Category: piperazines

New compounds and reactions of sulfonamides with amines. XXXI. Syntheses of some N-[4-[2-(acylamino)ethyl]benzenesulfonyl]-4-alkylpiperazine-1-carboxamides was written by Gajewski, Feliks;Kozakiewicz, Irena. And the article was included in Acta Poloniae Pharmaceutica in 1982.Product Details of 21867-64-1 This article mentions the following:

Nineteen title compounds I (R = Me, R¹ = 2-ClC₆H₄, 3-ClC₆H₄, 2-BrC₆H₄, 2-MeC₆H₄, 4-NO₂C₆H₄, 2,4-Cl₂C₆H₃, 2,5-(MeO)ClC₆H₃, 2-furyl, pyridyl, 2-quinolyl, 2-pyrazinyl, 2-amino-3-pyrazinyl; R = Et, Pr, R¹ = 2,5-(MeO)ClC₆H₃, 2-pyrazinyl; R = Bu, R¹ = 2-pyrazinyl) were prepared as potential hypoglycemic agents. Most I were prepared by heating 4-[R¹CONH(CH₂)₂]C₆H₄SO₂NHCONH₂ with a substituted piperazine in dioxane. I [R = Me, R¹ = 2,5-(MeO)ClC₆H₃] was prepared from 4-[R¹CONH(CH₂)₂]C₆H₄SO₂NHCONHCO₂Me and N-methylpiperazine in PhMe. I (R = Me, R¹ = 2-pyrazinyl) was also obtained via I (R = Me, R¹ = Me) which was deacetylated with aqueous NaOH and the product acylated with pyrazine-2-carboxylic acid chloride in C₆H₁₂. 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. 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. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Product Details of 21867-64-1

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

Influence of external stimuli on the network properties of cationic poly(N-acryloyl-N’-propyl piperazine) hydrogels was written by Deen, G. Roshan;Mah, Chin Hao. And the article was included in Polymer in 2016.Related Products of 21867-64-1 This article mentions the following:

Stimuli-responsive cationic hydrogels based on N-acryloyl-N’-Pr piperazine (AcrNPP) crosslinked with N,N’-methylenebisacrylamide (Mba) and 1,4-butanedioldiacrylate (Bda) were prepared by UV light-initiated free-radical polymerization in bulk. The effect of external stimuli and type of crosslinker on the equilibrium swelling behavior and dynamic swelling was investigated in detail in buffer solution of various pH and temperatures The equilibrium swelling capacity of the gels was large in swelling medium at pH 3.0 than at pH 10.0 due to ionization of polymer network under acidic conditions. With increase in temperature from 25 鎺矯 to 45 鎺矯, the gels exhibited neg. temperature-responsive (thermo-shrinking/thermophobic) behavior with neg. activation energy for diffusion of water. The thermodn. parameters such as Gibbs’ free energy (铻朑), enthalpy (铻朒), and entropy (铻朣) for the swelling of gels as function of temperature were neg. indicating an exothermic swelling process. Water (media) transport mechanism and diffusion process in thin rectangular gels was studied. At pH 3.0, the diffusion process was non-Fickian (anomalous) while at pH 10.0 it was quasi-Fickian. The transport mechanism was partly influenced by the type of crosslinker in the gel. The dynamic swelling data was analyzed using early-time, late-time and Etters diffusion models. From the equilibrium swelling studies the average mol. weight between crosslinks (M_c), the crosslink d. (锜?sub>c), and the mesh size (灏? were determined The M_c was large at pH 3.0 due to ionization of polymer and chain expansion. The exptl. M_c was much larger than the theor. M_c which implied that the gels were loosely crosslinked real networks. The mesh size of gels were between 447 and 786 鑴?in the swollen (ionized) state (pH 3.0), and between 100 and 231 鑴?in the collapsed (non-ionized) state (pH 10.0). The mesh size increased between three to four times during the pH-dependent swelling transition. The state of water in fully swollen hydrogels which influences many important biomaterial properties was determined by differential scanning calorimetry. The bound water content of gels increased linearly with increase in pH of the swelling medium while the unbound water decreased. These hydrogels have potential to be used as controlled drug delivery systems and sorbents for removal of pollutants from water. 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. 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.Related Products of 21867-64-1

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

Design, Synthesis, Biological Screening, and Molecular Docking Studies of Piperazine-Derived Constrained Inhibitors of DPP-IV for the Treatment of Type 2 Diabetes was written by Kushwaha, Ram N.;Srivastava, Rohit;Mishra, Akansha;Rawat, Arun K.;Srivastava, Arvind K.;Haq, Wahajul;Katti, Seturam B.. And the article was included in Chemical Biology & Drug Design in 2015.Application of 149554-29-0 This article mentions the following:

Novel piperazine-derived conformationally constrained compounds were designed, synthesized, and evaluated for in vitro Dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. From a library of compounds synthesized, 1-(2-(4-(7-Chloro-4-quinolyl)piperazin-1-yl)acetyl)pyrrolidine (2g) was identified as a potential DPP-IV inhibitor exhibiting better inhibitory activity than P32/98, reference inhibitor. The in vivo studies carried out in STZ and db/db mice models indicated that the compound 2g showed moderate antihyperglycemic activity as compared to the marketed drug Sitagliptin. A two-week repeated dose study in db/db mice revealed that compound 2g significantly declined blood glucose levels with no evidence of hypoglycemia risk. Furthermore, it showed improvement in insulin resistance reversal and antidyslipidemic properties. Mol. docking studies established good binding affinity of compound 2g at the DPP-IV active site and are in favor of the observed biol. data. These data collectively suggest that compound 2g is a good lead mol. for further optimization studies. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Application of 149554-29-0).

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

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

Modular click chemistry libraries for functional screens using a diazotizing reagent was written by Meng, Genyi;Guo, Taijie;Ma, Tiancheng;Zhang, Jiong;Shen, Yucheng;Sharpless, Karl Barry;Dong, Jiajia. And the article was included in Nature (London, United Kingdom) in 2019.Related Products of 373608-48-1 This article mentions the following:

Alkyl and aryl azides were prepared from the corresponding primary alkyl and aryl amines by reaction with fluorosulfonyl azide generated in situ from a fluorosulfonylimidazolium triflate and sodium azide, expanding access to azides and both to the 1,2,3-triazoles derived from them and to functional screens employing them. The method allowed the preparation of a library of >1000 azides from the corresponding amines; the azide library underwent copper-catalyzed azide-alkyne cycloaddition reactions to yield a library of >1000 1,2,3-triazoles. 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. Piperazine belongs to the family of medicines called anthelmintics. 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 373608-48-1

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

Design, Synthesis, and Biological Evaluation of Mitochondria-Targeted Flavone-Naphthalimide-Polyamine Conjugates with Antimetastatic Activity was written by Dai, Fujun;Li, Qian;Wang, Yuxia;Ge, Chaochao;Feng, Chenyang;Xie, Songqiang;He, Haoying;Xu, Xiaojuan;Wang, Chaojie. And the article was included in Journal of Medicinal Chemistry in 2017.Synthetic Route of C12H25N3O2 This article mentions the following:

Approx. 90% of cancer-associated deaths result from disseminated tumors, indicating the ineffectiveness of current therapies and the imperative need of antimetastatic drugs. A novel pharmacophore with flavonoid and naphthalimide moieties was constructed by using a fragment-based drug design and a series of eight flavone-naphthalimide-polyamine conjugates were synthesized. In vitro evaluation revealed that compound I with a homospermidine motif displayed better cell selectivity between cancerous and normal liver cells than amonafide did. The in vivo assays on two hepatocellular carcinoma (HCC) models verified that I potently suppressed pulmonary metastasis with improved organ indexes compared to amonafide. Various experiments showed that I as a potential fluorescent chem. probe could target the mitochondria. Preliminary investigation into the mechanism of action of I indicated that it might harness a polyamine transporter for cell entrance, localize in the mitochondria, selectively cause reactive oxygen species (ROS) overproduction in hepatoma cells instead of normal liver cells, and finally lead to HCC cell apoptosis and migration inhibition via multiple ROS-mediated signaling pathways. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Synthetic Route of C12H25N3O2).

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 鎺矯 and boils at 125閳?30 鎺矯. 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 C12H25N3O2

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

Synthesis of substituted 5-amino-3-aryl-4-(methoxycarbonyl)isoxazoles was written by Alyab’ev, S. B.;Kosul’nikova, T. S.;Dmitriev, D. E.;Il’in, A. P.;Kravchenko, D. V.;Filimonov, S. I.;Ivashchenko, A. V.. And the article was included in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2007.Category: piperazines This article mentions the following:

A combinatorial library of substituted 5-amino-3-aryl-4-(methoxycarbonyl)isoxazoles was obtained by reaction of 3-aryl-4-methoxycarbonyl-5-chloroisoxazoles with primary and secondary amines in 1,4-dioxane in the presence of NEt₃ under parallel synthesis conditions. Products were obtained in yields of 21-95%. This reaction proceeds less uniformly in DMF in the presence of K₂CO₃, and, in the case of primary amines, bis(4-methoxycarbonyl-3-aryl-isoxazol-5-yl)arylamines are also formed in 20-69% yields. In the experiment, the researchers used many compounds, for example, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6Category: piperazines).

4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 鎺矯 and boils at 125閳?30 鎺矯. 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.Category: piperazines

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

Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier was written by Receveur, Jean-Marie;Murray, Anthony;Linget, Jean-Michel;Norregaard, Pia K.;Cooper, Martin;Bjurling, Emelie;Nielsen, Peter Aadal;Hoegberg, Thomas. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile This article mentions the following:

A series of amides, amidines and amidoximes have been made from the corresponding nitrile compounds, to provide potent antagonists and inverse agonists for the CB1 receptor with considerably lower lipophilicity, higher polar surface area and improved plasma/brain ratios compared to the centrally acting rimonabant. Extensive investigations of ADME and in vivo pharmacol. properties led to selection of the amide series and specifically the 4-(4-fluorophenyl)piperidin-4-ol derivative D4. A clear improvement in the peripheral profile over rimonabant was seen, although some contribution of central effect on the pronounced weight reduction in obese mice cannot be ruled out. In the experiment, the researchers used many compounds, for example, 6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0Recommanded Product: 6-(Piperazin-1-yl)nicotinonitrile).

6-(Piperazin-1-yl)nicotinonitrile (cas: 149554-29-0) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 鎺矯 and boils at 125閳?30 鎺矯. 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: 6-(Piperazin-1-yl)nicotinonitrile

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

New 1-aryl-3-substituted propanol derivatives as antimalarial agents was written by Perez-Silanes, Silvia;Berrade, Luis;Garcia-Sanchez, Rory N.;Mendoza, Adela;Galiano, Silvia;Perez-Solorzano, Berta Martin;Nogal-Ruiz, Juan J.;Martinez-Fernandez, Antonio R.;Aldana, Ignacio;Monge, Antonio. And the article was included in Molecules in 2009.Application In Synthesis of 1-Boc-4-(4-Nitrophenyl)piperazine This article mentions the following:

This paper describes the synthesis and in vitro antimalarial activity against a P. falciparum 3D7 strain of some new 1-aryl-3-substituted propanol derivatives Twelve of the tested compounds showed an IC₅₀ lower than 1 娓璏. These compounds were also tested for cytotoxicity in murine J774 macrophages. The most active compounds were evaluated for in vivo activity against P. berghei in a 4-day suppressive test. Compound 12 inhibited more than 50% of parasite growth at a dose of 50 mg/kg/day. In addition, an FBIT test was performed to measure the ability to inhibit ferriprotoporphyrin biocrystn. This data indicates that 1-aryl-3-substituted propanol derivatives hold promise as a new therapeutic option for the treatment of malaria. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6Application In Synthesis of 1-Boc-4-(4-Nitrophenyl)piperazine).

1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) 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.Application In Synthesis of 1-Boc-4-(4-Nitrophenyl)piperazine

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

Two birds with one stone: dendrimer surface engineering enables tunable periphery hydrophobicity and rapid endosomal escape was written by Wang, Zheng;Chen, Chao;Liu, Ruihong;Fan, Aiping;Kong, Deling;Zhao, Yanjun. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2014.Quality Control of 1-Propylpiperazine This article mentions the following:

Multifunctional thermosensitive dendrimeric nanocarriers were generated via tailored surface modification. Such design not only facilitated the rapid endosomal escape of dendrimers, but also achieved tunable surface hydrophobicity, which could be employed to achieve on-demand cargo release. These smart dendrimers are promising for enhancing intracellular drug delivery. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Quality Control of 1-Propylpiperazine).

1-Propylpiperazine (cas: 21867-64-1) 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.Quality Control of 1-Propylpiperazine

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

Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR^L858R/T790M NSCLCs by the conformation constrained strategy was written by Chen, Yang;Yang, Linlin;Qiao, Hui;Cheng, Zhongyu;Xie, Jiahao;Zhou, Wenjuan;Huang, Xin;Jiang, Yaoxuan;Yu, Bin;Zhao, Wen. And the article was included in European Journal of Medicinal Chemistry in 2020.Related Products of 611225-86-6 This article mentions the following:

Studies on the third-generation of epidermal growth factor receptor tyrosine kinase inhibitors (EGFRTKIs) targeting EGFR^L858R/T790M mutant remain hotspots, specifically for non-small cell lung cancer(NSCLC) were described. In the current study, a new series of EGFR-TKIs with thieno[3,2-d]pyrimidine derivatives bearing quinolin-2(1H)-ones I (R = 4-fluoro-phenylamino, 4-(4-methyl-piperazin-1-yl)-phenylamino, 4-morpholin-4-ylmethyl-phenylamino, etc.) was designed and synthesized, through conformational constrained strategy from the third generation of EGFR-TKI olmutinib. In vitro structure-activity relationship (SAR) studies indicated that compounds I (R = 4-(4-methyl-piperazin-1-yl)-phenylamino, 4-[1,4′]bipiperidinyl-1′-yl-3-fluoro-phenylamino, 4-(4-methyl-piperazin-1-ylmethyl)-phenylamino, 4-(4-ethyl-piperazin-1-ylmethyl)-phenylamino, 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) exhibited good selective inhibition to EGFR^L858R/T790M (IC₅₀ 閳?250 nM) over wild type EGFR (IC₅₀ > 10000 nM). The observed selectivity of compounds I (R = 4-[1,4′]bipiperidinyl-1′-yl-3-fluoro-phenylamino, 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) (A) was also proved by the computational mol. docking and the cellular thermal shift assay. These compounds I had good growth inhibitory effect on the four tested cancer cell lines. Specifically, I (R = 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) could significantly inhibit the colony formation, wound healing and the expression of p-EGFR and its downstream p-ERK in EGFR^L858R/T790M H1975 lung cancer cells. The above finding results suggest that the thieno[3,2-d]pyrimidine compounds, especially compounds A, can selectively target the mutant EGFR^L858R/T790M in vitro and at cellular level and may serve as the lead compounds for generating new series of the third generation EGFR-TKIs. In the experiment, the researchers used many compounds, for example, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6Related Products of 611225-86-6).

4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. 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 611225-86-6

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