Tag: 100-200

Novel piperazine based benzamide derivatives as potential anti-glioblastoma agents inhibiting cell proliferation and cell cycle progression was written by Lu, Yingmei;Feng, Yiyue;Li, Zhao;Li, Junfang;Zhang, Honghua;Hu, Xiaoling;Jiang, Weifan;Shi, Tao;Wang, Zhen. And the article was included in European Journal of Medicinal Chemistry in 2022.Recommanded Product: 21867-64-1 This article mentions the following:

Highly efficacious and tolerable agents for the treatment of glioblastoma (GBM), the most common and aggressive primary brain tumor, are urgently needed. Herein, we reveal the design, synthesis and biol. evaluation of several piperazine based benzamide derivatives, which are based on the non-classical isostere principle and combination principle for GBM therapy. After structure-activity relationship (SAR) study, compound L19 was demonstrated as the most promising compound with IC₅₀ values of 0.15 μM, 0.29 μM, 1.25 μM against GBM C6, U87-MG, U251 cells, resp. Moreover, compound L19 could inhibit the proliferation, migration and invasion, as well as induce apoptosis and cell cycle arrest of GBM cell lines in vitro. From mechanism perspective, compound L19 could regulate the cell cycle-related proteins and influence the p16^INK4a-CDK4/6-pRb pathway by western blotting experiment What is worth mentioning is that compound L19 could penetrate the blood-brain barrier (BBB) with an exceptional brain-to-plasma ratio of 1.07 in vivo. Besides, the superior anti-glioblastoma potency in vivo of compound L19 was identified on U87-MG-xenograft model without any apparent host toxicity. Overall, the potential of compound L19 warrants further pre-clin. investigation for GBM therapy. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Recommanded Product: 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Recommanded Product: 21867-64-1

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

New antifilarial agents. 1. Epoxy sulfonamides and ethynesulfonamides was written by Brienne, Marie Josephe;Varech, Daniel;Leclercq, Martine;Jacques, Jean;Radembino, Nathalie;Dessalles, Christine;Mahuzier, Georges;Gueyouche, Chantal;Bories, Christian. And the article was included in Journal of Medicinal Chemistry in 1987.SDS of cas: 21867-64-1 This article mentions the following:

Two series of 2-substituted 1,2-epoxyethanesulfonamides I (R = Me, R¹ = Ph, substituted Ph, Me; NR₂ = morpholino, 4-methylpiperazinyl, etc.) and ethynesulfonamides, e.g., R₂NSO₂CCR¹ (II, R₂N = morpholino, 4-methylpiperazinyl, R¹ = Ph) were synthesized and evaluated for their antifilarial activity. Trans-I were stereospecifically prepared by a Darzens reaction between aldehydes and halomethanesulfonamides. Cis-I were obtained from ethynesulfonamides II by semihydrogenation followed by KOCl epoxidation 2-Substituted ethynesulfonamides II were synthesized from appropriate trans-ethensulfonamides by bromination-dehydrobromination. These products, as well as several synthetic intermediates, were evaluated for antifilarial activity against Molinema dessetae either in vivo in its natural host, the rodent Proechimys oris, or in vitro by a new test using cultures of the infective larvae. Most of the trans–I and II bearing a 2-aryl substituent were active in vitro. trans–I (NR₂ = morpholino, NMe₂, 4-methylpiperazinyl; R¹ = Ph, 3,4-Cl₂C₆H₃) and PhCCSO₂NR² (NR² = morpholino) showed marked macrofilaricidal activity in vivo without any microfilaricidal activity. The differences between the in vivo and in vitro results may be due, in part, to the low chem. stability of trans-I. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1SDS of cas: 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) 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. SDS of cas: 21867-64-1

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

Catalytic C(sp³)-H bond activation in tertiary alkylamines was written by Rodrigalvarez, Jesus;Nappi, Manuel;Azuma, Hiroki;Floden, Nils J.;Burns, Matthew E.;Gaunt, Matthew J.. And the article was included in Nature Chemistry in 2020.Name: 1-Propylpiperazine This article mentions the following:

The development of robust catalytic methods to assemble tertiary alkylamines provides a continual challenge to chem. synthesis. In this regard, transformation of a traditionally unreactive C-H bond, proximal to the nitrogen atom, into a versatile chem. entity would be a powerful strategy for introducing functional complexity to tertiary alkylamines. A practical and selective metal-catalyzed C(sp³)-H activation facilitated by the tertiary alkylamine functionality, however, remains an unsolved problem. Here, we report a Pd(II)-catalyzed protocol that appends arene feedstocks to tertiary alkylamines via C(sp³)-H functionalization. A simple ligand for Pd(II) orchestrates the C-H activation step in favor of deleterious pathways. The reaction can use both simple and complex starting materials to produce a range of multifaceted γ-aryl tertiary alkylamines and can be rendered enantioselective. The enabling features of this transformation should be attractive to practitioners of synthetic and medicinal chem. as well as in other areas that use biol. active alkylamines. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Name: 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) 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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Name: 1-Propylpiperazine

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

The discovery of potent antagonists of NPBWR1 (GPR7) was written by Romero, F. Anthony;Hastings, Nicholas B.;Moningka, Remond;Guo, Zhiqiang;Wang, Ming;Di Salvo, Jerry;Lei, Ying;Trusca, Dorina;Deng, Qiaolin;Tong, Vincent;Terebetski, Jenna L.;Ball, Richard G.;Ujjainwalla, Feroze. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Synthetic Route of C10H12N4 This article mentions the following:

The synthesis and evaluation of small mol. antagonists of the G protein-coupled receptor NPBWR1 (GPR7) are reported for the first time. [4-(5-Chloropyridin-2-yl)piperazin-1-yl][(1S,2S,4R)-4-{[(1R)-1-(4-methoxyphenyl)ethyl]amino}-2-(thiophen-3-yl)cyclohexyl]methanone (I) emerged as a hit from a high-throughput screen. Examination of substituents that focused on replacing the 5-chloropyridine and 4-methoxybenzylamino groups of I led to the identification of compounds that exhibited subnanomolar potencies as low as 660 pM {II [X = NH]} in the functional assay and 200 pM in the binding assay {II [X = O]}. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Synthetic Route of C10H12N4).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) 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 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 C10H12N4

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

Studies on the compounds related to azulene. I. Synthesis and antiallergic activity of guaiazulenylglyoxylamides, guaiazulenylglyoxylic acid esters and acylaminoguaiazulenes was written by Hamajima, Ryo;Iwano, Katsuyuki;Okuda, Hirohisa. And the article was included in Yakugaku Zasshi in 1978.Name: 1-Propylpiperazine This article mentions the following:

New guaiazulenylglyoxylamides, guaiazulenglyoxylic acid esters, guaiazulenylglyoxypiperazines, and acylaminoguaiazulenes were prepared, and their antiallergic activities were evaluated by passive cutaneous anaphylaxis (PCA) test in the rat. Guaiazulenylglyoxalyl chloride I (R = Cl) derived from guaiazulene and oxalyl chloride was converted into glyoxylamides, glyoxylic acid esters, and glyoxylpiperazines with appropriate amines, alcs., and piperazines. Acylaminoguaiazulenes were prepared from 3-aminoguaiazulene with the corresponding acid anhydride or acid chloride. Many of guaiazulenylglyoxylpiperazines, especially I (R = 4-R¹-piperazin-1-yl; R¹ = H, Me, Et, CH₂CO₂H, PhCH₂) showed a high antiallergic activity by oral administration, but none of the other types of compounds showed a significant activity. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Name: 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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.Name: 1-Propylpiperazine

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

A novel co-production process for piperazine and its N-monoalkyl derivatives was written by Wu, Zhiwei;Wang, Huabang;Sun, Meng;Du, Xiaobao;Chen, Ligong;Li, Yang. And the article was included in Research on Chemical Intermediates in 2012.Product Details of 21867-64-1 This article mentions the following:

A novel co-production process for piperazine and its N-monoalkyl derivatives has been established. N-β-hydroxyethyl-1,2-ethylenediamine and alcs. were used as the starting materials and the process was carried out over Cu-Cr-La/γ-Al₂O₃ in a fixed-bed reactor. Alcs. acted not only as the solvent but also as the alkylating reagent. The catalyst was characterized by XRD, XPS and BET. The results obtained showed that Cu⁰ particles in the catalyst were the active sites and doping with La led to enhancement of catalyst activity. Process conditions including reaction temperature, hydrogen pressure, and molar ratio of the reagents were optimized and the distribution of the products was found to be markedly dependent on reaction temperature Using optimum conditions, piperazine and its N-monoalkyl derivatives were obtained with satisfactory yields and distributions. The catalyst performed well for over 300 h. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Product Details of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) 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. 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.Product Details of 21867-64-1

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

Silica-bonded N-propylpiperazine sodium n-propionate as recyclable catalyst for synthesis of 4H-pyran derivatives was written by Niknam, Khodabakhsh;Borazjani, Nassim;Rashidian, Reza;Jamali, Abbas. And the article was included in Cuihua Xuebao in 2013.Computed Properties of C7H16N2 This article mentions the following:

Silica-bonded N-propylpiperazine sodium n-propionate (SBPPSP) was found to act as an efficient solid base for the preparation of a series of 4H-benzo[b]pyran derivatives SBPPSP was used as a recyclable heterogeneous solid base catalyst for the synthesis of 3,4-dihydropyrano[c]chromenes I [R = C₆H₅, 4-BrC₆H₄, 4-ClC₆H₄, etc.], 2-amino-4H-pyrans II, 1,4-dihydropyrano[2,3-c]pyrazoles III and 2-amino-4H-benzo[e]-chromenes IV via condensation reaction of dimedone, Et acetoacetate, 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one, and α-naphthol, resp., with aromatic aldehydes and malononitrile in refluxing aqueous ethanol. The heterogeneous solid base showed similar efficiency when reused in consecutive reactions. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Computed Properties of C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) 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. 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 C7H16N2

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

The use of solid-supported reagents within EOF-based micro reactors was written by Wiles, Charlotte;Watts, Paul;Haswell, Stephen J.. And the article was included in Special Publication – Royal Society of Chemistry in 2004.Formula: C7H16N2 This article mentions the following:

By incorporating a series of silica-supported bases into an EOF (electroosmotic flow)-based flow reactor, we have demonstrated the synthesis of eight condensation products in excellent yields, without the need for addnl. purification steps. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Formula: C7H16N2).

1-Propylpiperazine (cas: 21867-64-1) 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 125â€?30 °C. 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. Formula: C7H16N2

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

Synthesis of new and potent analogs of anti-tuberculosis agent 5-nitrofuran-2-carboxylic acid 4-(4-benzylpiperazin-1-yl)benzylamide with improved bioavailability was written by Tangallapally, Rajendra P.;Lee, Robin E. B.;Lenaerts, Anne J. M.;Lee, Richard E.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2006.Synthetic Route of C10H12N4 This article mentions the following:

Previously, the lead compound 5-nitrofuran-2-carboxylic acid 4-(4-benzylpiperazin-1-yl)benzylamide was identified in our anti-tuberculosis drug discovery program. Although this compound demonstrated excellent in vitro activity, it did not meet the expected in vivo profiles due to structural features that resulted in rapid metabolic cleavage and poor absorption, which therefore limited its bioavailability. In efforts to increase the bioavailability, a new series of analogs was successfully synthesized using three modification schemes: replacement of the benzyl group on the piperazine C-ring with carbamate and urea functional groups; introduction of a nitrogen atom into the aromatic ring-B; and expansion of the ring-B to a bicyclic tetrahydroisoquinoline moiety. These modifications retained strong activity and in some case gained superior anti-tuberculosis activity, increased absorption, and serum half life. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Synthetic Route of C10H12N4).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) 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.Synthetic Route of C10H12N4

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

Gas-liquid chromatography of some aliphatic and heterocyclic polyfunctional amines. II. Thermodynamics of the dissolution of amines in fixed phases was written by Andersons, A.;Shimanskaya, M. V.. And the article was included in Latvijas PSR Zinatnu Akademijas Vestis, Kimijas Serija in 1969.Related Products of 21867-64-1 This article mentions the following:

Solution thermodynamics in some nonpolar and polar stationary phases of 19 polyfunctional amines by means of gas-liquid chromatog. has been studied. The heats of solution, the excess heats of solution, the free energies, and entropies of the solution have been estimated The linear dependence of the thermodynamic properties on mol. weight or b.ps. of amines was shown to take place in nonpolar liquid phases. The maximum values of the thermodynamic properties were obtained in cases of polar liquid phases. Specific interactions take place between the amines and polar stationary phases: polyethylene glycols and Reoplex. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Related Products of 21867-64-1).

1-Propylpiperazine (cas: 21867-64-1) 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 125â€?30 °C. 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 21867-64-1

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