Tag: 100-200

《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

Erol, Meryem; Celik, Ismail; Kuyucuklu, Gulcan published an article in 2021. The article was titled 《Synthesis, Molecular Docking, Molecular Dynamics, DFT and Antimicrobial Activity Studies of 5-substituted-2-(p-methylphenyl)benzoxazole Derivatives》, and you may find the article in Journal of Molecular Structure.Product Details of 109-01-3 The information in the text is summarized as follows:

In this study, new 2-(p-methylphenyl)-5-(2-substituted acetamido)benzoxazole derivatives I [X = N, O; R = H, Me, Meo] were synthesized and antimicrobial activities on six bacteria and their twelve drug-resistant isolates and one fungus and its two drug-resistant isolates were investigated by microdilution method. I [X = O; R = Me] against Staphylococcus aureus isolate and I [X = O; R = Me, MeO] against Escherichia coli isolate showed more potent antimicrobial activity with MIC value of 16μg/mL than some of the reference drugs. The compounds’ I interactions on the DNA gyrase enzyme were evaluated by mol. docking and mol. dynamics simulations. Docked compounds I have demonstrated superimposition in the DNA gyrase ATP binding site with similar protein-ligand interactions. With 50 ns duration mol. dynamics simulations, the average RMSD value of the DNA gyrase subunit B protein and I [X = N, O; R = H, Me, Meo] complexes were measured at about 0.15 nm. The ligands-bound DNA gyrase subunit B protein is a little less RMSF value and more stable than the apoprotein form between 45-49 residues in the active site amino acids region. Geometric optimization parameters, HOMO-LUMO orbital energies, and other electronic parameters derived from these energies, MEP, and NBO anal. were performed the DFT/B3LYP theory and 6-311G (d,p) basis set. The ΔE: LUMO-HOMO of the two most active compounds I [X = O; R = Me, MeO] were 4.2928 and 4.3219, resp. The compounds’ I predicted ADME profiles were in line with Lipinski and other limiting rules. In the part of experimental materials, we found many familiar compounds, such as 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

Cao, Yue; Zhou, Xiaoying; Luan, Lindong; Zeng, Hongmei; Zou, Guohong; Lin, Zhien published an article in 2021. The article was titled 《Organically templated metal phosphate-oxalates: Solvent-free synthesis, crystal structure, and proton conduction》, and you may find the article in Inorganic Chemistry Communications.COA of Formula: C5H12N2 The information in the text is summarized as follows:

Two new metal phosphate-oxalates, namely, H2api·Mn2(H2PO4)2(C2O4)2 (1) and H2mpip·Sc(H2PO4)2(C2O4)·0.5C2O4·1.5H2O (2), were prepared under solvent-free conditions, where api = 1-(3-aminopropyl)imidazole and mpip = 1-methylpiperazine. Compound 1 has a honeycomb-like structure with 12-ring windows. Compound 2 has a one-dimensional structure with scandium phosphate ladders decorated with oxalate ligands. The proton-conducting behaviors of this compound under 95% relative humidity were investigated. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3COA of Formula: 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..COA of Formula: C5H12N2

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

《Discovery of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great In Vivo Efficacy in a Mouse Lung Fibrosis Model》 was written by Lei, Hongrui; Guo, Ming; Li, Xiaopeng; Jia, Fang; Li, Changtao; Yang, Yu; Cao, Meng; Jiang, Nan; Ma, Enlong; Zhai, Xin. SDS of cas: 109-01-3 And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:

Autotaxin (ATX) is the dominant catalytic enzyme accounting for the lipid mediator lysophosphatidic acid (LPA) through hydrolysis of lysophosphatidylcholine (LPC). There is great interest in developing nonacidic ATX inhibitors with a specific binding mode to serve as potential in vivo effective therapeutic tools. Herein, dating from a high-throughput screening (HTS) product Indole-1 (740 nM), a dedicated optimization campaign was implemented through derivatizing the -COOH group to versatile linkers that well-bridged the indole skeleton and the hydrophobic pocket binding groups. Ultimately, it was established that the coexistence of a carbamate linker and -OH-group-containing amines could generally furnish excellent indole-based ATX inhibitors with even below 1 nM in vitro activities. Two optimal entities were advanced to a bleomycin-induced mice pulmonary fibrosis model, which exerted promising efficacy in alleviating the damaged lung texture caused by bleomycin exposure. The novel carbamate-containing indole-based ATX inhibitors with a concrete binding mode may contribute to the identification of potential therapeutic agents to intervene in fibrotic diseases. In the part of experimental materials, we found many familiar compounds, such as 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