Category: 109-01-3

《Synthesis and Molecular Docking Study of New Thiazole Derivatives as Potential Tubulin Polymerization Inhibitors》 was written by El-Abd, Azhar O.; Bayomi, Said M.; El-Damasy, Ashraf K.; Mansour, Basem; Abdel-Aziz, Naglaa I.; El-Sherbeny, Magda A.. Application of 109-01-3This research focused ontrimethoxyphenylthiazole preparation antitumor SAR tubulin polymerization inhibition mol docking. The article conveys some information:

A new series of 2,4-disubstituted thiazole derivatives I [R = 2-chloroacetyl, 2-(butylamino)acetyl, 2-piperazin-1-ylacetyl, etc.] containing 4-(3,4,5-trimethoxyphenyl) moiety was synthesized and evaluated for their potential anticancer activity as tubulin polymerization inhibitors. All designed compounds I were screened for cytotoxic activity against four human cancer cell lines, namely, HepG2, MCF-7, HCT116, and HeLa, using 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay, with combretastatin A-4 as a reference drug. Compounds I [R = 2-(isopropylamino)acetyl, 2-[4-(4-fluorophenyl)piperazin-1-yl]acetyl, 2-(4-nitroanilino)acetyl, 2-hydrazinoacetyl, 2-[(2Z)-2-(5-chloro-2-oxo-indolin-3-ylidene)hydrazino]acetyl, 2-[(2Z)-2-(5-methyl-2-oxo-indolin-3-ylidene)hydrazino]acetyl] showed superior activity against the tested cell lines, with IC50 values ranging from 3.35 ± 0.2 to 18.69 ± 0.9 μM. Further investigation for the most active cytotoxic agents as tubulin polymerization inhibitors was also performed in order to explore the mechanism of their antiproliferative activity. The obtained results suggested that compounds I [R = 2-(isopropylamino)acetyl, 2-(4-nitroanilino)acetyl, 2-[(2Z)-2-(5-chloro-2-oxo-indolin-3-ylidene)hydrazino]acetyl] remarkably inhibit tubulin polymerization, with IC50 values of 2.95 ± 0.18, 2.00 ± 0.12, and 2.38 ± 0.14 μM, resp., which exceeded that of the reference drug combretastatin A-4 (IC50 2.96 ± 0.18 μM). Mol. docking studies were also conducted to investigate the possible binding interactions between the targeted compounds and the tubulin active site. The interpretation of the results showed clearly that compounds I [R = 2-(4-nitroanilino)acetyl, 2-[(2Z)-2-(5-chloro-2-oxo-indolin-3-ylidene)hydrazino]acetyl] were identified as the most potent tubulin polymerization inhibitors with promising cytotoxic activity and excellent binding mode in the docking study. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Application 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..Application of 109-01-3

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

Recommanded Product: 109-01-3In 2020 ,《One-pot multicomponent synthesis and bioevaluation of tetrahydroquinoline derivatives as potential antioxidants, a-amylase enzyme inhibitors, anti-cancerous and anti-inflammatory agents》 was published in Molecules. The article was written by Farooq, Samra; Mazhar, Aqsa; Ghouri, Areej; Ihsan-Ul-Haq; Ullah, Naseem. The article contains the following contents:

Mankind has always suffered from multiple diseases. Therefore, there has been a rigorous need in the field of medicinal chem. for the design and discovery of new and potent mol. entities. In this work, thirteen tetrahydroquinoline derivatives were synthesized and evaluated biol. for their antioxidant, a-amylase enzyme inhibitory, anti-proliferative and anti-inflammatory activities. SF8 showed the lowest IC50 of 29.19 ± 0.25 microg/mL by scavenging DPPH free radicals. SF5 showed significant antioxidant activity in total antioxidant capacity (TAC) and total reducing power (TRP) assays. SF5 and SF9 showed the maximum inhibition of a-amylase enzyme i.e., 97.47% and 89.93%, resp., at 200 microg/mL concentration Five compounds were shortlisted to determine their anti-proliferative potential against Hep-2C cells. The study was conducted for 24, 48 and 72 h. SF8 showed significant results, having an IC50 value of 11.9 ± 1.04 microM at 72 h when compared with standard cisplatin (IC50 value of 14.6 ± 1.01 microM). An in vitro nitric oxide (NO) assay was performed to select compounds for in vivo anti-inflammatory activity evaluation. SF13 scavenged the NO level to a maximum of 85% at 50 microM concentration, followed by SF1 and SF2. Based on the NO scavenging assay results, in vivo anti-inflammatory studies were also performed and the results showed significant activity compared to the standard, acetylsalicylic acid (ASA). In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 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..Recommanded Product: 109-01-3

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

Jiang, Feng; Gao, Donghui; Feng, Xi; Pan, Jiaming; Pu, Wanfen published an article in 2021. The article was titled 《W/O high internal phase emulsions (HIPEs) stabilized by a piperazinyl based emulsifier》, and you may find the article in Soft Matter.Recommanded Product: 1-Methylpiperazine The information in the text is summarized as follows:

In this study, a piperazinyl-based emulsifier (EA/AMPA) was synthesized to prepare water-in-oil (W/O) high internal phase emulsions (HIPEs). Using kerosene as the oil phase, stable HIPEs with internal phase fractions of up to 98% were prepared This enabled the EA/AMPA to have a high efficiency, as the HIPEs with a 90% internal phase fraction could be easily prepared with 0.1% of EA/AMPA. In addition, the formation of HIPEs was not affected by the addition of Na+. Because of the fact that EA/AMPA has a hydrophilic head with two tertiary amines, EA/AMPA could be easily recovered from the oil phase by adjusting the pH to acidic values. Moreover, the unique structure promoted the formation of stable HIPEs, even with crude oil used as the oil phase. The results indicate that EA/AMPA has the potential to significantly contribute to the preparation of W/O HIPEs and that the design of the hydrophilic head with two tertiary amines can provide a reference for the fabrication of new W/O emulsifiers. 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

《Wormlike micelles with a unique ladder shape formed by a C22-tailed zwitterionic surfactant bearing a bulky piperazine group》 was written by Han, Yugui; Wang, Yefei; Meng, Xianghai; Wang, Qiuxia; Han, Xiaodong. Application In Synthesis of 1-MethylpiperazineThis research focused onzwitterionic surfactant wormlike micelle zero shear viscosity surface tension. The article conveys some information:

Wormlike micelles (WLMs) have been successfully constructed from many different C22-tailed surfactants. Here, we creatively introduced a bulky piperazine group onto a C22-tailed zwitterionic surfactant, N-erucamidopropyl-N,N-piperazine-N-Me ammonium propanesulfonate (EDPS), and investigated the micellar structure and properties of the EDPS WLMs via mol. dynamics simulation, cryo-TEM and rheol. techniques. It was found that 25 mM EDPS increased the zero-shear viscosity to as high as ~106 mPa s. Furthermore, abnormal rheol. behaviors, such as an inflection in the shear thinning region of steady rheol. and an abrupt decrease of the shear stress at a critical shear rate, were observed, which was attributed to the unique ladder shape micellar structure. The EDPS WLMs were superior to other C22-tailed surfactants in many aspects, such as a low overlapping concentration, higher viscosity, stable viscosity over the whole pH range, and great temperature and salt (NaCl, CaCl2 and MgCl2) tolerance. In the part of experimental materials, we found many familiar compounds, such as 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

《Design, synthesis and biological evaluation of novel pleuromutilin derivatives containing piperazine and 1,2,3-triazole linker》 was written by Zhang, Guang-Yu; Zhang, Zhe; Li, Kang; Liu, Jie; Li, Bo; Jin, Zhen; Liu, Ya-Hong; Tang, You-Zhi. HPLC of Formula: 109-01-3 And the article was included in Bioorganic Chemistry in 2020. The article conveys some information:

A series of novel pleuromutilin derivatives containing piperazine ring, 1,2,3-triazoles and secondary amines on side chain of C14 e.g., I were synthesized under mild conditions via click reaction. The in vitro antibacterial activities of synthesized derivatives against four strains of Staphylococcus aureus (MRSA ATCC 43300, ATCC 29213,144 and AD3) and one strain of Escherichia coli (ATCC 25922) were evaluated by broth dilution method. Among these derivatives, 22-[2-(4-((4-nitrophenyl piperazine)methyl)-1,2,3-triazol-1-yl)-1-(piperazine-1-yl) ethyl-1-one] deoxy pleuromutilin I showed most prominent in vitro antibacterial effect against MRSA (MIC = 1μg/mL). Furthermore, compound I displayed more rapid bactericidal kinetic than tiamulin time-kill studies and possessed a longer PAE than tiamulin against MRSA in vitro. In addition, in vivo antibacterial activities of compound I against MRSA were further evaluated employing thigh infection model. And compound I (-8.89 log10 CFU/mL) displayed superior activities than tiamulin. Compound I was further evaluated in CYP450 inhibition assay and the results showed that it exhibited low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6 and CYP3A4 enzymes. The PK properties of compound I were then measured. The half-life (t1/2), clearance rate (Cl) and area under the plasma concentration time curve (AUC0→∞) of compound I were 0.74 h, 0.29 L/h/kg and 46.28μg·h/mL, resp.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

In 2022,Chen, Xiao-Xian; Liu, De-Xuan; Gong, Ya-Ping; Wang, Sha-Sha; Zhang, Wei-Xiong; Chen, Xiao-Ming published an article in Inorganic Chemistry. The title of the article was 《Above-Room-Temperature Ferroelastic Phase Transitions in Two Tetrafluoroborate-Based Hexagonal Molecular Perovskites》.Name: 1-Methylpiperazine The author mentioned the following in the article:

ABX3-type mol. perovskites provide an important platform to tune phase transitions, via judiciously choosing A-, B-, and X-site components, to approach advanced functional materials for applications. Although tetrafluoroborate can act as X-site component to assemble ten instances of ABX3 mol. perovskites, only two of them possess hexagonal perovskite structures. Herein, we report two tetrafluoroborate-based hexagonal mol. perovskites, A[Na(BF4)3], by judiciously choosing two different A-site cations: 1-methyl-1,4-diazabicyclo[2.2.2]octane-1,4-diium (Hmdabco2+) for 1 and 1-methylpiperazine-1,4-diium (H2mpz2+) for 2. They have high-temperature phases in the same space group (P63/mmc) revealing highly disordered A-site cations. Upon cooling, 1 undergoes two-step P63/mmc ↔ P3̅c1 ↔ P21/n transitions at 344 and 338 K, resp., including a ferroelastic one (3̅mF2/m) accompanied by a spontaneous strain of 0.013. In contrast, the smaller H2mpz2+ cation with more adoptable conformations induces a one-step sharp P63/mmc ↔ P21/c ferroelastic transition (6/mmmF2/m(s)) at 418 K in 2, leading to more significant symmetry breaking and a considerable spontaneous strain of 0.129. This study provides important clues to modulate structural phase transitions by tuning diverse components for the multicomponent dense hybrid crystals. In the experiment, the researchers used many compounds, for example, 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

In 2022,Prabha, Kolandaivel; Satheeshkumar, Rajendran; Nasif, Vesim; Saranya, Jayapalan; Sayin, Koray; Natarajan, Jeyakumar; Chandrasekar, Chinnarasu; Rajendra Prasad, K. J. published an article in ChemistrySelect. The title of the article was 《Synthesis, In Vitro Cytotoxicity, and DFT Studies of Novel 2-Amino Substituted Benzonaphthyridines as PDK1 Inhibitors》.Product Details of 109-01-3 The author mentioned the following in the article:

The present work emphasizes the utility of 2,4-dichloro-5-methylbenzo[h][1,6]naphthyridine as starting precursors. The reaction of 2,4-dichloro-5-methylbenzo[h][1,6]naphthyridine with a variety of aliphatic and aromatic amines yielded 2-amino substituted 2,4-dichlorobenzo[h]naphthyridines. All the compounds were examined for their in vitro anticancer activity against six human cancer lines and docked with PDK1 inhibitors. The structure-activity relationship studies are revealed that the compounds holding aminocarbazole moiety and triazole amine moiety improve the activity profile. All the structures of synthesized compounds were optimized at B3LYP-D3/6-31G(d) level in the water. Furthermore, the electronic properties and biol. reactivity of the synthesized compounds are explored using computational techniques. In the experiment, the researchers used many compounds, for example, 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

《Long-term exposure of activated sludge in chemostats leads to changes in microbial communities composition and enhanced biodegradation of 4-chloroaniline and N-methylpiperazine》 was published in Chemosphere in 2020. These research results belong to Poursat, Baptiste A. J.; van Spanning, Rob J. M.; Braster, Martin; Helmus, Rick; de Voogt, Pim; Parsons, John R.. Recommanded Product: 1-Methylpiperazine The article mentions the following:

Exposure history and adaptation of the inoculum to chems. have been shown to influence the outcome of ready biodegradability tests. However, there is a lack of information about the mechanisms involved in microbial adaptation and the implication thereof for the tests. In the present study, we investigated the impact of a long-term exposure to N-methylpiperazine (NMP) and 4-chloroaniline (4CA) of an activated sludge microbial community using chemostat systems. The objective was to characterize the influence of adaptation to the chems. on an enhanced biodegradation testing, following the OECD 310 guideline. Cultures were used to inoculate the enhanced biodegradability tests, in batch, before and after exposure to each chem. independently in chemostat culture. Composition and diversity of the microbial communities were characterized by 16s rRNA gene amplicon sequencing. Using freshly sampled activated sludge, NMP was not degraded within the 28 d frame of the test while 4CA was completely eliminated. However, after one month of exposure, the community exposed to NMP was adapted and could completely degrade it. This result was in complete contrast with that from the culture exposed for 3 mo to 4CA. Long term incubation in the chemostat system led to a progressive loss of the initial biodegradation capacity of the community, as a consequence of the loss of key degrading microorganisms. This study highlights the potential of chemostat systems to induce adaptation to a specific chem., ultimately resulting in its biodegradation At the same time, one should be critical of these observations as the dynamics of a microbial community are difficult to maintain in chemostat, as the loss of 4CA biodegradation capacity demonstrates. 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

《Rediscovering aminal chemistry: copper(II) catalysed formation under mild conditions》 was published in Green Chemistry in 2020. These research results belong to Pereira, Juliana G.; Antonio, Joao P. M.; Mendonca, Ricardo; Gomes, Rafael F. A.; Afonso, Carlos A. M.. Synthetic Route of C5H12N2 The article mentions the following:

An efficient and mild methodol. for the preparation of aminals from aromatic aldehydes, including furanic platforms was studied. These mild conditions allowed ease of access to a plethora of aminals and as such we set out explored previously unaccessible potential applications. By studying the stability of various aminals, we were able to develop a simple aldehyde protecting group based on a com. diamine which was deprotected under mind conditions. We developed a protocol for the scavenging of genotoxic aldehydes by taking advantage of our methodol. and a diamine resin, as well as early studied on the development of a stimuli-responsive release system using a salycil aldehyde derived aminal. The results came from multiple reactions, including the reaction of 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

In 2019,Nucleic Acids Research included an article by Hu, Ming-Hao; Wu, Tian-Ying; Huang, Qiong; Jin, Guangyi. Synthetic Route of C5H12N2. The article was titled 《New substituted quinoxalines inhibit triple-negative breast cancer by specifically downregulating the c-MYC transcription》. The information in the text is summarized as follows:

Conventional chemotherapy remains the primary treatment option for triple-neg. breast cancer (TNBC). However, the current chemotherapeutic drugs have limited effects on TNBC, and often lead to serious side effects as well as drug resistance. Thus, more effective therapeutic options are sorely needed. As c-MYC oncogene is highly expressed during TNBC pathogenesis, inhibiting c-MYC expression would be an alternative anti-TNBC strategy. In this study, we designed and synthesized a serial of quinoxaline analogs that target c-MYC promoter G-quadruplex (G4), which is believed to be a repressor of c-MYC transcription. Among them, a difluoro-substituted quinoxaline QN-1(I) was identified as the most promising G4-stabilizing ligand with high selectivity to c-MYC G4 over other G4s, which is distinguished from many other reported ligands. Intracellular studies indicated that QN-1 induced cell cycle arrest and apoptosis, repressed metastasis and inhibited TNBC cell growth, primarily due to the downregulation of c-MYC transcription by a G4-dependent mechanism. Notably, inhibition by QN-1 was significantly greater for c-MYC than other G4-driven genes. Cancer cells with c-MYC overexpression were more sensitive to QN-1, relative to normal cells. Furthermore, QN-1 effectively suppressed tumor growth in a TNBC mouse model. Accordingly, this work provides an alternative strategy for treating TNBC. In the part of experimental materials, we found many familiar compounds, such as 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