Month: January 2023

Synthesis and amination of 2,4-dichloro-5-fluoropyrimidine was written by Kovalenko, A. L.;Krutikov, V. I.;Zolotukhina, M. M.;Alekseeva, L. E.. And the article was included in Zhurnal Obshchei Khimii in 1992.Formula: C7H16N2 This article mentions the following:

Chlorination of 5-fluorouracil by PCl₅ in the absence of solvent gave 92% dichlorofluoropyrimidine I which underwent amination by primary, secondary, and heterocyclic amines in aqueous solution to give 42-100% amines II [R = NH₂, H₂NC(:NH)NH, CH₂:CHCH₂NH, piperidino, 1-propylpiperazinyl, morpholino, imidazol-1-yl]. Amines II were fungicidal at 100 μg/mL against Candida, Cryptococcus, Aspergillus et al. 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. 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.Formula: C7H16N2

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

An integrated flow and microwave approach to a broad spectrum protein kinase inhibitor was written by Russell, Cecilia;Lin, Andrew J. S.;Hains, Peter;Simone, Michela I.;Robinson, Phillip J.;McCluskey, Adam. And the article was included in RSC Advances in 2015.Quality Control of 1-Boc-4-(4-Nitrophenyl)piperazine This article mentions the following:

The protein kinase inhibitor CTx-0152960 (6, 2-((5-chloro-2-((4-morpholinophenyl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide), and the piperazinyl analog, CTx-0294885 (7, 2-((5-chloro-2-((4-piperazin-1-ylphenyl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide), were prepared using a hybrid flow and microwave approach. The use of flow chem. approaches avoided the need for Boc-protection of piperidine in the key S_NAr coupling with 1-fluoro-4-nitrobenzene. Microwave coupling of 4-morphilinoaniline 8 and 4-(piperazine-1-yl)aniline 9 with 2-(2,5-dichloropyrimidine-4-ylamino)-N-methylbenzamide 10, proved to be the most efficacious route to the target analogs 6 and 7. This hybrid methodol. reduced the number of synthetic steps, gave enhanced overall yields and increased atom economy through step reduction and minimal requirement for chromatog. purification, relative to the original batch synthesis approach. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Quality Control of 1-Boc-4-(4-Nitrophenyl)piperazine).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) 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. Quality Control of 1-Boc-4-(4-Nitrophenyl)piperazine

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

Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability was written by Liu, Yu;Liu, Zining;Cao, Xufeng;Liu, Xin;He, Huili;Yang, Yushe. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Category: piperazines This article mentions the following:

To improve antifungal activities, water solubility and bioavailability, a series of novel analogs of itraconazole-containing pyridine rings were designed and synthesized. Their antifungal activities were evaluated in vitro against six clin. important fungi by measuring the minimal inhibitory concentrations (MICs). Most of the compounds showed more potent antifungal activities than that of itraconazole. In particular, I [X = CH, X¹ = N, R = CH₂CHMe₂, CHMe₂; X = N, X¹ = CH, R = CHMe₂, CH₂CMe₂CH₂OH, II] exhibited much higher solubility and bioavailability than that of itraconazole. The bioavailability of II (42.2%) was five times higher than that of itraconazole (8%) and was neg. for genetic toxicol. in the Ames test. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3Category: piperazines).

tert-Butyl 4-(5-aminopyridin-2-yl)piperazine-1-carboxylate (cas: 119285-07-3) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands was written by Zhao, Hong-Yi;Wang, Hai-Peng;Mao, Yu-Ze;Zhang, Hao;Xin, Minhang;Xi, Xiao-Xiao;Lei, Hao;Mao, Shuai;Li, Dong-Hui;Zhang, San-Qi. And the article was included in Journal of Medicinal Chemistry in 2022.Product Details of 182618-86-6 This article mentions the following:

To overcome the intractable problem of drug resistance, proteolysis targeting chimeras (PROTACs) targeting EGFR mutants were developed by optimizing covalent EGFR ligands. Covalent or reversible covalent pyrimidine- or purine-containing PROTACs were designed, synthesized, and evaluated. As a consequence, covalent PROTAC I, with a novel purine-containing EGFR ligand, was discovered as a highly potent degrader against EGFR^L858R/T790M and EGFR^del19, reaching the lowest DC₅₀ values among all reported EGFR-targeting PROTACs. Furthermore, I exhibited excellent cellular activity against the H1975 and HCC827 cell lines with high selectivity. Mechanism investigation indicated that the lysosome was involved in the degradation process. Importantly, the covalent binding strategy was proven to be an effective approach for the design of PROTACs targeting EGFR^L858R/T790M, which laid the practical foundation for further development of potent EGFR-targeting PROTACs. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Product Details of 182618-86-6).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) 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.Product Details of 182618-86-6

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

Orally Active 7-Substituted (4-Benzylphthalazin-1-yl)-2-methylpiperazin-1-yl]nicotinonitriles as Active-Site Inhibitors of Sphingosine 1-Phosphate Lyase for the Treatment of Multiple Sclerosis was written by Weiler, Sven;Braendlin, Nadine;Beerli, Christian;Bergsdorf, Christian;Schubart, Anna;Srinivas, Honnappa;Oberhauser, Berndt;Billich, Andreas. And the article was included in Journal of Medicinal Chemistry in 2014.HPLC of Formula: 149554-29-0 This article mentions the following:

Sphingosine 1-phosphate (S1P) lyase has recently been implicated as a therapeutic target for the treatment of multiple sclerosis (MS), based on studies in a genetic mouse model. Potent active site directed inhibitors of the enzyme are not known so far. Here we describe the discovery of (4-benzylphthalazin-1-yl)-2-methylpiperazin-1-yl]nicotinonitrile 5 in a high-throughput screen using a biochem. assay, and its further optimization. This class of compounds was found to inhibit catalytic activity of S1PL by binding to the active site of the enzyme, as seen in the cocrystal structure of derivative 31 with the homodimeric human S1P lyase. 31 induces profound reduction of peripheral T cell numbers after oral dosage and confers pronounced protection in a rat model of multiple sclerosis. In conclusion, this novel class of direct S1P lyase inhibitors provides excellent tools to further explore the therapeutic potential of T cell-targeted therapies in multiple sclerosis and other autoimmune and inflammatory diseases. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0HPLC of Formula: 149554-29-0).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) 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.HPLC of Formula: 149554-29-0

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

Tricyclic pharmacophore-based molecules as novel integrin α_vβ₃ antagonists. Part 1: Design and synthesis of a lead compound exhibiting α_vβ₃/α_IIbβ₃ dual antagonistic activity was written by Kubota, Dai;Ishikawa, Minoru;Yamamoto, Mikio;Murakami, Shoichi;Hachisu, Mitsugu;Katano, Kiyoaki;Ajito, Keiichi. And the article was included in Bioorganic & Medicinal Chemistry in 2006.Electric Literature of C16H22N2O4 This article mentions the following:

In order to generate novel compounds with integrin α_vβ₃-antagonistic activity together with antiplatelet activity, tricyclic pharmacophore-based mols. were designed and synthesized. Although piperazine-containing compounds initially prepared were selective α_IIbβ₃ antagonists, replacement of piperazine with piperidine furnished a potent α_vβ₃/α_IIbβ₃ dual antagonist. Structure-activity relationship (SAR) studies provided clues for further development of tricyclic pharmacophore-based integrin antagonists. In the experiment, the researchers used many compounds, for example, 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4Electric Literature of C16H22N2O4).

4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid (cas: 162046-66-4) 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.Electric Literature of C16H22N2O4

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

Effects of inclusion complexation and degree of protonation on cloud point of poly(N-acryloyl-N’-propylpiperazine) was written by Guo, Kai;Sun, Liang;Wu, Meng-chun;Wang, Shao-dan;Wang, Li-yan. And the article was included in Gaodeng Xuexiao Huaxue Xuebao in 2011.Application In Synthesis of 1-Propylpiperazine This article mentions the following:

Poly(N-acryloyl-N’-propylpiperazine) (PAcrNPP) is a pH- and temperature-responsive homopolymer. Degree of protonation of PAcrNPP can be changed by adjusting pH of the solution Cloud point of PAcrNPP increased with increasing degree of protonation. We investigated the effects of different sizes of cyclodextrins( CD) on cloud point of PAcrNPP. It was found that α-CD showed a significant effect on cloud point of PAcrNPP while γ-CD had almost no effect on its cloud point. At pH = 9.0 and pH = 7.4, we measured cloud points of PAcrNPP solutions containing different concentrations of α-CD. Cloud point of PAcrNPP solutions rises with increase of concentration of α-CD. Further more, we deduced an equation on the basis of contributions of different forms of PAcrNPP to cloud point. This equation describes the combined effect of complexation of CD and degree of protonation on cloud point from the viewpoint of chem. equilibrium In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Application In Synthesis of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) 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.Application In Synthesis of 1-Propylpiperazine

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

Optimization of Small Molecules That Sensitize HIV-1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity was written by Grenier, Melissa C.;Ding, Shilei;Vezina, Dani;Chapleau, Jean-Philippe;Tolbert, William D.;Sherburn, Rebekah;Schon, Arne;Somisetti, Sambasivarao;Abrams, Cameron F.;Pazgier, Marzena;Finzi, Andres;Smith, Amos B.. And the article was included in ACS Medicinal Chemistry Letters in 2020.Related Products of 149057-19-2 This article mentions the following:

With approx. 37 million people living with HIV worldwide and an estimated 2 million new infections reported each year, the need to derive novel strategies aimed at eradicating HIV-1 infection remains a critical worldwide challenge. One potential strategy would involve eliminating infected cells via antibody-dependent cellular cytotoxicity (ADCC). HIV-1 has evolved sophisticated mechanisms to conceal epitopes located in its envelope glycoprotein (Env) that are recognized by ADCC-mediating antibodies present in sera from HIV-1 infected individuals. Our aim is to circumvent this evasion via the development of small mols. that expose relevant anti-Env epitopes and sensitize HIV-1 infected cells to ADCC. Rapid elaboration of an initial screening hit using parallel synthesis and structure-based optimization has led to the development of potent small mols. that elicit this humoral response. Efforts to increase the ADCC activity of this class of small mols. with the aim of increasing their therapeutic potential was based on our recent cocrystal structures with gp120 core. In the experiment, the researchers used many compounds, for example, 4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (cas: 149057-19-2Related Products of 149057-19-2).

4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid (cas: 149057-19-2) 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. 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.Related Products of 149057-19-2

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

Synthesis and evaluation of novel amonafide-polyamine conjugates as anticancer agents was written by Wang, Yuxia;Zhang, Jianying;Li, Meng;Li, Ming;Xie, Songqiang;Wang, Chaojie. And the article was included in Chemical Biology & Drug Design in 2017.Related Products of 373608-48-1 This article mentions the following:

Hydrochloride salts of aminoacetamido and ureido-substituted analogs of amonafide I [R = Bu, cyclohexyl, Me₂NCH₂CH₂, H₂N(CH₂)₃, H₂N(CH₂)₄, 3-(4-Boc-1-piperazinyl)propyl, H₂N(CH₂)_nNH(CH₂)_m, H₂N(CH₂)_mNH(CH₂)_nNH(CH₂)_m; m, n = 1, 2; X = bond, CH₂] were prepared as potential antitumor agents; their antitumor activity against various human cancer cell lines, the toxicities of selected compounds, and the in vivo antitumor activity and inhibition of cell migration and metastasis of I•5 HCl [R = H₂N(CH₂)₂NH(CH₂)₂NH(CH₂)₂; X = CH₂] (II) alone in concert with aspirin were determined Amonafide analogs with urea linkers were not active. Aspirin elevated the potency of II against tumor cells, wound healing, and the protein expression of cyclic D1 and MMP9; in vivo trials on three H22 tumor transplant models demonstrated that the combination of II and aspirin inhibited tumor growth and metastasis and extended lifespan while showing reduced side effects compared to amonafide. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Related Products of 373608-48-1).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) 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 125–130 °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 373608-48-1

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

N-aryl- or N-alkylpiperazine derivatives: the role of N-substituent on σ₁, σ₂, 5-HT_1A and D₂ receptor affinity was written by Perrone, Roberto;Berardi, Francesco;Colabufo, Nicola A.;Leopoldo, Marcello;Abate, Carmen;Tortorella, Vincenzo. And the article was included in Medicinal Chemistry Research in 2000.Recommanded Product: 21867-64-1 This article mentions the following:

The binding profile at σ₁, σ₂, 5-HT_1A and D₂ receptors of eight N-substituted-N’-[3-(1,2,3,4-tetrahydro-5-methoxy-1-naphthalenyl)propyl]piperazines is reported. Results indicated that a suitable substitution can lead to potent 5-HT_1A or σ₁, or σ₂ ligands. 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 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.Recommanded Product: 21867-64-1

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