Month: October 2022

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

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

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

Related Products of 109-01-3In 2019 ,《Solvent-free syntheses of two pcu topological indium phosphite-oxalates with a novel butterfly motif and proton conductivity》 was published in Microporous and Mesoporous Materials. The article was written by Jiang, Yansong; Song, Jianshu; Xiu, Zhijia; Huang, Liangliang; Gao, Fan; Jiao, Shufei; Bi, Yanfeng. The article contains the following contents:

Under solvent-free conditions, two new 3D open-framework indium phosphite-oxalates In5(HPO3)6(H1.5PO3)2(C2O4)2·(H2A)2, where A = C5N2H12 (compound 1) and C6N2H14 (compound 2), are synthesized by using 1-methylpiperazine and 1-ethylpiperazine as the structure-directing agent, resp. Single crystal x-ray diffraction reveals that these two compounds have the analog inorganic framework structures, which may be viewed as the assembly of butterfly motifs and [C2O2-4] groups. Interestingly, the butterfly motif is firstly reported in metal phosphite/phosphite-oxalate. By regarding the butterfly motifs as topol. equivalent 4-connected nodes and thus framework can be simplified into a uninodal pcu network with point symbol of (412, 63). 1 And 2 are also characterized by powder x-ray diffraction, IR spectroscopy, SEM, TGA, ICP-AES and elemental analyses. In addition, proton conduction was investigated by alternating-current impedance anal. and the results demonstrate that both compounds show high proton-conductive properties with the conductivity of 3.4 × 10-3 S cm-1 and 2.1 × 10-3 S cm-1 at 75° and 98% RH, resp. 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

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

《A Simplified Protocol for Routine Chemoselective Syntheses of Piperazines Substituted in the 1-Position by an Electron Withdrawing Group》 was written by Nemeckova-Herova, Dana; Pazdera, Pavel. Electric Literature of C10H15ClN2O2S And the article was included in Current Organic Synthesis on April 30 ,2015. The article conveys some information:

A simplified protocol for the routine direct chemoselective preparation of various piperazines substituted in the 1-position by an electron withdrawing group were reported. These synthesis were based on the reaction of piperazine-1-ium cation with different electrophilic reagents, such as acyl chlorides, anhydrides, sulfonyl chlorides, carbamoyl chlorides, and nitrourea as well. Piperazine-1-ium cation was chosen because the reactions of piperazine with electrophilic reagents in different solvents at usual temperatures were not chemoselective and provide mixtures, e.g., I, comprising 1-substituted, 1,4-disubstituted and unsubstituted piperazine as well. It was found that for in situ generating of starting piperazine-1-ium cation from piperazine the application of acetic acid as reaction medium or the chemisorption of piperazine on weakly acidic cation exchanger resin were highly acceptable in terms of both reaction times and yields. The usage of resin supported piperazine-1-ium cation in reaction with carboxylic anhydrides or nitrourea is an example of the solid phase synthesis with ionically bonded substrate. Furthermore, synthesis in acetic acid medium were effectively catalyzed by Cu+, Cu2+ or Al3+ ions supported on weakly acidic cation-exchanger resin as well. Finally, it was observed that application of the solid support metal catalysis afforded target products in shortened reaction times and in 82-95% yields. The experimental part of the paper was very detailed, including the reaction process of 1-(Phenylsulfonyl)piperazine hydrochloride(cas: 412293-98-2Electric Literature of C10H15ClN2O2S)

1-(Phenylsulfonyl)piperazine hydrochloride(cas: 412293-98-2) belongs to piperazines. 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).Electric Literature of C10H15ClN2O2S

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

《Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning》 was written by Stewart, Andrew O.; Cowart, Marlon D.; Moreland, Robert B.; Latshaw, Steve P.; Matulenko, Mark A.; Bhatia, Pramila A.; Wang, Xueqing; Daanen, Jerome F.; Nelson, Sherry L.; Terranova, Marc A.; Namovic, Marian T.; Donnelly-Roberts, Diana L.; Miller, Loan N.; Nakane, Masaki; Sullivan, James P.; Brioni, Jorge D.. Category: piperazines And the article was included in Journal of Medicinal Chemistry on April 22 ,2004. The article conveys some information:

A series of subtype selective dopamine D4 receptor ligands from the heteroarylmethylphenylpiperazine class have been discovered that exhibit a remarkable structure-activity relation (SAR), revealing a substituent effect in which regiosubstitution on the terminal arylpiperazine ring can modulate functional or intrinsic activity. Other structure-dependent efficacy studies in the dopamine D4 field have suggested a critical interaction of the heteroarylmethyl moiety with specific protein microdomains in controlling intrinsic activity. The authors studies indicate that for some binding orientations, the phenylpiperazine moiety also plays a key role in determining efficacy. These data also implicate a kinetic or efficiency term, contained within measured functional affinities for agonists, which support a sequential binding and conformational stabilization model for receptor activation. The structural similarity between partial agonist and antagonist, within this subset of ligands, and lack of bioisosterism for this substituent effect are key phenomena for these hypotheses. In the experimental materials used by the author, we found Abt-724(cas: 70006-24-5Category: piperazines)

Abt-724(cas: 70006-24-5) belongs to piperazines. 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).Category: piperazines

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