Category: 109-01-3

In 2022,Wangngae, Sirilak; Chansaenpak, Kantapat; Weeranantanapan, Oratai; Piyanuch, Pornthip; Sumphanapai, Thitima; Yamabhai, Montarop; Noisa, Parinya; Lai, Rung-Yi; Kamkaew, Anyanee published an article in Scientific Reports. The title of the article was 《Effect of morpholine and charge distribution of cyanine dyes on cell internalization and cytotoxicity》.Application In Synthesis of 1-Methylpiperazine The author mentioned the following in the article:

To improve the potency of Heptamethine cyanines (Hcyanines) in cancer research, we designed and synthesized two novel Hcyanines based theranostic probes, IR794-Morph and IR794-Morph-Mpip, to enhance cancer cell internalization and targeting. In acidic conditions that resemble to tumor environment, both IR794 derivatives exhibited broad NIR absorption band (704-794 nm) and fluorescence emission (798-828 nm) that is suitable for deep seated tumor imaging. Moreover, in vitro study revealed that IR794-Morph-Mpip exhibited better cancer targetability towards various cancer cell lines under physiol. and slightly acidic conditions compared to normal cells. IR794-Morph-Mpip was fast internalized into the cancer cells within the first 5 min and mostly localized in lysosomes and mitochondria. In addition, the internalized signal was brighter when the cells were in the hypoxic environment. Furthermore, cellular uptake mechanism of both IR794 dyes, investigated via flow cytometry, revealed that endocytosis through OATPs receptors and clathrin-mediated endocytosis were the main routes. Moreover, IR794-Morph-Mpip, displayed anti-cancer activity towards all tested cancer cell types with IC50 below 7 μM (at 6 h incubation), which is approx. three times lower than that of the normal cells. Therefore, increasing protonated cites in tumor environment of Hcyanines together with incorporating morpholine in the mol. can enhance structure-inherent targeting of these dyes. The results came from multiple reactions, including the reaction of 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

Application In Synthesis of 1-MethylpiperazineIn 2020 ,《Design, synthesis, molecular docking and antiproliferative activity of some novel benzothiazole derivatives targeting EGFR/HER2 and TS》 was published in Bioorganic Chemistry. The article was written by Abdellatif, Khaled R. A.; Belal, Amany; El-Saadi, Mohamed T.; Amin, Noha H.; Said, Eman G.; Hemeda, Loah R.. The article contains the following contents:

A new series of benzothiazoles hybridized with a pyrimidine moiety, e.g., I (R = Cl), was designed and synthesized using the lead compound II (R1 = Ph). Various chem. modifications on the pyrimidine ring of II (R1 = Ph) at four different positions were done in a trial to get new multi-targeted anticancer agents. The structures of the newly synthesized compounds were established by their elemental analyses and spectral data. All final synthesized derivatives were submitted to the National Cancer Institute (NCI), USA, to be screened for their in vitro anticancer activity. Further evaluation for the cytotoxic activity of the most active compounds was performed using the MTT assay method. Compounds I [R = (4-acetylphenyl)amino, morpholin-4-yl, 4-methylpiperazin-1-yl], II (R1 = 4-oxo-4H-chromen-3-yl), and III were then selected for examination of their in vitro inhibitory activities against EGFR, HER2 and TS enzymes using lapatinib and 5FU as standards Furthermore, cell cycle anal. and apoptosis induction detection were also evaluated. Finally, mol. docking studies were carried out for compounds I [R = (4-acetylphenyl)amino, morpholin-4-yl, 4-methylpiperazin-1-yl], II (R1 = 4-oxo-4H-chromen-3-yl), and III to interpret their observed enzymic activities based on the ligand-protein interactions. The results came from multiple reactions, including the reaction of 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

In 2022,Ashworth, Ian W.; Frodsham, Lianne; Moore, Peter; Ronson, Thomas O. published an article in Journal of Organic Chemistry. The title of the article was 《Evidence of Rate Limiting Proton Transfer in an SNAr Aminolysis in Acetonitrile under Synthetically Relevant Conditions》.Application In Synthesis of 1-Methylpiperazine The author mentioned the following in the article:

An early synthetic step in the synthesis of adavosertib, AZD1775, is the SNAr reaction between 4-fluoronitrobenzene and 1-methylpiperazine in acetonitrile. A simple kinetics-based design of four reaction profiling experiments was used to investigate the kinetics of the reaction for the purpose of building a kinetic model. Fitting of the reaction profile data from two experiments conducted at 70°C with a different excess of 1-methylpiperazine showed the reaction to follow a third-order rate law with a second-order dependence upon 1-methylpiperazine. This was rationalized in terms of the reaction following a rate-limiting proton transfer mechanism (base catalyzed) in which the progress to product is driven by a proton transfer involving a second mol. of 1-methylpiperazine. The exptl. determined entropy of activation of -180 J K-1 is consistent with this mechanism. The formation of a low level impurity was found to be due to the presence of traces of piperazine in the 1-methylpiperazine, which was shown to react approx. 15 times faster than 1-methylpiperazine at 70°C. The rate constants for the 1-methylpiperazine catalyzed reaction of piperazine, 1-methylpiperazine, and the piperazine derived impurity were found to correlate in a Bronsted type anal. with the pKa’s (acetonitrile) of the amine nucleophile. In the experiment, the researchers used 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

《Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants》 was published in Bioorganic & Medicinal Chemistry in 2020. These research results belong to Zhu, Minglin; Li, Wei; Zhao, Tianming; Chen, Yuxiang; Li, Tong; Wei, Shangfei; Guo, Ming; Zhai, Xin. Related Products of 109-01-3 The article mentions the following:

The ALK and ROS1 dual inhibitors had capable of overcoming crizotinib-resistant mutants, two series of 2,4-diarylaminopyrimidine derivatives were designed, synthesized and evaluated for their in-vitro cytotoxic activity. The 2,4-diarylaminopyrimidine scaffold and derivatize the DAAP scaffold with sulfonyl and acrylamide moieties to extend the structure-activity relationship (SAR) study was retained. Some compounds exhibited excellent inhibitory activity with a double-digit nanomolar level in MTT assay. Four compounds were selected for enzymic assays further, the results led to the identification of a potent ALK and ROS1 dual inhibitor I [R = 4-ethylpiperazinyl], with IC50 values of 3.7 nM, 2.3 nM, 8.9 nM and 1.9 nM against ALK, ALKL1196M, ALKG1202R and ROS1, resp. Ultimately, the mol. docking studies on I [R = 4-ethylpiperazinyl] clearly disclosed reasonable and optimal binding interactions with ALK. In the experimental materials used by the author, we found 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

The author of 《Discovery of 4′-OH-flurbiprofen Mannich base derivatives as potential Alzheimer’s disease treatment with multiple inhibitory activities》 were Liu, Hongyan; Qiang, Xiaoming; Song, Qing; Li, Wei; He, Yuxi; Ye, Chanyuan; Tan, Zhenghuai; Deng, Yong. And the article was published in Bioorganic & Medicinal Chemistry in 2019. HPLC of Formula: 109-01-3 The author mentioned the following in the article:

A series of 4′-OH flurbiprofen Mannich base derivatives were designed, synthesized and evaluated as potential multifunctional agents for the treatment of Alzheimer’s disease. The biol. screening results indicated that most of these derivatives exhibited good multifunctional activities. Among them, compound 8n(I) demonstrated the best inhibitory effects on self-induced Aβ1-42 aggregation (65.03% at 25.0 μM). Moreover, this representative compound also exhibited good antioxidant activity, biometal chelating ability and anti-neuroinflammatory activity in vitro. Furthermore, I displayed appropriate blood-brain barrier permeability. These multifunctional properties highlight I as a promising candidate for further development of multi-functional drugs against AD.1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 109-01-3) 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..HPLC of Formula: 109-01-3

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

Wang, Xintong; Xiao, Haoran; Wang, Jing; Huang, Zongze; Peng, Geng; Xie, Wenjun; Bian, Xiling; Liu, Huijie; Shi, Cheng; Yang, Taoyi; Li, Xin; Gao, Jian; Meng, Ying; Jiang, Qianchen; Chen, Wei; Hu, Fang; Wei, Ningning; Wang, Xiaowei; Zhang, Liangren; Wang, KeWei; Sun, Qi published an article in 2021. The article was titled 《Synthesis and Biological Evaluation of Novel Triazine Derivatives as Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors》, and you may find the article in Journal of Medicinal Chemistry.Reference of 1-Methylpiperazine The information in the text is summarized as follows:

The design, synthesis, and evaluation of N-(4-(trifluoromethoxy)phenyl)-1,3,5-triazin-2-amine derivatives I [R = 4-Me, 4-F, 3,4-di-F, etc.], II [R1 = 4-Me, 4-MeO, 4-F3C, 4-F3CO, 3-F3CO; R2 = 4-F, 4-MeO, 4-Cl, etc.] and III [R3 = Me, methylamino, prop-1-ynyl, etc.] as a series of novel α7 nAChR pos. allosteric modulators (PAMs). The representative compound III [R3 = methylamino] functioned as a type I PAM with an EC50 of 3.0μM and approx. 38-fold enhancement of α7 current in the presence of agonist acetylcholine (100μM). It specifically enhanced α7 current with high selectivity. Compound III [R3 = methylamino] showed good pharmacokinetic property in mice. I.p. injection of III [R3 = methylamino] (3 mg/kg) exhibited sufficient blood-brain barrier penetration in mice. Furthermore, III [R3 = methylamino] were also rescued the auditory gating deficit in mice with schizophrenia-like behavior. Mol. docking of III [R3 = methylamino] with homopentameric α7 nAChR reveald a new mode of action. These results supported the potential of III [R3 = methylamino] for treatment for schizophrenia and Alzheimer’s disease. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Reference 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..Reference of 1-Methylpiperazine

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

《Nickel-Catalyzed Amination of (Hetero)aryl Halides Facilitated by a Catalytic Pyridinium Additive》 was published in Chemistry – A European Journal in 2020. These research results belong to Han, Dongyang; Li, Sasa; Xia, Siqi; Su, Mincong; Jin, Jian. Quality Control of 1-Methylpiperazine The article mentions the following:

An efficient and operationally simple Ni-catalyzed amination protocol has been developed. This methodol. features a simple NiII salt, an organic base and catalytic amounts of both a pyridinium additive and Zn metal. A diverse number of (hetero)aryl halides RX (R = 4-methanesulfonylphenyl, 3-cyanopyridin-2-yl, 1,3-benzoxazol-2-yl, etc.; X = Br, Cl) were coupled successfully with primary and secondary alkyl amines and anilines such as cyclohexanamine, pyrrolidine, 4-methylaniline, etc. in good to excellent yields RR1 [R1 = cyclohexylaminyl, pyrrolidin-1-yl, (4-methylphenyl)aminyl, etc.]. Similarly, benzophenone imine gave the corresponding N-arylation product N-(4-(methylsulfonyl)phenyl)-1,1-diphenylmethanimine in an excellent yield.1-Methylpiperazine(cas: 109-01-3Quality Control of 1-Methylpiperazine) 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..Quality Control of 1-Methylpiperazine

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

The author of 《Anticancer activities of novel Mannich bases against prostate cancer cells》 were Demirci, Serpil; Demirbas, Neslihan. And the article was published in Medicinal Chemistry Research in 2019. Product Details of 109-01-3 The author mentioned the following in the article:

This study was designed to synthesize hybridizing mols. starting from compound of 6-(4-phenyl-piperazin-1-yl)pyridine-3-ylamine by enhancing its biol. activity with other heterocycles and to determine anticancer activity of the resulting compounds To this end, 6-(4-phenylpiperazin-1-yl)pyridin-3-ylamine was used as the leading compound, which was known to exert anticancer activities. The synthesis of the leading compound was carried out using 1-(5-nitropyridin-2-yl)-4-phenylpiperazine which was obtained by a novel method with the reaction of N-phenylpiperazine and 2-chloro-5-nitropyridine. 6-(4-Phenylpiperazin-1-yl)pyridin-3-ylamine was converted to ester compound, an active intermediate compound, by substitution of one of the amine hydrogens with Et bromoacetate. The resulting ester product followed by the hydrazidation was added arylisocyanate to obtain the active intermediate. Then, by a series of substitution through cyclization and condensation reactions, thiazolidinone, 1,3,4-oxadiazole and 1,2,4-triazole were synthesized. Novel Mannich bases were obtained using oxazole and triazole hetero rings with primer or secondary amine compounds The characterization of the compounds was completed using FT IR, 1H-NMR, 13C-NMR, HRMS spectroscopic methods and elemental anal. technique. The chems., then, were tested for their anticancer activities against prostate cancer cell lines PC3 [ATCC, CRL-1435], LNCaP [ATCC, CRL-1740] and DU145 [ATCC, HTB-81]. The results revealed that the Mannich bases exhibited moderate cytotoxic activity against cancer cells tested. The experimental part of the paper was very detailed, including the reaction process of 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 《Turn-on fluorescent sensor for the detection of lipopolysaccharides based on a novel bispyrenyl terephtalaldehyde-bis-guanylhydrazone》 were Khownium, Kriangsak; Romsaiyud, Jariya; Borwornpinyo, Suparerk; Wongkrasant, Preedajit; Pongkorpsakol, Pawin; Muanprasat, Chatchai; Boekfa, Bundet; Vilaivan, Tirayut; Ruchirawat, Somsak; Limtrakul, Jumras. And the article was published in New Journal of Chemistry in 2019. Related Products of 109-01-3 The author mentioned the following in the article:

A novel bispyrene compound (BPTG) was developed as a selective lipopolysaccharide (LPS) sensor. The BPTG probe exhibited high selectivity and sensitivity toward LPS with a fluorescence ‘off-on’ behavior in HEPES-buffered DMSO-H2O (1 : 6 (volume/volume), HEPES = 10 mM, pH = 7.4) with a low detection limit of 5 nM. The turn-on fluorescence sensing of the LPS occurred through monomer and excimer emissions. The mechanism of the probe was supported by computational experiments and was found to be unique for its sandwich conformation and self-quenching ability at ground state prior to the binding to the LPS with a butterfly-like skeleton. Upon binding with LPS in an aqueous medium, the probe showed a dose-dependent increase in fluorescent emissions and exhibited a typical excimer emission peak at 485 nm along with a monomer emission peak at 375 nm. BPTG is highly selective for LPS over heparin and other anionic biol. species. Due to the expression of LPS on the cell surface of Gram neg. bacteria, BPTG was successfully applied as a fluorescent dye to visualize live Vibrio cholerae, which are life-threatening bacteria causing diarrheal disease. After reading the article, we found that the author used 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

SDS of cas: 109-01-3In 2021 ,《Synthesis and antimicrobial activity evaluation of some new 7-substituted quinolin-8-ol derivatives: POM analyses, docking, and identification of antibacterial pharmacophore sites》 appeared in Chemical Data Collections. The author of the article were Faydy, Mohamed El; Dahaieh, Naoufal; Ounine, Khadija; Rastija, Vesna; Almalki, Faisal; Jamalis, Joazaizulfazli; Zarrouk, Abdelkader; Hadda, Taibi Ben; Lakhrissi, Brahim. The article conveys some information:

Eight new 7-substituted quinolin-8-ol derivatives were synthesized in moderate to good yields through quinolin-8-ol, and secondary amines as the starting reagents. The antimicrobial activity of this new series of heterocyclic compounds has been achieved “”in vitro”” against some bacterial strains by means of the disk method, and most of the tested compounds have shown comparable or greater antibacterial activity than nitroxoline (standard antibiotic). It was very motivating to observe that POM (Petra/Osiris/Molinspiration) bioinformatic analyses of compound 7-[(4-methylpiperazin-1-yl)methyl]quinolin-8-ol exhibited better antibacterial activity (MIC = 10μg/mL against B. subtilis bacteria), and higher drug score (DS = 0.57) compared with Nitroxoline (DS = 0.47; MIC = 20μg/mL). Mol. docking investigations were also conducted to investigate the binding affinities as well as interactions of some compounds with the target proteins. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3SDS of cas: 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..SDS of cas: 109-01-3

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