Month: October 2022

Ouyang, Jia-Sheng; Liu, Siqi; Pan, Bendu; Zhang, Yaqi; Liang, Hao; Chen, Bin; He, Xiaobo; Chan, Wesley Ting Kwok; Chan, Albert S. C.; Sun, Tian-Yu; Wu, Yun-Dong; Qiu, Liqin published an article in 2021. The article was titled 《A Bulky and Electron-Rich N-Heterocyclic Carbene Palladium Complex (SIPr)Ph2Pd(cin)Cl: Highly Efficient and Versatile for Buchwald-Hartwig Amination of (Hetero)aryl Chlorides with (Hetero)aryl Amines at Room Temperature》, and you may find the article in ACS Catalysis.Name: 1-Methylpiperazine The information in the text is summarized as follows:

A bulky and electron-rich N-heterocyclic carbene palladium complex (SIPr)Ph2Pd(cin)Cl was synthesized and characterized. It was found to be highly efficient and versatile for the synthesis of substituted amines via coupling of different (hetero)aryl chlorides with various (hetero)aryl amines at room temperature, especially for the challenging amination of five- or six-membered ring heteroaryl chlorides with five- or six-membered ring heteroaryl amines. It was also successfully applied to the synthesis of various com. pharmaceuticals and candidate drugs or compounds with potential pharmacol. activities in high yields. All of these demonstrate its excellent catalytic efficacy in Buchwald-Hartwig amination and broad application prospects in relevant pharmaceutical preparations DFT calculations suggest that the steric-induced electronic interaction makes the ligand more electron-donating and the steric effect effectively regulates the rotation of iPr-Ph-iPr group in the catalyzed system due to the introduction of the di-Ph skeleton. Considering the electronic effect and steric effect together, the oxidative addition activation barriers by (SIPr)Ph2 and (SIPr) ligands are close to each other. The reductive elimination was the rate-determining step of (SIPr)Ph2Pd(cin)Cl-catalyzed system in the catalytic cycle, the appropriate steric hindrance of (SIPr)Ph2 ligand greatly reduces the energy barrier of this step. The perfect combination of electron-donating and steric hindrance ability of the ligand significantly improves the catalytic activity. In the part of experimental materials, we found many familiar compounds, such as 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

Product Details of 109-01-3In 2022 ,《Design and Synthesis of New Thiophene/Thieno[2,3-d]pyrimidines along with Their Cytotoxic Biological Evaluation as Tyrosine Kinase Inhibitors in Addition to Their Apoptotic and Autophagic Induction》 was published in Molecules. The article was written by Elmongy, Elshaymaa I.; Attallah, Nashwah G. M.; Altwaijry, Najla; AlKahtani, Manal Mubarak; Henidi, Hanan Ali. The article contains the following contents:

This work describes the synthesis and anticancer activity against kinase enzymes of newly designed thiophene and thieno[2,3-d]pyrimidines I [R = 2-(2-chloroacetyl)hydrazino, (3-methyl-2,5-dioxo-pyrrol-1-yl)amino, 2-[2-[(5-tert-butylisoxazol-3-yl)amino]acetyl]hydrazino, etc.] and II [R1 = Cl, (5-tert-butylisoxazol-3-yl)amino, (3-tert-butylisoxazol-5-yl)amino] along with their potential to activate autophagic and apoptotic cell death in cancer cells. The designed compounds were scanned for their affinity for kinases. The results were promising with affinity ranges from 46.7% to 13.3%. Mol. docking studies were performed, and the compounds were then screened for their antiproliferative effects. Interestingly, compounds I [R = 2-(2-chloroacetyl)hydrazino, (3-methyl-2,5-dioxo-pyrrol-1-yl)amino] resulted in higher cytotoxic effects than the reference standard against MCF-7 and HepG-2. The compounds were evaluated for their induction of apoptosis and/or necrosis on HT-29 and HepG-2. Three compounds induced significant early apoptosis compared to untreated control HT-29 cells, and four derivatives were more significant compared to untreated HepG-2 cells. Further investigated the effect of four compounds on the autophagy process within HT-29, HepG-2, and MCF-7 cells with flow cytometry. Similar to the apoptosis results, I [R = 2-(2-chloroacetyl)hydrazino] showed the highest autophagic induction among all compounds The potential inhibitory activity of the synthesized compounds on kinases was assessed. Screened compounds showed inhibition activity ranging from 41.4% to 83.5%. Compounds recorded significant inhibition were further investigated for their specific FLT3 kinase inhibitory activity. Noticeably, I [R = 2-(2-chloroacetyl)hydrazino] exhibited the highest inhibitory activity against FLT3. In the experimental materials used by the author, we found 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

The author of 《Antimicrotubular activity of 2-(4-methyl-1-piperazinylmethyl)acrylophenone dihydrochloride》 were Lesieur, I.; Delacourte, A.; Cazin, M.. And the article was published in Acta Therapeutica in 1984. Application In Synthesis of 1-Methylpiperazine dihydrochloride The author mentioned the following in the article:

The antimicrotubular activity of 3-(4-methyl-1-piperazinyl)propiophenone (I) [60868-01-1] was due to contamination of the synthetic product with 2-(4-methyl-1-piperazinylmethyl)acrylophenone (II) [91401-12-6]. Synthesis of I-2HCl [5470-92-8] and II-2HCl [91401-13-7] is described. Whereas I was devoid of any antimicrotubular activity, II, although less potent than colchicine, showed antimicrotubular activity. 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

The author of 《Anion exchange membranes with “”rigid-side-chain”” symmetric piperazinium structures for fuel cell exceeding 1.2 W cm-2 at 60°C》 were Gao, Li; Wang, Ying; Cui, Chunyu; Zheng, Wenji; Yan, Xiaoming; Zhang, Peng; Hu, Lei; Wu, Xuemei; Zhuang, Lin; He, Gaohong. And the article was published in Journal of Power Sources in 2019. Category: piperazines The author mentioned the following in the article:

Developing anion exchange membranes (AEMs) having high hydroxide conductivity, swelling resistance and excellent alk. stability is a challenge for fuel cells now. Herein, a universal and controllable approach of grafting rigid side chain is first proposed to construct connected ion transport nano-channels. A new route is also provided to prepare AEMs with stable sym. saturated heterocyclic ammonium. The rigid side chain is introduced onto poly(2,6-dimethyl-1,4-phenylene oxide) (PPO) by the Friedel-Crafts acylation with 4-fluorobenzoyl chloride and subsequent reaction between Ph fluoride and secondary amine of 1-methylpiperazine. Then the terminal piperazinium is produced by the reaction between tertiary amine of 1-methylpiperazine and Me iodide. Rigid branches expand free volume to construct connected ion transport nano-channels, leading to excellent conductivity (108 mS cm-1 at 60°C) that is higher than those of other reported sym. heterocyclic ammonium functionalized AEMs (33-89 mS cm-1 at 60°C). Due to the high conductivity, the H2/O2 cell employing this membrane achieves one of the highest peak power densities (1210 mW cm-2 at 2600 mA cm-2) so far. In addition, the IEC of the membrane remains constant after testing in 1 M NaOH at 60°C over 500 h.1-Methylpiperazine(cas: 109-01-3Category: piperazines) was used in this study.

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

《Design and synthesis of quinoxaline-1,3,4-oxadiazole hybrid derivatives as potent inhibitors of the anti-apoptotic Bcl-2 protein》 was written by Ono, Yukari; Ninomiya, Masayuki; Kaneko, Daiki; Sonawane, Amol D.; Udagawa, Taro; Tanaka, Kaori; Nishina, Atsuyoshi; Koketsu, Mamoru. Quality Control of 1-Methylpiperazine And the article was included in Bioorganic Chemistry in 2020. The article conveys some information:

A series of quinoxaline-1,3,4-oxadiazole hybrids I [R = chloro, Ph, 4-methylpiperazin-1-yl, 4-phenylpiperazin-1-yl, etc.; R1 = hydroxy, amino, 2-phenylethoxy, etc.] were synthesized and assessed for their anticancer potential on human leukemia HL-60 cells. Although these hybrids I exerted significant inhibition of HL-60 cell proliferation, they showed high cytotoxicity on human normal cells (WI-38). Utilizing information from mol. modeling of the hybrids I to the anti-apoptotic Bcl-2 protein, substructures including Ph, piperazine, piperidine and morpholine rings were added to their frameworks. The designed compounds I successfully induced apoptotic response on HL-60 cells with low toxicity on WI-38 cells. Furthermore, RT-PCR anal. demonstrated that these compounds I predominantly inhibited Bcl-2 expression. These findings highlight the great potential for the development of synthetic quinoxaline-1,3,4-oxadiazole hybrid derivatives as proapoptotic anticancer agents. In the experiment, the researchers used 1-Methylpiperazine(cas: 109-01-3Quality Control 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..Quality Control of 1-Methylpiperazine

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

《Synthesis, characterization, and in vivo pharmacological evaluation of novel Mannich bases derived from 1,2,4-triazole containing a naproxen moiety》 was written by Avci, Ahmet; Tasci, Hayrunnisa; Kandemir, Ummuhan; Can, Ozgur Devrim; Gokhan-Kelekci, Nesrin; Tozkoparan, Birsen. Synthetic Route of C5H12N2This research focused ontriazolethione regioselective preparation antinociceptive antiinflammatory mol docking; methoxynaphthylethylmercaptotriazole piperazine Mannich reaction; 1,2,4-Triazole-5-thione N-Mannich derivatives; Anti-inflammatory activity; Antinociceptive activity; Gastric toxicity; Mannich reaction; Naproxen analogs. The article conveys some information:

A new series of 1,2,4-triazole-5-thione Mannich derivatives I (R = Me, 4-fluorophenyl, 4-pyridyl, etc.) containing a naproxen moiety was designed and synthesized to create naproxen analogs, with the aim of developing novel anti-inflammatory/analgesic agents with improved safety profiles. Target compounds were synthesized using classical Mannich reaction (i.e. one-pot three component condensation reaction), by reacting 3-[1-(6-methoxy-2-naphtyl)ethyl]-5-mercapto-1,2,4-triazole, formaldehyde, and diverse secondary amines II in ethanol. Compounds were then evaluated for their potential antinociceptive and anti-inflammatory activities using some validated in vivo methods. Data obtained from acetic acid induced-writhing and carrageenan-induced paw edema tests revealed that all compounds induced peripherally-mediated antinociceptive activities, as well as notable anti-inflammatory effects. The results of hot-plate and tail-clip tests indicated that compounds I (R = Me, Et, 2-fluorophenyl, 4-fluorophenyl, 4-methylphenyl, 4-acetylphenyl) have also centrally-mediated antinociceptive activities in addition to their peripherally-mediated effects. Mol. docking studies were performed to investigate the putative binding modes of the interactions between all compounds and COX-1/COX-2 enzymes using AutoDock Vina software. Docking of the compounds into the COX-2 active site produced binding interactions that are essential for COX-2 inhibitory activity. None of the compounds in the serial, except for I (R = Boc and 4-acetylphenyl), induced significant gastrointestinal irritation. Overall, the results indicated that triazole Mannich bases bearing a naproxen moiety potentially represent a novel class of antinociceptive and anti-inflammatory agent with an improved gastric safety profile. In the experiment, the researchers used many compounds, for example, 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

Nagata, Mao; Yokooji, Tomoharu; Nakai, Tomoe; Miura, Yumika; Tomita, Takashi; Taogoshi, Takanori; Sugimoto, Yumi; Matsuo, Hiroaki published their research in Scientific Reports on December 31 ,2019. The article was titled 《Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic beta cells》.Related Products of 70006-24-5 The article contains the following contents:

Clin. use of olanzapine frequently causes severe hyperglycemia as an adverse effect. In this study, we elucidated mechanisms by which olanzapine reduced insulin secretion using the hamster pancreatic beta cell line HIT-T15. Reverse transcriptional-PCR anal. revealed expression of dopamine (D2, D3 and D4), serotonin (5-HT2A, 5-HT2B, 5-HT2C, and 5-HT6), and histamine (H1 and H2) receptors in HIT-T15 cells. Olanzapine decreased insulin secretion from HIT-T15 cells at clin. relevant concentrations (64-160 nM). A dopamine D2 agonist, D3 antagonist, and D4 antagonist suppressed insulin secretion, whereas a D2 antagonist and D3 agonist increased it. A serotonin 5-HT2B agonist slightly increased insulin secretion, while a 5-HT2C antagonist slightly decreased it. Our results suggest that dopamine (D2, D3 and D4), serotonin (5-HT2B and 5-HT2C), and histamine (H1 and H2) receptors, which are expressed on pancreatic beta cells, directly modulate insulin secretion from pancreatic beta -cells. Thus, olanzapine may induce hyperglycemia in clin. settings by suppressing insulin secretion from beta cells through inhibition of dopamine D3, serotonin 5-HT2B and 5-HT2C, and histamine H1 receptors. In addition to this study using Abt-724, there are many other studies that have used Abt-724(cas: 70006-24-5Related Products of 70006-24-5) was used in this study.

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).Related Products of 70006-24-5

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

The author of 《Development of a FRET-based ratiometric fluorescent probe to monitor the changes in palladium(II) in aqueous solution and living cells》 were Wang, Li; Ren, Mingguang; Li, Zihong; Dai, Lixuan; Lin, Weiying. And the article was published in New Journal of Chemistry in 2019. Formula: C5H12N2 The author mentioned the following in the article:

The enrichment of palladium ions in organisms can harm organisms to a great extent. It is necessary and critical to develop mol. tools that can ratiometrically image Pd2+ in living cells. Herein, we have developed a new FRET-based ratiometric fluorescent probe (CR-Pd, I) for the specific determination of Pd2+ in living cells. Moreover, fluorescence imaging shows that CR-Pd could be used as a probe for the ratiometric visualization of Pd2+ in mitochondria. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Formula: 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..Formula: C5H12N2

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

《Drug-like biimidazole derivatives dually target c-MYC/BCL-2 G-quadruplexes and inhibit acute myeloid leukemia》 was published in Bioorganic Chemistry in 2020. These research results belong to Hu, Ming-Hao; Yu, Bing-Ying; Wang, Xiaodong; Jin, Guangyi. Formula: C5H12N2 The article mentions the following:

Chemotherapy is the main approach for treating acute myeloid leukemia (AML). However, this therapy can cause severe side effects as well as drug resistance, hence calling for new therapeutic strategies. As c-MYC and BCL-2 are often overexpressed in AML, and synergism between c-MYC and BCL-2 promotes tumorigenesis, therefore, dual targeting of c-MYC/BCL-2 promoter G-quadruplexes (G4s) and then inhibiting the targeted gene expression would be a potential strategy in ALM treatment. In this work, in the search of dual ligands, we performed a screening assay with an inhouse, imidazole-based compound library. Consequently, two drug-like biimidazole derivatives were identified as selective c-MYC/BCL-2 G4 binders, of which, BIM-2 was selected as the candidate for inhibiting AML cell growth. Then, BIM-2 was demonstrated to downregulate both c-MYC and BCL-2 expression, and thereby cause cell cycle arrest at G0/G1 phase and apoptosis in AML cells. Furthermore, the possible end-stacking binding modes between BIM-2 and c-MYC/BCL-2 G4s were revealed by NMR and mol. docking studies. Accordingly, this study provides a new class of drug-like dual-selective c-MYC/BCL-2 G4 ligands for the potential treatment of AML. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Formula: 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..Formula: C5H12N2

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

《Metal-Free Molecular Perovskite High-Energetic Materials》 was written by Shang, Yu; Huang, Rui-Kang; Chen, Shao-Li; He, Chun-Ting; Yu, Zhi-Hong; Ye, Zi-Ming; Zhang, Wei-Xiong; Chen, Xiao-Ming. Quality Control of 1-Methylpiperazine And the article was included in Crystal Growth & Design in 2020. The article conveys some information:

Metal-free energetic materials generally have the advantages of high gas yield and metal-free residue after combustion or explosion, enabling them to be widely used as explosives and propellant components. As part of a series of our investigations on ABX3 mol. perovskite high-energetic materials, here we report five new metal-free members, (H2A)[NH4(ClO4)3], by using different organic cations H2A2+, i.e., 1-hydroxy-1,4-diazabicyclo[2.2.2]octane-1,4-diium for DAP-O4, piperazine-1,4-diium for PAP-4, 1-methyl-piperazine-1,4-diium for PAP-M4, homopiperazine-1,4-diium for PAP-H4, and 1-methyl-1,4-diazabicyclo-[2.2.2]octane-1,4-diium for DAP-M4, resp. Together with the previously reported member, (H2dabco)[NH4(ClO4)3] (DAP-4, H2dabco2+ = 1,4-diazabicyclo[2.2.2]octane-1,4-diium), these six metal-free mol. perovskite high-energetic materials provide nice instances to fine-tune the oxygen balance, crystal d., thermal stability, and detonation performance, by changing the A-site organic cations solely. The d. functional theory (DFT) calculations and the Kamlet-Jacob (K-J) equation suggested that improving the oxygen balance while keeping the spherical shape of the organic cations to match the anionic cage in these metal-free energetic materials facilitates obtaining a better detonation performance, providing an important clue for designing advanced practicable high-energetic materials. It is worth noting that three compounds (PAP-4, PAP-H4, and DAP-O4) are expected to exceed the performances of RDX as both explosive and propellant, in which DAP-O4 has the highest detonation heat (6.21 kJ mol-1), detonation velocity (8.900 km s-1), and detonation pressure (35.7 GPa), as well as a higher specific impulse value (262 s). The oxygen balance, d., thermal stability and detonation performance were fine-tuned by changing A-site organic fuel cations solely in six metal-free mol. perovskite high-energetic materials. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Quality Control 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..Quality Control of 1-Methylpiperazine

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