Category: 109-01-3

Product Details of 109-01-3In 2021 ,《Synthesis and characterization of new potent TLR7 antagonists based on analysis of the binding mode using biomolecular simulations》 appeared in European Journal of Medicinal Chemistry. The author of the article were Pal, Sourav; Paul, Barnali; Bandopadhyay, Purbita; Preethy, Nagothy; Sarkar, Dipika; Rahaman, Oindrila; Goon, Sunny; Roy, Swarnali; Ganguly, Dipyaman; Talukdar, Arindam. The article conveys some information:

Aberrant activation of the endosomal Toll-like receptor 7 (TLR7) has been implicated in myriad autoimmune diseases and is an established therapeutic target in such conditions. Development of diverse TLR7 antagonists is mainly accomplished through random screening. To correlate human TLR7 (hTLR7) antagonistic activity with the structural features in different chemotypes, a hypothetical binding model is derived based on mol. docking anal. along with mol. dynamics (MD) simulations study. The binding hypothesis revealed different pockets, grooves and a central cavity where ligand-receptor interaction with specific residues through hydrophobic and hydrogen bond interactions take place, which correlate with TLR7 antagonistic activity, thus paving the way for rational design using varied chemotypes. Based on the structural insight thus gained, TLR7 antagonists with quinazoline, e.g., I were designed to understand the effect of engagement of these pockets as well as boundaries of the chem. space associated with them. The newly synthesized most potent hTLR7 antagonist, e.g., I, showed IC50 value of 1.03 ± 0.05μM and was validated by performing primary assay in human plasmacytoid dendritic cells (pDC) (ICpDC50: 1.42μM). The biol. validation of the synthesized mols. was performed in TLR7-reporter HEK293 cells as well as in human plasmacytoid dendritic cells (pDCs). This study provides a rational design approach, thus facilitating further development of novel small mol. hTLR7 antagonists based on different chem. scaffolds. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Product Details 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..Product Details of 109-01-3

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

Category: piperazinesIn 2020 ,《Synthesis and Aminoalkylation of N-Propargyl Triterpene Aldimines》 appeared in Russian Journal of Organic Chemistry. The author of the article were Petrova, A. V.; Khusnutdinova, E. F.; Mustafin, A. G.; Kazakova, O. B.. The article conveys some information:

Mannich reaction of N-propargyl triterpene aldimines obtained from betulonic and oleanonic aldehydes gave new aminoalkyl derivatives containing an N-methylpiperazine fragment. In the part of experimental materials, we found many familiar compounds, such as 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

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

Nguyen, William; Dans, Madeline G.; Ngo, Anna; Gancheva, Maria R.; Romeo, Ornella; Duffy, Sandra; de Koning-Ward, Tania F.; Lowes, Kym N.; Sabroux, Helene Jousset; Avery, Vicky M.; Wilson, Danny W.; Gilson, Paul R.; Sleebs, Brad E. published an article in 2021. The article was titled 《Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion》, and you may find the article in European Journal of Medicinal Chemistry.Synthetic Route of C5H12N2 The information in the text is summarized as follows:

The optimization and further characterization of the phenylsulfonyl piperazine class I [R = 4-Me, 3-t-Bu, 4-Br, etc.; R1 = pyrrolidin-1-yl, piperidin-1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, etc.; X = -(N(CH2)2N(CH2)2)-CH(CH3), -(NCH(CH3)N(CH2)2)-CH(CH3), -(NC(CH3)2N(CH2)2)-CH(CH3), etc.] was described. During the optimization process the functionality required for P. falciparum asexual stage activity was defined and determined the alpha-carbonyl S-Me isomer was important for antimalarial potency. The optimized compounds I also possessed comparable activity against multidrug resistant strains of P. falciparum and displayed weak activity against sexual stage gametocytes. The optimized compounds I blocked erythrocyte invasion consistent with the asexual activity observed and therefore the phenylsulfonyl piperazine analogs described could serve as useful tools for studying Plasmodium erythrocyte invasion. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Synthetic Route of C5H12N2)

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..Synthetic Route of C5H12N2

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

Paul, Anirudra; Kim, Jae Hyun; Daniel, Scott D.; Seidel, Daniel published their research in Angewandte Chemie, International Edition in 2021. The article was titled 《Diversification of Unprotected Alicyclic Amines by C-H Bond Functionalization: Decarboxylative Alkylation of Transient Imines》.Recommanded Product: 109-01-3 The article contains the following contents:

Despite extensive efforts by many practitioners in the field, methods for the direct α-C-H bond functionalization of unprotected alicyclic amines remain rare. A new advance in this area utilizes N-lithiated alicyclic amines. These readily accessible intermediates are converted to transient imines through the action of a simple ketone oxidant, followed by alkylation with a β-ketoacid under mild conditions to provide valuable β-amino ketones with unprecedented ease. Regioselective α’-alkylation is achieved for substrates with existing α-substituents. The method is further applicable to the convenient one-pot synthesis of polycyclic dihydroquinolones through the incorporation of a SNAr step. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 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..Recommanded Product: 109-01-3

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

In 2019,Journal of the American Chemical Society included an article by Paul, Anirudra; Seidel, Daniel. Electric Literature of C5H12N2. The article was titled 《α-Functionalization of Cyclic Secondary Amines: Lewis Acid Promoted Addition of Organometallics to Transient Imines》. The information in the text is summarized as follows:

Cyclic imines, generated in situ from their corresponding N-lithiated amines and a ketone hydride acceptor, undergo reactions with a range of organometallic nucleophiles to generate α-functionalized amines in a single operation. Activation of the transient imines by Lewis acids that are compatible with the presence of lithium alkoxides is crucial to accommodate a broad range of nucleophiles including lithium acetylides, Grignard reagents, and aryllithiums with attenuated reactivities. In the experimental materials used by the author, we found 1-Methylpiperazine(cas: 109-01-3Electric Literature of C5H12N2)

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..Electric Literature of C5H12N2

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

Zhang, Xiangyu; Huang, Hailan; Zhang, Ziheng; Yan, Jiangkun; Wu, Tianxiao; Yin, Wenbo; Sun, Yixiang; Wang, Xinran; Gu, Yanting; Zhao, Dongmei; Cheng, Maosheng published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors》.HPLC of Formula: 109-01-3 The article contains the following contents:

A series of benzofurans I [R = 3-aminopropylamino, pyrrolidin-3-ylamino, piperazin-1-yl, etc.; Ar = pyrimidin-5-yl, p-tolyl, 1-methylindazol-5-yl, etc.] were designed, synthesized and biochem. evaluated as LSD1 inhibitors based on scaffold hopping and conformational restriction strategy. Most of the compounds I potently suppressed the enzymic activities of LSD1 and potently inhibited tumor cells proliferation. In particular, the representative compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] exhibited excellent LSD1 inhibition at the mol. levels with IC50 = 0.065μM, as well as anti-proliferation against MCF-7, MGC-803, H460, A549 and THP-1 tumor cells with IC50 values of 2.90 ± 0.32, 5.85 ± 0.35, 2.06 ± 0.27, 5.74 ± 1.03 and 6.15 ± 0.49μM, resp. The binding modes of these compounds I were rationalized by mol. docking. Meanwhile, a preliminary druggability evaluation showed that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] displayed favorable liver microsomal stability and weak inhibitory activity against CYPs at 10μM. Remarkably, H460 xenograft tumors studies revealed that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] demonstrated robust in-vivo antitumor efficacy without significant side effects. All the results demonstrated that compound I [R = (3S)-3-amino-1-piperidyl; Ar = p-tolyl] could represent a promising lead for further development. In the experimental materials used by the author, we found 1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 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..HPLC of Formula: 109-01-3

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

The author of 《Synthesis, crystal structure, vibrational, optical properties, and a theoretical study of a new Pb(II) complex with bis(1-methylpiperazine-1,4-diium): [C5H14N2]2PbCl6·3H2O》 were Mrad, Mohamed Lahbib; Belhajsalah, Souhir; Abdelbaky, Mohammed Said M.; Garcia-Granda, Sergio; Essalah, Khaled; Ben Nasr, C.. And the article was published in Journal of Coordination Chemistry in 2019. Name: 1-Methylpiperazine The author mentioned the following in the article:

A study of the solid-state x-ray structure of the new organic-inorganic compound [C5H14N2]2PbCl6·3H2O shows a layered organization of the (PbCl6)4- anions, with (R2NH2)+ groups and water mols. developed in the [001] plane at x = (2n + 1)/4. The crystal structure is stabilized by N – H···Cl, N – H···O, O – H···Cl, O – H···O, and C – H···Cl hydrogen bonds. The powder x-ray diffraction and X-ray photoelectron spectroscopic (XPS) analyses confirm the phase purity of the crystal sample. The intermol. contacts are quantified using the Hirshfeld surfaces computational method. The major inter-contacts contributing to the Hirshfeld surfaces are H…Cl, H…H, and O…H. The vibrational modes were identified and assigned by IR and Raman spectroscopies. The optical properties were studied by UV-visible and photoluminescence spectroscopic studies. The compound was characterized by thermal anal. to determine its thermal behavior with respect to the temperature Finally, XPS anal. is reported for analyzing the surface chem. of [C5H14N2]2PbCl6·3H2O. In the experiment, the researchers used 1-Methylpiperazine(cas: 109-01-3Name: 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..Name: 1-Methylpiperazine

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