol. characteristics of SkMSCs. SkMSCs were identified by cell surface markers using flow cytometry. The present study observed that miR-217-5p mimics accelerated the proliferation and suppressed the differentiation in SkMSCs. In addition, the results of the present study revealed that fibroblast growth factor receptor 2 (FGFR2) was a target of miR-217-5p, as miR-217-5p bound directly to the 3′-untranslated region of FGFR2 mRNA, resulting in increased FGFR2 mRNA and protein levels. In addition, the present study suppressed the expression of FGFR2 in SkMSCs using a selective FGFR inhibitor AZD4547 and detected the efficiency of inhibition by reverse transcription-quant. PCR and western blotting. miR-217-5p levels were pos. associated with FGFR2 expression, which was upregulated and accelerated the proliferation of SkMSCs compared with that of the miR-NC group. MiR-217-5p levels were pos. associated with FGFR2 expression, which was upregulated and accelerated the proliferation of SkMSCs compared with that of the miR-NC group. Collectively, these results demonstrated that miR-217-5p may act as a myogenesis promoter in SkMSCs by directly targeting FGFR2 and may regulate the myogenesis of these cells. 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: 1035270-39-3Quality Control of 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. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.Quality Control of 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

Synthesis, biological evaluation and structure-activity correlation study of a series of imidazol-based compounds as Candida albicans inhibitors was written by Moraca, Francesca;De Vita, Daniela;Pandolfi, Fabiana;Di Santo, Roberto;Costi, Roberta;Cirilli, Roberto;D’Auria, Felicia Diodata;Panella, Simona;Palamara, Anna Teresa;Simonetti, Giovanna;Botta, Maurizio;Scipione, Luigi. And the article was included in European Journal of Medicinal Chemistry in 2014.Recommanded Product: 87394-48-7 This article mentions the following:

A new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives was synthesized. The antifungal activity was evaluated in vitro against different fungal species. The biol. results show that the most active compounds possess an antifungal activity comparable or higher than Fluconazole against Candida albicans, non-albicans Candida species, Cryptococcus neoformans and dermathophytes. Because of their racemic nature, the most active compounds I and II were tested as pure enantiomers. For II the (R)-enantiomer resulted more active than the (S)-one, otherwise for 5f the (S)-enantiomer resulted the most active. To rationalize the exptl. data, a ligand-based computational study was carried out; the results of the modeling study show that (S)-I and (R)-II perfectly align to the ligand-based model, showing the same relative configuration. Preliminary studies on the human lung adenocarcinoma epithelial cells (A549) have shown that II, III and I possess a low cytotoxicity. In the experiment, the researchers used many compounds, for example, 1-(3-Nitropyridin-2-yl)piperazine (cas: 87394-48-7Recommanded Product: 87394-48-7).

1-(3-Nitropyridin-2-yl)piperazine (cas: 87394-48-7) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Recommanded Product: 87394-48-7

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

Reduction of bitterness of antihistaminic drugs by complexation with β-cyclodextrins was written by Ono, Nao;Miyamoto, Yuji;Ishiguro, Takako;Motoyama, Keiichi;Hirayama, Fumitoshi;Iohara, Daisuke;Seo, Hakaru;Tsuruta, Satoshi;Arima, Hidetoshi;Uekama, Kaneto. And the article was included in Journal of Pharmaceutical Sciences in 2011.Synthetic Route of C21H29Cl3N2O2 This article mentions the following:

Reduction of bitterness of antihistaminic drugs by cyclodextrin (CyD) complexation was examined The stability constant (Kc) of the 1:1 CyD inclusion complexes with antihistaminic drugs increased in the order of 2-hydroxypropyl-β-CyD (HP-β-CyD) ≈ β-CyD > γ-CyD > α-CyD for diphenhydramine and epinastine, and HP-β-CyD ≈ β-CyD > α-CyD > γ-CyD for hydroxyzine, cetirizine, and dl-chlorpheniramine. The inclusion complexes inhibited the adsorption of antihistaminic drugs to lipid membrane using liposomes, as the magnitude of Kc increased. From human gustatory sensation tests, β-CyD and HP-β-CyD potently suppressed the bitterness of antihistaminic drugs in a dose-dependent manner. Further, an artificial taste sensor anal. revealed that β-CyD and HP-β-CyD inhibited the bitterness of antihistaminic drugs in solution The results suggest that CyDs suppress the bitterness of antihistaminic drugs in solutions through the formation of inclusion complexes. These results may provide useful information for masking or elimination of bitterness of drugs using CyDs. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:1935-1943, 2011. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Synthetic Route of C21H29Cl3N2O2).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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.Synthetic Route of C21H29Cl3N2O2

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

Nalfurafine hydrochloride enabled to reduce dosage or discontinue conventional treatment for uremic pruritus was written by Yoshizawa, Taku;Kumagai, Junko;Takahashi, Naoko;Tsuchiya, Shinichiro. And the article was included in Jin to Toseki in 2013.Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride This article mentions the following:

In this paper, nalfurafine hydrochloride enabled to reduce dosage or discontinue conventional treatment for uremic pruritus was reported. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Application In Synthesis of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride

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

Research progress of 70 kDa ribosomal protein S6 kinase (P70S6K) inhibitors as effective therapeutic tools for obesity, type II diabetes and cancer was written by Zhang, Na;Ma, Shutao. And the article was included in Current Medicinal Chemistry in 2020.Reference of 1255517-76-0 This article mentions the following:

At present, diseases such as obesity, type II diabetes and cancer have brought serious health problems, which are closely related to mTOR pathway. 70 kDa ribosomal protein S6 kinase (p70S6K), as a significant downstream effector of mTOR, mediates protein synthesis, RNA processing, glucose homeostasis, cell growth and apoptosis. Inhibiting the function of p70S6K can reduce the risk of obesity which helps to treat dyslipidemia, enhance insulin sensitivity, and extend the life span of mammals. Therefore, p70S6K has become a potential target for the treatment of these diseases. So far, except for the first p70S6K specific inhibitor PF-4708671 developed by Pfizer and LY2584702 developed by Lilai, all of them are in preclin. research. This paper briefly introduces the general situation of p70S6K and reviews their inhibitors in recent years, which are mainly classified into two categories: natural compounds and synthetic compounds In particular, their inhibitory activities, structure-activity relationships (SARs) and mechanisms are highlighted. In the experiment, the researchers used many compounds, for example, 2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-6-(trifluoromethyl)-1H-benzo[d]imidazole (cas: 1255517-76-0Reference of 1255517-76-0).

2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-6-(trifluoromethyl)-1H-benzo[d]imidazole (cas: 1255517-76-0) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.Reference of 1255517-76-0

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

Synthesis of the third comonomer of Kevlar 1414, p,p’-diaminophenylpiperazine was written by Hong, Youji;Xiao, Ruojian;Ye, Xiuzhen. And the article was included in Huadong Fangzhi Gongxueyuan Xuebao in 1985.Name: 4,4′-(Piperazine-1,4-diyl)dianiline This article mentions the following:

Piperazine  [110-85-0] was treated with p-ClC₆H₄NO₂  [100-00-5] in N-methylpyrolidone in the presence of CaH₂ to give 1,4-bis(p-nitrophenyl)piperazine (I) [16264-05-4] with productivity <82.3%, compared with 57.9% without CaH₂. I was refluxed with SnCl₂, 95% EtOH, and concentrated HCl for 2 h to give 1,4-bis(p-aminophenyl)piperazine  [7479-12-1] in 80.6% yield. In the experiment, the researchers used many compounds, for example, 4,4′-(Piperazine-1,4-diyl)dianiline (cas: 7479-12-1Name: 4,4′-(Piperazine-1,4-diyl)dianiline).

4,4′-(Piperazine-1,4-diyl)dianiline (cas: 7479-12-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. 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.Name: 4,4′-(Piperazine-1,4-diyl)dianiline

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

HMG-CoA Reductase Inhibitor Statins Activate the Transcriptional Activity of p53 by Regulating the Expression of TAZ was written by Miyajima, Chiharu;Hayakawa, Yurika;Inoue, Yasumichi;Nagasaka, Mai;Hayashi, Hidetoshi. And the article was included in Pharmaceuticals in 2022.HPLC of Formula: 548472-68-0 This article mentions the following:

Transcriptional coactivator with PDZ-binding motif (TAZ) is a downstream transcriptional regulator of the Hippo pathway that controls cell growth and differentiation. The aberrant activation of TAZ correlates with a poor prognosis in human cancers, such as breast and colon cancers. We previously demonstrated that TAZ inhibited the tumor suppressor functions of p53 and enhanced cell proliferation. Statins, which are used to treat dyslipidemia, have been reported to suppress the activity of TAZ and exert anti-tumor effects. In the present study, we focused on the regulation of p53 functions by TAZ and investigated whether statins modulate these functions via TAZ. The results obtained suggest that statins, such as simvastatin and fluvastatin, activated the transcriptional function of p53 by suppressing TAZ protein expression. Furthermore, co-treatment with simvastatin and anti-tumor agents that cooperatively activate p53 suppressed cancer cell survival. These results indicate a useful mechanism by which statins enhance the effects of anti-tumor agents through the activation of p53 and may represent a novel approach to cancer therapy. In the experiment, the researchers used many compounds, for example, 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0HPLC of Formula: 548472-68-0).

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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.HPLC of Formula: 548472-68-0

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

Revealing the Unbinding Kinetics and Mechanism of Type I and Type II Protein Kinase Inhibitors by Local-Scaled Molecular Dynamics Simulations was written by Du, Yu;Wang, Renxiao. And the article was included in Journal of Chemical Theory and Computation in 2020.COA of Formula: C26H33N5O3 This article mentions the following:

Protein kinase inhibitors disrupt phosphorylation of the target kinases, which are an important class of drug for treating cancer and other diseases. Conventional structure-based design methods (such as mol. docking) focus on the static binding mode of the kinase inhibitor with its target. However, dissociation kinetic properties of a drug mol. are found to correlate with its residence time in vivo and thus have drawn the attention of drug designers in recent years. In this study, we have applied the local-scaled mol. dynamics (MD) simulation enabled in GROMACS software to explore the unbinding mechanism of a total of 41 type I and type II kinase inhibitors. Our simulation considered multiple starting configurations as well as possible protonation states of kinase inhibitors. Based on our local-scaled MD results, we discovered that the integrals of the favorable binding energy during dissociation correlated well (R² = 0.64) with the exptl. dissociation rate constants of those kinase inhibitors on the entire data set. Given its accuracy and tech. advantage, this method may serve as a practical option for estimating this important property in reality. Our simulation also provided a reasonable explanation of the dynamic properties of kinase and its inhibitor as well as the role of relevant water mols. in dissociation 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: 1035270-39-3COA of Formula: C26H33N5O3).

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 is a fairly basic compound and is an amine solvent. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.COA of Formula: C26H33N5O3

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

Combination of miR-143 and miR-506 reduces lung and pancreatic cancer cell growth through the downregulation of cyclin-dependent kinases was written by Hossian, A. k. m. nawshad;Mackenzie, Gerardo g.;Mattheolabakis, George. And the article was included in Oncology Reports in 2021.Reference of 1211441-98-3 This article mentions the following:

Lung cancer (LC) and pancreatic cancer (PC) are the first and fourth leading causes of cancer-related deaths in the US. Deregulated cell cycle progression is the cornerstone for rapid cell proliferation, tumor development, and progression. Here, we provide evidence that a novel combinatorial miR treatment inhibits cell cycle progression at two phase transitions, through their activity on the CDK4 and CDK1 genes. Following transfection with miR-143 and miR-506, we analyzed the differential gene expression of CDK4 and CDK1, using qPCR or western blot anal., and evaluated cell cycle inhibition, apoptosis and cytotoxicity. The combinatorial miR-143/506 treatment downregulated CDK4 and CDK1 levels, and induced apoptosis in LC cells, while sparing normal lung fibroblasts. Moreover, the combinatorial miR treatment demonstrated a comparable activity to clin. tested cell cycle inhibitors in inhibiting cell cycle progression, by presenting substantial inhibition at the G1/S and G2/M cell cycle transitions. More importantly, the miR-143/506 treatment presented a broader application, effectively downregulating CDK1 and CDK4 levels, and reducing cell growth in PC cells. These findings suggest that the miR-143/506 combination acts as a promising approach to inhibit cell cycle progression for cancer treatment with minimal toxicity to normal cells. 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: 1211441-98-3Reference of 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 causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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. Reference of 1211441-98-3

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