Category: piperazines

Thermal Stability and Utility of Dienes as Protecting Groups for Acrylamides was written by Hooper, Annie R.;Burns, Alexander S.. And the article was included in ACS Medicinal Chemistry Letters in 2022.Category: piperazines This article mentions the following:

Herein, several diene-acrylamide adducts with a range of thermal stabilities toward retro-Diels-Alder deprotection of the acrylamide, enabling this masked functionality to be introduced early in a synthetic route and deprotected in a specific temperature range was reported. Through kinetic studies, solvent and structural trends that impact the stability of trimethylsilyl cyclopentadiene (TMS-CP) acrylamide adducts was identified. TMS-CP protected acrylamides were installed on several amine-containing drugs, whose acrylamides were thermally unveiled (T = 160掳C, time 鈮?1 h) in moderate to high yields. The potential utility of this protection strategy by improving the yield of a base-promoted S_NAr reaction when the acrylamide WAs masked. 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: 571190-30-2Category: piperazines).

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. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. 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

Characteristics of drugs evaluated by computational chemistry. (5). Typical antipsychotics was written by Hayano, Taizo;Kishioka, Shiroh;Yamamoto, Hiroyuki;Ikoma, Yoshihisa. And the article was included in Wakayama Igaku in 2005.Synthetic Route of C22H30N4O2S2 This article mentions the following:

Antipsychotics are divided into two types, i.e. typical type and atypical type. Typical type mainly includes phenothiazines and butyrophenones. Risperidone is located on the boundary. We furthermore divide the typical type into umbrella shape and cylindrical shape based on the mol. form. They have the side chain that connect with main ring with characteristic bond angle. Electron d. was high on main ring where HOMO and LUMO localized and low on terminal chain. Statistical anal. showed that there are no significant difference on the electron energies, the dipole moments, the dihedral angles between umbrella shape mols. and cylindrical ones. These results suggested the importance of the Pr group joining to the side chain with main ring. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Synthetic Route of C22H30N4O2S2).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) 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. 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 C22H30N4O2S2

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

Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors was written by Cumming, J. N.;Le, T. X.;Babu, S.;Carroll, C.;Chen, X.;Favreau, L.;Gaspari, P.;Guo, T.;Hobbs, D. W.;Huang, Y.;Iserloh, U.;Kennedy, M. E.;Kuvelkar, R.;Li, G.;Lowrie, J.;McHugh, N. A.;Ozgur, L.;Pan, J.;Parker, E. M.;Saionz, K.;Stamford, A. W.;Strickland, C.;Tadesse, D.;Voigt, J.;Wang, L.;Wu, Y.;Zhang, L.;Zhang, Q.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2008.COA of Formula: C16H22N2O3 This article mentions the following:

Guided by structure-based design two series of potent inhibitors of BACE1, were synthesized and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2′ pocket. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate (cas: 78551-60-7COA of Formula: C16H22N2O3).

tert-Butyl 4-benzyl-3-oxopiperazine-1-carboxylate (cas: 78551-60-7) 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. 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.COA of Formula: C16H22N2O3

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

Inhibition of Fibroblast Growth Factor Receptor by AZD4547 Protects Against Inflammation in Septic Mice was written by Huang, Yueyue;Wang, Fen;Li, Hao;Xu, ShunYao;Xu, Wenwei;Pan, XiaoJun;Hu, Yufeng;Mao, Lingjie;Qian, Songzan;Pan, Jingye. And the article was included in Inflammation in 2019.Related Products of 1035270-39-3 This article mentions the following:

Sepsis is a life-threatening condition caused by the dysregulated host immune response to infection characterized by excessive secretion of inflammatory factors. AZD4547 is a selective inhibitor of fibroblast growth factor receptors that participates in the inflammatory response. The aim of this study was to investigate the inflammation-targeting effects and related mol. mechanisms of AZD4547 in sepsis using a cecal ligation and puncture model and RAW264.7 macrophages stimulated with lipopolysaccharide. AZD4547 improved the survival of CLP mice and exhibited a robust protective function against lung damage histol. Pretreatment with AZD4547 significantly alleviated the expression of the pro-inflammatory factors IL-1尾, IL-6, TNF-伪, MMP9, and CXCL10 both in vivo and in vitro. In addition, AZD4547 suppressed the proliferative activity of macrophages in lung tissue and RAW264.7 macrophages. In addition, the LPS-induced phosphorylation of key proteins of NF-魏B/MAPK/STAT3 pathways in RAW264.7 macrophages, such as p65, I魏B-伪, Erk1/2, JNK, and STAT3 proteins, could be inhibited by AZD4547 pretreatment. In conclusion, AZD4547 exerts a protective effect against excessive inflammatory damage in septic mice and may have the potential for use as an effective drug for the management of sepsis. 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: 1035270-39-3Related Products of 1035270-39-3).

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. 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.Related Products of 1035270-39-3

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

Virtual screening and biological characterization of novel histone arginine methyltransferase PRMT1 inhibitors was written by Heinke, Ralf;Spannhoff, Astrid;Meier, Rene;Trojer, Patrick;Bauer, Ingo;Jung, Manfred;Sippl, Wolfgang. And the article was included in ChemMedChem in 2009.Reference of 129-74-8 This article mentions the following:

Lysine and arginine methyltransferases participate in the posttranslational modification of histones and regulate key cellular functions. Protein arginine methyltransferase 1 (PRMT1) has been identified as an essential component of mixed lineage leukemia (MLL) oncogenic complexes, revealing its potential as a novel therapeutic target in human cancer. The first potent arginine methyltransferase inhibitors were recently discovered by random- and target-based screening approaches. Herein we report virtual and biol. screening for novel inhibitors of PRMT1. Structure-based virtual screening (VS) of the Chembridge database composed of 328 000 mols. was performed with a combination of ligand- and target-based in silico approaches. Nine inhibitors were identified from the top-scored docking solutions; these were exptl. tested using human PRMT1 and an antibody-based assay with a time-resolved fluorescence readout. Among several aromatic amines, an aliphatic amine and an amide were also found to be active in the micromolar range. In the experiment, the researchers used many compounds, for example, 1-(4-(tert-Butyl)benzyl)-4-((4-chlorophenyl)(phenyl)methyl)piperazine dihydrochloride (cas: 129-74-8Reference of 129-74-8).

1-(4-(tert-Butyl)benzyl)-4-((4-chlorophenyl)(phenyl)methyl)piperazine dihydrochloride (cas: 129-74-8) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. 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.Reference of 129-74-8

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

Spectrophotometric determination of some phenothiazine derivatives in pharmaceutical preparations was written by Revanasiddappa, H.D.;Ramappa, P.G.. And the article was included in Eastern Pharmacist in 1995.Related Products of 316-81-4 This article mentions the following:

A simple, accurate and rapid method for the quant. determination of phenothiazine drugs in either the bulk or in pharmaceuticals is based on the development of colored compounds with vanadoboric acid in acid medium. The reaction is suggested to proceed via oxidation of the phenothiazine nucleus into a semiquinonoid radical. A study of the effect of commonly associated excipients revealed that they did not cause any interference. Statistical anal. of results indicates that the method is precise and accurate. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Related Products of 316-81-4).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. 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).Related Products of 316-81-4

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

Selectivity Data: Assessment, Predictions, Concordance, and Implications was written by Gao, Cen;Cahya, Suntara;Nicolaou, Christos A.;Wang, Jibo;Watson, Ian A.;Cummins, David J.;Iversen, Philip W.;Vieth, Michal. And the article was included in Journal of Medicinal Chemistry in 2013.Application of 692737-80-7 This article mentions the following:

Could high-quality in silico predictions in drug discovery eventually replace part or most of exptl. testing. To evaluate the agreement of selectivity data from different exptl. or predictive sources, we introduce the new metric concordance min. significant ratio (cMSR). Empowered by cMSR, we find the overall level of agreement between predicted and exptl. data to be comparable to that found between exptl. results from different sources. However, for mols. that are either highly selective or potent, the concordance between different exptl. sources is significantly higher than the concordance between exptl. and predicted values. We also show that computational models built from one data set are less predictive for other data sources and highlight the importance of bias correction for assessing selectivity data. Finally, we show that small-mol. target space relationships derived from different data sources and predictive models share overall similarity but can significantly differ in details. In the experiment, the researchers used many compounds, for example, 4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7Application of 692737-80-7).

4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7) 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.Application of 692737-80-7

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

Effect of buspirone, a serotonin1A partial agonist, on cognitive function in schizophrenia: a randomized, double-blind, placebo-controlled study. was written by Sumiyoshi, Tomiki;Park, Sohee;Jayathilake, Karu;Roy, Ajanta;Ertugrul, Aygun;Meltzer, Herbert Y. And the article was included in Schizophrenia research in 2007.Application of 112457-95-1 This article mentions the following:

In previous studies, we demonstrated that tandospirone, a serotonin-5-HT1A partial agonist, added to ongoing treatment with small to moderate doses of typical antipsychotic drugs, improved executive function and verbal learning and memory. However, tandospirone is not available in most countries, and atypical antipsychotic drugs (AAPDs) have largely replaced typical antipsychotic drugs as the primary treatment for schizophrenia. Therefore, the goal of this randomly assigned placebo-controlled double-blind study was to determine if the addition of buspirone, a widely available 5-HT1A partial agonist, would enhance cognitive function, in subjects with schizophrenia treated with AAPDs. Seventy-three patients with schizophrenia, who had been treated with an AAPD for at least three months, were randomly assigned to receive either buspirone, 30 mg/day, or matching placebo. All other medications remained unchanged. Attention, verbal fluency, verbal learning and memory, verbal working memory, and executive function, as well as psychopathology, were assessed at baseline, and 6 weeks, and 3 and 6 months after baseline. A significant Time x Group interaction effect was noted on the Digit Symbol Substitution Test, a measure of attention/speeded motor performance, due to better performance of the buspirone group compared to the placebo group at 3 months. No significant interaction effects were noted for other domains of cognition. Scores on the Brief Psychiatric Rating Scale (Total, Positive) were improved during treatment with buspirone but not placebo, but the effects did not reach statistical significance. The results of this study showed a possible benefit of buspirone augmentation of AAPDs to enhance attention. However, we did not replicate the results of the previous study with tandospirone, which may be due to the differences between tandospirone and buspirone, between typical antipsychotics and AAPDs, or a combination of the above. Further study to determine the usefulness of 5-HT1A agonist treatment in schizophrenia is indicated. In the experiment, the researchers used many compounds, for example, rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1Application of 112457-95-1).

rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1) 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).Application of 112457-95-1

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

TP-0903 inhibits neuroblastoma cell growth and enhances the sensitivity to conventional chemotherapy was written by Aveic, Sanja;Corallo, Diana;Porcu, Elena;Pantile, Marcella;Boso, Daniele;Zanon, Carlo;Viola, Giampietro;Sidarovich, Viktoryia;Mariotto, Elena;Quattrone, Alessandro;Basso, Giuseppe;Tonini, Gian Paolo. And the article was included in European Journal of Pharmacology in 2018.Related Products of 1341200-45-0 This article mentions the following:

Neuroblastoma (NB) is an embryonal tumor with low cure rate for patients classified as high-risk. This class of NB tumors shows a very complex genomic background and requires aggressive treatment strategies. In this work we evaluated the efficacy of the novel multi-kinase inhibitor TP-0903 in impairing NB cells’ growth, proliferation and motility. In vitro studies were performed using cell lines with different mol. background, and in vivo studies were done using the zebrafish exptl. model. Our results confirmed a strong cytotoxicity of TP-0903 already at the sub-micro molar concentrations The observed cytotoxicity of TP-0903 was irreversible and the resulting apoptosis was caspase dependent. In addition, TP-0903 impaired colony formation and neurosphere creation. Depending on the mol. background of the selected NB cell lines, TP-0903 influenced either their capacity to migrate, to complete their cell cycle or both. Likewise, TP-0903 reduced NB cells intravasation in vitro and in vivo. Importantly, TP-0903 showed remarkable pharmacol. efficacy not only as a mono-treatment, but also in combination with conventional chemotherapy drugs (ATRA, cisplatin, and VP16) in different types of NB cells. In conclusion, the multi-kinase activity of TP-0903 allowed the impairment of several biol. processes required for expansion of NB cells, making them more vulnerable to the conventional chemotherapeutics. Altogether, our results support the eligibility of TP-0903 for further (pre)clin. assessments in NB. In the experiment, the researchers used many compounds, for example, 2-((5-Chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide (cas: 1341200-45-0Related Products of 1341200-45-0).

2-((5-Chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide (cas: 1341200-45-0) 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. Related Products of 1341200-45-0

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

Population structure of the Salmonella enterica serotype Oranienburg reveals similar virulence, regardless of isolation years and sources was written by Gonzalez-Torres, Berenice;Gonzalez-Gomez, Jean P.;Ramirez, Karina;Castro-del Campo, Nohelia;Gonzalez-Lopez, Irvin;Garrido-Palazuelos, Lennin I.;Chaidez, Cristobal;Medrano-Felix, Jose A.. And the article was included in Gene in 2023.Synthetic Route of C17H18FN3O3 This article mentions the following:

Salmonella enterica serotype Oranienburg is a multi-host, ubiquitous, and prevalent Non-typhoidal Salmonella (NTS) in subtropical rivers, particularly in sediments; little studied so far possible the adaptation and establishment of this microorganism based on its genetic content. This study was focused on the first five genomes of S. Oranienburg in sediments through whole-genome sequencing (WGS) and 61 river water genomes isolated in previous studies. Results showed an open pangenome with 5,594 gene clusters (GCs), and the division of their categories showed; 3,303 core genes, 741 persistent genes, 1,282 accessory genes, and 268 unique genes. Addnl., it showed three main subclades within the same serotype and showed a conserved genetic content, suggesting the display of different adaptation strategies to its establishment. Nine genes for antimicrobial resistance were detected: aac (6鈥? – Iy, H-NS, golS, marA, mdsABC, mdtK, and sdiA, and a mutation in the parC gene p. T57S generating a resistance. In addition, virulence genes and pathogenicity islands (SPI鈥瞫) were analyzed, finding 92 genes and an identity above 80 % in the SPI鈥瞫 1 to 5, and the centisomes 54 and 63. The environmental strains of S. Oranienburg do not represent a concern as multidrug resistance (MDR) bacterium; however, virulence genes remain a potential health risk. This study contributes to understanding its adaptation to aquatic environments in Mexico. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1Synthetic Route of C17H18FN3O3).

1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid (cas: 85721-33-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Synthetic Route of C17H18FN3O3

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