Tag: 100-200

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

Product Details of 109-01-3In 2020 ,《Discovery of 7H-pyrrolo[2,3-d]pyridine derivatives as potent FAK inhibitors: Design, synthesis, biological evaluation and molecular docking study》 appeared in Bioorganic Chemistry. The author of the article were Wang, Ruifeng; Zhao, Xiangxin; Yu, Sijia; Chen, Yixuan; Cui, Hengxian; Wu, Tianxiao; Hao, Chenzhou; Zhao, Dongmei; Cheng, Maosheng. The article conveys some information:

Focal adhesion kinase (FAK) is an intracellular non-receptor tyrosine kinase responsible for development of various tumor types. Aiming to explore new potent inhibitors, two series of 2,4-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives were designed and synthesized on the base of structure-based design strategy. Biol. evaluation indicated that most of these new compounds could potently inhibit FAK kinase, leading to the promising inhibitors against the proliferation of U-87MG, A-549, and MDA-MB-231 cancer cell lines. Among them, the optimized compound I potently inhibited the enzyme (IC50 = 19.1 nM) and displayed stronger potency than TAE-226 in U-87MG, A-549 and MDA-MB-231 cells, with IC50 values of 0.35, 0.24, and 0.34μM, resp. Compound I is a multi-target kinase inhibitor. Furthermore, compound I also exhibited relatively less cytotoxicity (IC50 = 3.72μM) toward a normal human cell line, HK2. According to the flow cytometry and wound healing assay results, compound I effectively induced apoptosis and G0/G1 phase arrest of MDA-MB-231 cells and suppressed the migration of U-87MG, A-549 and MDA-MB-231 cells. The docking study of compound I was performed to elucidate its possible binding modes and to provide a structural basis for the further structural guidance design of FAK inhibitors. Collectively, these data support the further development of compound I as a lead compound for FAK-targeted anticancer drug discovery.1-Methylpiperazine(cas: 109-01-3Product Details of 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..Product Details of 109-01-3

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

《A drug-like imidazole-benzothiazole conjugate inhibits malignant melanoma by stabilizing the c-MYC G-quadruplex》 was written by Wu, Tian-Ying; Huang, Qiong; Huang, Zhi-Shu; Hu, Ming-Hao; Tan, Jia-Heng. Product Details of 109-01-3 And the article was included in Bioorganic Chemistry in 2020. The article conveys some information:

Aberrant expression of c-MYC oncogene is significantly associated with the occurrence and development of malignant melanoma. Suppression of the c-MYC transcriptional activity accordingly provides a new idea for treating melanoma. Notably, stabilizing the G-quadruplex (G4) structure in the promoter is proved to be effective in downregulating c-MYC transcription. In this work, we developed a drug-like imidazole-benzothiazole conjugate called IZTZ-1, which was confirmed to preferentially stabilize the promoter G4 and thus lower c-MYC expression. Intracellular assays revealed that IZTZ-1 induced cell cycle arrest, apoptosis, thereby inhibiting cell proliferation. Furthermore, IZTZ-1 was demonstrated to effectively inhibit tumor growth in a melanoma mouse model. Consequently, IZTZ-1 showed good potential in the treatment of melanoma. This study provides an alternative strategy to treat melanoma by targeting the c-MYC G4. 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

The author of 《Electrooxidative Amination of sp2 C-H Bonds: Coupling of Amines with Aryl Amides via Copper Catalysis》 were Kathiravan, Subban; Suriyanarayanan, Subramanian; Nicholls, Ian A.. And the article was published in Organic Letters in 2019. Related Products of 109-01-3 The author mentioned the following in the article:

Metal-catalyzed cross-coupling reactions are among the most important transformations in organic synthesis. However, the use of C-H activation for sp2 C-N bond formation remains one of the major challenges in the field of cross-coupling chem. Described herein is the first example of the synergistic combination of copper catalysis and electrocatalysis for aryl C-H amination under mild reaction conditions in an atom-and step-economical manner with the liberation of H2 as the sole and benign byproduct. In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3Related Products of 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..Related Products of 109-01-3

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

In 2019,Bioorganic Chemistry included an article by Zhang, Xiaoyu; Song, Qing; Cao, Zhongcheng; Li, Yan; Tian, Chaoquan; Yang, Ziyi; Zhang, Heng; Deng, Yong. Recommanded Product: 109-01-3. The article was titled 《Design, synthesis and evaluation of chalcone Mannich base derivatives as multifunctional agents for the potential treatment of Alzheimer’s disease》. The information in the text is summarized as follows:

A series of chalcone Mannich base derivatives were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer’s disease based on the multi-target directed ligands design strategy. In vitro assays demonstrated that most of the derivatives exerted potent selective inhibitory potency on AChE with good multifunctional properties. Among them, representative compound 7c exhibited moderate inhibitory potency for EeAChE (IC50 = 0.44 μM) and MAO-B inhibition (IC50 = 1.21 μM), good inhibitory effect on self-induced Aβ1-42 aggregation (55.0%, at 25 μM), biometal chelating property, moderate antioxidant activity with a value 1.93-fold of Trolox. Moreover, both kinetic anal. of AChE inhibition and mol. modeling study revealed that 7c showed a mixed-type inhibition, binding simultaneously to CAS and PAS of AChE. In addition, 7c also displayed high BBB permeability. These properties indicated 7c may be a promising multifunctional agent for the treatment of AD. In the experimental materials used by the author, we found 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

Ozenil, Marius; Skos, Lukas; Roller, Alexander; Gajic, Natalie; Holzer, Wolfgang; Spreitzer, Helmut; Platzer-Ozenil, Sonja; Vraka, Chrysoula; Hacker, Marcus; Wadsak, Wolfgang; Pichler, Verena published an article in 2021. The article was titled 《Unexpected scaffold rearrangement product of pirenzepine found in commercial samples》, and you may find the article in Scientific Reports.Synthetic Route of C5H12N2 The information in the text is summarized as follows:

Pharmacovigilance aims at a better understanding of the mol. events triggered by medications to prevent adverse effects, which despite significant advances in our anal. repertoire plague the use of drugs until today. In this study, we find that clin. prescribed and com. available pirenzepine may not be the correct compound Pirenzepine can undergo an unexpected scaffold rearrangement from the pharmaceutical active ingredient (API) to a previously uncharacterized benzimidazole. The rearrangement occurs under highly acidic conditions, which were believed to favor the dihydrochloride formation of pirenzepine. The rearranged products of pirenzepine and the structurally related telenzepine have significantly decreased affinity for the muscarinic acetylcholine receptor, the pharmacol. target of these compounds Fortunately, in situ rearrangement after oral application is no safety issue, as we show that reaction kinetics in gastric acid prevent rearrangement. The research community should consider appropriate measures to perform reliable receiving inspections in the com. supply of well described and frequently used chems., in particular if experiments yield unexpected results. 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

《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