Tag: 100-200

Melin, Lea; Calosing, Cyrus; Kharenko, Olesya A.; Hansen, Henrik C.; Gagnon, Alexandre published an article in 2021. The article was titled 《Synthesis of NVS-BPTF-1 and evaluation of its biological activity》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Category: piperazines The information in the text is summarized as follows:

BPTF (bromodomain and PHD finger containing transcription factor) is a multidomain protein that plays essential roles in transcriptional regulation, T-cell homeostasis and stem cell pluripotency. As part of the chromatin remodeling complex hNURF (nucleosome remodeling factor), BPTF epigenetic reader subunits are particularly important for BPTF cellular function. Thus, in this paper, the synthesis of NVS-BPTF-1, I, a previously reported highly potent and selective BPTF-bromodomain inhibitor, is reported. Evaluation of the impact of the inhibition of BPTF-bromodomain using NVS-BPTF-1 on selected proteins involved in the antigen processing pathway revealed that exclusively targeting BPTF-bromodomain was insufficient to observe an increase of PSMB8, PSMB9, TAP1, and TAP2 proteins. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Category: piperazines)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Category: piperazines

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

In 2019,Chemistry & Biology Interface included an article by Ismail, Pathan Sultan; Khan, Irfan; Kumar, Vivek; Verma, Ved Prakash; Shukla, Monika; Dhasmana, Anupam; Pandey, Shashi; Singh, Girdhar Pal; Khan, Shahnawaz; Singh, Jaybir. Recommanded Product: 1-Methylpiperazine. The article was titled 《Synthesis and biological evaluation of 2,4-diaminopyrimidine-5-carbonitrile and N-(2-amino-5-cyanopyrimidin-4-yl)benzamide derivatives as EGFR inhibitors》. The information in the text is summarized as follows:

A series of 2,4-diaminopyrimidine-5-carbonitriles and N-(2-amino-5-cyanopyrimidin-4-yl)benzamides I and II [R = 1-piperidyl, 1-morpholinyl, 4-methylpiperazin-1-yl, 4-benzylpiperazin-1-yl, 4-(2-methoxyphenyl)piperazin-1-yl] were synthesized and their chem. structures were confirmed by 1H, 13C NMR and mass spectral data. Anticancer activity of all the synthesized compounds I and II were evaluated for in-vitro cytotoxic activity against a panel of four human cancer cell lines i.e., human breast (MCF-7), cervical cancer (C33A), oral (KB) and prostrate (DU-145). All the examined compounds, I and II demonstrated potent to moderate anticancer activity. Among all the synthesized compounds, I [ R = 1-(2-methoxyphenyl)piperazinyl] and II [R1 = 1-(2-methoxyphenyl)piperazinyl] exhibited more potent activity. Docking studies for I [ R = 1-(2-methoxyphenyl)piperazinyl] and II [R1 = 1-(2-methoxyphenyl)piperazinyl] into EGFR active site was carried out to investigate their potential binding modes. Therefore, compounds I [ R = 1-(2-methoxyphenyl)piperazinyl] and II [R1 = 1-(2-methoxyphenyl)piperazinyl] was considered as fascinating candidates for further expansion of more potent anticancer agents. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 1-Methylpiperazine

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

In 2019,Rasayan Journal of Chemistry included an article by Venkatasubramanian, H.; Sha, Sarojkumar; Hemalatha, S.; Easwaramoorthy, D.. Recommanded Product: 1-Methylpiperazine. The article was titled 《Synthesis, characterisation and antimicrobial activity of new nicotinamide-thiazole derivatives》. The information in the text is summarized as follows:

This work selected the already known mild active mols. such as Nicotinamide and Thiazole I [R = cyclopropyl, cyclobutyl, Ph, etc.] to enhance the activity against the disease-causing pathogens. Using peptide coupling reagent EDCI, nine compounds I were prepared and characterized by 1H NMR, Mass spectroscopy. The characterized compounds I were evaluated in-vitro antibacterial and antifungal activity against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumonia, Candida albicans by broth dilution method and zone of inhibition measured in millimeter. All the derivatives I showed good to moderate activity. Out of nine compounds I [R = thiomorpholinyl] showed better zone of inhibition between 27 mm and 34 mm. The outcomes of the result revealed that the diamide bond acts as an important pharmacophore and exposed the good inhibition behavior. The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 1-Methylpiperazine

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

The author of 《The Synthesis of 1,3,5-triazine Derivatives and JNJ7777120 Analogues with Histamine H4 Receptor Affinity and Their Interaction with PTEN Promoter》 were Latacz, Gniewomir; Kechagioglou, Petros; Papi, Rigini; Lazewska, Dorota; Wiecek, Malgorzata; Kaminska, Katarzyna; Wencel, Przemyslaw; Karcz, Tadeusz; Schwed, Johannes S.; Stark, Holger; Kyriakidis, Dimitrios A.; Kiec-Kononowicz, Katarzyna. And the article was published in Chemical Biology & Drug Design in 2016. Quality Control of 1-Methylpiperazine dihydrochloride The author mentioned the following in the article:

The involvement of histamine and H4 receptor (H4R) in cancer has been investigated recently using the H4R agonists and antagonists. The scope of the research project was synthesis and exploration of the consequences of a group of compounds with histamine H4 receptor (H4R) affinity on the promoter of PTEN gene encoding the antitumor PTEN protein. The series of novel compounds based either on H4R antagonists JNJ7777120 structure or 1,3,5-triazine scaffold were synthesized, evaluated for histamine H4R affinity and used in this study. Compounds 5 and 7 belonging to the group of JNJ7777120 analogs showed the highest interaction with the promoter of PTEN gene and weak affinity against H4R with Ki value >100 μm. These compounds showed no significant effect on neuroblastoma IMR-32 cells viability indicating no correlation between PTEN gene promoter affinity and antitumor activity. Compound 6, another JNJ7777120 analog, showed the highest effect on IMR-32 viability with calculated IC50 = 23.27 μm. The 1,3,5-triazine derivatives exhibited generally low or medium interaction with PTEN gene promoter. However, the 1,3,5-triazine derivative 11 with the para-bromo substituent showed the highest affinity against H4R with Ki value of 520 nm and may be considered as a new lead structure. The experimental process involved the reaction of 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Quality Control of 1-Methylpiperazine dihydrochloride)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Quality Control of 1-Methylpiperazine dihydrochloride

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

Hubert, Terrance D.; Eyman, Darrell P.; Wiemer, David F. published an article in Journal of Organic Chemistry. The title of the article was 《A convenient synthesis of bis(N-methylpiperazinyl)aluminum hydride: a reagent for the reduction of carboxylic acids to aldehydes》.Electric Literature of C5H14Cl2N2 The author mentioned the following in the article:

The reaction of LiAlH4 with N-methylpiperazine (HL) and N-methylpiperazine dihydrochloride (2:3:1) is a convenient method for the preparation of AlL2H. AlL2H reduces aliphatic, aromatic, and unsaturated carboxylic acids directly to the analogous aldehydes. The facile preparation of the reagent, together with the high yields and the ease of work-up in the reductions, make AlL2H an attractive reagent for this transformation. The results came from multiple reactions, including the reaction of 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Electric Literature of C5H14Cl2N2)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Electric Literature of C5H14Cl2N2

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

Application In Synthesis of 1-Methylpiperazine dihydrochlorideOn September 30, 1994 ,《Studies on anti-platelet agents. IV. A series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines as novel anti-platelet agents》 was published in Chemical & Pharmaceutical Bulletin. The article was written by Tanaka, Akito; Motoyama, Yukio; Takasugi, Hisashi. The article contains the following contents:

The syntheses and structure-activity relationships of a series of 2-substituted 4,5-bis(4-methoxyphenyl)pyrimidines, designed on the basis of structural analyses of several cyclooxygenase (CO) inhibitors, and their derivatives as anti-platelet agents based on CO inhibition are described. Among them, 4,5-bis(4-methoxyphenyl)-2-morpholinopyrimidine and 4,5-bis(4-methoxyphenyl)-2-(3,5-dimethylmorpholin-4-yl)pyrimidine showed potent inhibitory activity on malondialdehyde, formed by the CO-catalyzed oxygenation of arachidonic acid (A.A.) in prostanoids, production in vitro (73.4% inhibition at 10-8 M and IC50 = 1.4 × 10-8 M, resp.). Certain compounds were also examined in ex vivo studies. Of these compounds, 4,5-bis(4-methoxyphenyl)-2-(1-methyl-1,2,3,6,-tetrahydropyrid-4-yl)pyrimidine (11a) exhibited potent and long-lasting anti-platelet activity ex vivo, i.e., 11a showed 97% inhibition of platelet aggregation induced by A.A. even 24 h after oral administration of 3.2 mg/kg in guinea pigs, and 60-70% inhibition at 6 h after lower doses (1.0 mg/kg). The ex vivo activity of 11a is more than three times that of aspirin (aspirin showed 81% inhibitory activity on platelet aggregation induced by A.A. at 6 h after oral administration at 10 mg/kg is this study). Compound 11a also showed vasodilatory activity (ED50 = 5.3 × 10-6 M, while aspirin has no vasodilatory activity at 6.0 × 10-4 M). In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Application In Synthesis of 1-Methylpiperazine dihydrochloride) was used in this study.

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Application In Synthesis of 1-Methylpiperazine dihydrochloride

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

Category: piperazinesOn October 31, 2014 ,《Crystal growth, thermal and magnetic characterizations of a new ferromagnetic Ni(II) dimer》 appeared in Monatshefte fuer Chemie. The author of the article were Ben Salah, Assila Maatar; Walha, Sondra; Yahyaoui, Samia; Abdalrahman, Mahmoud; Turnbull, Mark M.; Mhiri, Tahar; Naili, Houcine. The article conveys some information:

Abstract: Single crystals of 1-methylpiperazine-1,4-diium hexaaquatetrachlorodinickel(II) dichloride, (C5H14N2)[Ni2Cl4(H2O)6]Cl2, were grown by hydrothermal techniques in aqueous solution The compound was characterized by DTA (TG-TDXD), single crystal x-ray diffraction, and variable temperature magnetic susceptibility. The compound crystallizes in the triclinic system (space group P1̅, Z = 2) with the following unit cell dimensions: a 6.611(3), b 8.776(4), c 17.457(8) Å, α 101.34(2), β 96.31(2), and γ 105.38(2)°. The structure was solved using 4,243 independent reflections and refined to R = 0.024. The structure of (C5H14N2)[Ni2Cl4(H2O)6]Cl2 can be described as mixed organic-inorganic layers along the [-101] direction. The Ni dimers show ferromagnetic exchange (J ∼ 15 K), while the interactions between the dimers are antiferromagnetic (J approx. -3 K). The 3-dimensional network is further linked by three types of H bonds (N-H···Cl, OW-H···Cl, and N-H···O), to build cation-anion cohesion. Dehydration of the precursor proceeds through three stages, leading to crystalline intermediary hydrate phases and an anhydrous compound Crystallog. data are given. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Category: piperazines)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Category: piperazines

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

Recommanded Product: 1-(Isopropylsulfonyl)piperazineOn September 28, 2017 ,《Structure-Activity Relationships of Potent, Targeted Covalent Inhibitors That Abolish Both the Transamidation and GTP Binding Activities of Human Tissue Transglutaminase》 was published in Journal of Medicinal Chemistry. The article was written by Akbar, Abdullah; McNeil, Nicole M. R.; Albert, Marie R.; Ta, Viviane; Adhikary, Gautam; Bourgeois, Karine; Eckert, Richard L.; Keillor, Jeffrey W.. The article contains the following contents:

Human tissue transglutaminase (hTG2) is a multifunctional enzyme. It is primarily known for its calcium-dependent transamidation activity that leads to formation of an isopeptide bond between glutamine and lysine residues found on the surface of proteins, but it is also a GTP binding protein. Overexpression and unregulated hTG2 activity have been associated with numerous human diseases, including cancer stem cell survival and metastatic phenotype. Herein, the authors present a series of targeted covalent inhibitors (TCIs) based on the previously reported Cbz-Lys scaffold. From this structure-activity relationship (SAR) study, novel irreversible inhibitors were identified that block the transamidation activity of hTG2 and allosterically abolish its GTP binding ability with a high degree of selectivity and efficiency (kinact/KI > 105 M-1 min-1). One optimized inhibitor (VA4) was also shown to inhibit epidermal cancer stem cell invasion with an EC50 of 3.9 μM, representing a significant improvement over the previously reported “”hit”” NC9. After reading the article, we found that the author used 1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4Recommanded Product: 1-(Isopropylsulfonyl)piperazine)

1-(Isopropylsulfonyl)piperazine(cas: 534615-34-4) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.Recommanded Product: 1-(Isopropylsulfonyl)piperazine

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

Bouassiria, M.; Laabaissi, T.; Benhiba, F.; El Faydy, M.; Fakhry, H.; Oudda, H.; Assouag, M.; Touir, R.; Guenbour, A.; Lakhrissi, B.; Warad, I.; Zarrouk, A. published an article in 2021. The article was titled 《Corrosion inhibition effect of 5-(4-methylpiperazine)-methylquinoline-8-ol on carbon steel in molar acid medium》, and you may find the article in Inorganic Chemistry Communications.Application In Synthesis of 1-Methylpiperazine The information in the text is summarized as follows:

The present study provides a new application of the 5-(4-methylpiperazinyl)-methylquinolin-8-ol (MPMQ) as an inhibitor for corrosion of carbon steel (CS) in acidic media (1 M HCl). The inhibition performance of MPMQ was evaluated using various methods including electrochem. impedance spectroscopy (EIS), potentiodynamic polarization (PDP), surface morphol. anal. (SEM), quantum chem. computations (DFT), and Monte Carlo simulations (MC). The obtained results, indicating that the compound as a mixed-type inhibitor significantly reduced the corrosion rate of CS due to the formation of a stable protective film on the metal surface. As confirmed by EIS, SEM and theor. studies, chem. adsorbed MPMQ mol. is a better corrosion inhibitor with higher corrosion performance of about 95% at room temperature Langmuir isotherm model is the most acceptable one to describe the MPMQ mols. adsorption on the CS-surface. Finally, the exptl. data correlated well with the theor. study. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Application In Synthesis of 1-Methylpiperazine)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Application In Synthesis of 1-Methylpiperazine

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

Related Products of 109-01-3In 2020 ,《Synthesis, biological evaluation and kinase profiling of novel S-benzo[4,5]thiazolo[2,3-c][1,2,4]triazole derivatives as cytotoxic agents with apoptosis-inducing activity》 was published in Journal of Molecular Structure. The article was written by Abdelazeem, Ahmed H.; Alqahtani, Alaa M.; Omar, Hany A.; Bukhari, Syed Nasir Abbas; Gouda, Ahmed M.. The article contains the following contents:

A novel set of S-benzo[4,5]thiazolo[2,3-c][1,2,4]triazoles I [R = (adamantan-1-yl)aminyl, pyrrolidin-1-ylmethyl, (hexylamino)methyl, [(1,3-benzothiazol-2-yl)amino]methyl, etc.] was synthesized. Cytotoxicity of these compounds was evaluated against three cancer cell lines of different origins, Hep3B, A549, and MCF-7. Three of these compounds I [R = (4-chlorophenyl)aminyl, piperidin-1-ylmethyl, [(adamantan-1-yl)amino]methyl] were screened by NCI for growth inhibitory activities against 60 cancer cell lines. The results revealed significant cytotoxic activities for compounds I [R = pyrrolidin-1-ylmethyl, (hexylamino)methyl, [(1,3-benzothiazol-2-yl)amino]methyl, etc.]. Among these derivatives, compounds I [R = azepan-1-ylmethyl, (4-methylpiperazin-1-yl)methyl (A), (hexylamino)methyl (B), [(adamantan-1-yl)amino]methyl (C), [(1,3-benzothiazol-2-yl)amino]methyl (D)] exhibited the highest cytotoxicity against the selected cancer cell lines with IC50 values between 3.17 and 14.18μM. The structure-activity relationship of compounds I [R = pyrrolidin-1-ylmethyl, (hexylamino)methyl, [(1,3-benzothiazol-2-yl)amino]methyl, etc.] indicated favorable cytotoxic results on the expansion of the cyclic amine and the substitution with aminothiazole moiety. A mechanistic study revealed the activation of caspase-3/7 in A549 cells on treatment with compounds A-D at 5-20μM. Moreover, the results of flow cytometric anal. suggested that compound D efficiently induced apoptosis in a dose-dependent manner. Compounds A, B, D also exhibited a weak to moderate inhibition of multiple kinases where compound D was the most active in inhibiting the activity of CDK2/Cyclin A1 (IC50 = 4.65μM). The current work provided a novel set of compounds I with cytotoxic, kinase inhibition, and apoptosis-inducing activities, which can serve as a lead for further optimization. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Related Products of 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Related Products of 109-01-3

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