Month: October 2022

Product Details of 939983-66-1On May 9, 2013 ,《Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Vu, Binh; Wovkulich, Peter; Pizzolato, Giacomo; Lovey, Allen; Ding, Qingjie; Jiang, Nan; Liu, Jin-Jun; Zhao, Chunlin; Glenn, Kelli; Wen, Yang; Tovar, Christian; Packman, Kathryn; Vassilev, Lyubomir; Graves, Bradford. The article conveys some information:

The p53 tumor suppressor is a potent transcription factor that plays a key role in the regulation of cellular responses to stress. It is controlled by its neg. regulator MDM2, which binds directly to p53 and inhibits its transcriptional activity. MDM2 also targets p53 for degradation by the proteasome. Many tumors produce high levels of MDM2, thereby impairing p53 function. Restoration of p53 activity by inhibiting the p53-MDM2 interaction may represent a novel approach to cancer treatment. RG7112 (2g) is the first clin. small-mol. MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. In cancer cells expressing wild-type p53, RG7112 stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts. In the experimental materials used by the author, we found 1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride(cas: 939983-66-1Product Details of 939983-66-1)

1-(3-(Methylsulfonyl)propyl)piperazine dihydrochloride(cas: 939983-66-1) is a member of sulfones.The sulfones, like the sulfonamides, are structural analogs of para-aminobenzoic acid that interfere with folic acid metabolism by acting as competitive inhibitors of dihydropteroate synthetase. All sulfones of clinical value are derivatives of dapsone, the most widely used member of this class.Product Details of 939983-66-1

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

In ,Physical Chemistry Chemical Physics included an article by Sauter, Eric; Nascimbeni, Giulia; Trefz, Daniel; Ludwigs, Sabine; Zojer, Egbert; von Wrochem, Florian; Zharnikov, Michael. Recommanded Product: 412293-98-2. The article was titled 《A dithiocarbamate anchoring group as a flexible platform for interface engineering》. The information in the text is summarized as follows:

The mol. organization and electronic properties of dithiocarbamate (DTC) anchored self-assembled monolayers (SAMs) linked to Au(111) substrates are studied by a combination of XPS, near-edge X-ray absorption fine structure (NEXAFS) spectroscopy, and state-of-the-art d. functional theory calculations For that, several piperidine/piperazine precursors with different architecture and substitution patterns are selected. The presented data show that the DTC anchor provides a useful building block for monomol. self-assembly on coinage metals with both sulfur atoms bonded to the substrate in a way similar to what is usually observed for the more commonly applied thiolate docking group. The combination of the DTC group with the quite flexible piperidine/piperazine cyclic linkers results in a dense mol. packing with an upright orientation of the terminal moieties. The latter comprise Ph rings bearing various substituents, which enables tuning the interfacial dipole over a wide range. Simulations on two prototypical DTC-docked SAMs help to better understand the exptl. observations and provide insight into the local origin of the SAM-induced shifts in the electrostatic energy. In particular, a comparison of measured and simulated XP spectra reveals the significant contribution of the DTC group to the interfacial dipole. In the experiment, the researchers used 1-(Phenylsulfonyl)piperazine hydrochloride(cas: 412293-98-2Recommanded Product: 412293-98-2)

1-(Phenylsulfonyl)piperazine hydrochloride(cas: 412293-98-2) 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).Recommanded Product: 412293-98-2

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

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

《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

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

《Synthesis and anthelmintic activity of 2-(N4-substituted-N1-piperazinyl)methyl-5-(or 6)-substituted benzimidazoles》 was written by Sule, D. P.; Shah, M. H.; Ghooi, Shaila; Bhide, M. B.. SDS of cas: 70006-24-5 And the article was included in Bulletin of Haffkine Institute on August 31 ,1978. The article conveys some information:

Sixteeen piperazinylmethylbenzimidazoles I (R = NO2, H; R1 = Me, CH2CH2OH, benzyl, Ph, p-ClC6H4, o-MeOC6H4, o-tolyl, 2-pyridyl, 2-thiazolyl) were prepared by reaction of the piperazine II with the resp. 2-chloromethylbenzimidazoles, which were prepared from 3,4-(H2N)2C6H3R and ClCH2CO2H. The majority of I showed anthelmintic activity >80% at 500 mg/kg as compared to Yomesan showing 100% activity at 500 mg/kg. I (R = NO2) were more active than I (R = H).Abt-724(cas: 70006-24-5SDS of cas: 70006-24-5) was used in this study.

Abt-724(cas: 70006-24-5) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.SDS of cas: 70006-24-5

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

《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

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