Tag: 200-300

On April 12, 2018, Crew, Andrew P.; Hornberger, Keith R.; Snyder, Lawrence B.; Zimmermann, Kurt; Wang, Jing; Berlin, Michael; Crews, Craig M.; Dong, Hanqing published a patent.Category: piperazines The title of the patent was Preparation of bifunctional compounds for the targeted degradation of androgen receptor. And the patent contained the following:

The invention relates to bifunctional compounds, which find utility to degrade and (inhibit) androgen receptor. In particular, the invention is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds androgen receptor, such that androgen receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of androgen receptor. The invention exhibits a broad range of pharmacol. activities associated with compounds according to the present invention, consistent with the degradation/inhibition of androgen receptor (data given). The invention compounds are claimed to be useful for the treatment of cancer or Kennedy’s disease, or both. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Category: piperazines

The Article related to protac modulator preparation targeted ubiquitination androgen receptor degradation inhibition, preparation bifunctional compound degradation androgen receptor, treatment cancer kennedy disease preparation bifunctional compound and other aspects.Category: piperazines

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

In 2016,Lab on a Chip included an article by Jang, Sungho; Lee, Byungjin; Jeong, Heon-Ho; Jin, Si Hyung; Jang, Sungyeon; Kim, Seong Gyeong; Jung, Gyoo Yeol; Lee, Chang-Soo. Category: piperazines. The article was titled 《On-chip analysis, indexing and screening for chemical producing bacteria in a microfluidic static droplet array》. The information in the text is summarized as follows:

Economic production of chems. from microbes necessitates development of high-producing strains and an efficient screening technol. is crucial to maximize the effect of the most popular strain improvement method, the combinatorial approach. However, high-throughput screening has been limited for assessment of diverse intracellular metabolites at the single-cell level. Herein, we established a screening platform that couples a microfluidic static droplet array (SDA) and an artificial riboswitch to analyze intracellular metabolite concentration from single microbial cells. Using this system, we entrapped single Escherichia coli cells in SDA to measure intracellular L-tryptophan concentrations It was validated that intracellular L-tryptophan concentration can be evaluated by the fluorescence from the riboswitch. Moreover, high-producing strains were successfully screened from a mutagenized library, exhibiting up to 145% productivity compared to its parental strain. This platform will be widely applicable to strain improvement for diverse metabolites by developing new artificial riboswitches.4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Category: piperazines) was used in this study.

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Category: piperazines

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

COA of Formula: C11H17ClN4OOn May 16, 2019 ,《Synthesis of N-pyrimidin[1,3,4]oxadiazoles and N-pyrimidin[1,3,4]-thiadiazoles from 1,3,4-oxadiazol-2-amines and 1,3,4-thiadiazol-2-amines via Pd-catalyzed heteroarylamination》 appeared in Tetrahedron Letters. The author of the article were Yan, Longjia; Deng, Minggao; Chen, Anchao; Li, Yongliang; Zhang, Wanzheng; Du, Zhi-yun; Dong, Chang-zhi; Meunier, Bernard; Chen, Huixiong. The article conveys some information:

An efficient and practical procedure was developed to prepare various N-pyrimidin[1,3,4]oxadiazole I (R1 = Cl, Ph, N-methylpiperazinyl, etc.; R2 = Me, Ph, C(O)OCH2CH3, etc.; X = O) and thiadiazole scaffolds I (X = S) from 1,3,4-oxadiazol-2-amines II (X = O) and 1,3,4-thiadiazol-2-amines II (X = S) with chloropyrimidines III via Pd-catalyzed heteroarylamination using a Buchwald-type coupling. The products of this reaction are otherwise difficult to access and could be used as building blocks in drug design. After reading the article, we found that the author used 2-(4-(6-Chloro-2-methylpyrimidin-4-yl)piperazin-1-yl)ethanol(cas: 127116-19-2COA of Formula: C11H17ClN4O)

2-(4-(6-Chloro-2-methylpyrimidin-4-yl)piperazin-1-yl)ethanol(cas: 127116-19-2) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.COA of Formula: C11H17ClN4O

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

Nagata, Mao; Yokooji, Tomoharu; Nakai, Tomoe; Miura, Yumika; Tomita, Takashi; Taogoshi, Takanori; Sugimoto, Yumi; Matsuo, Hiroaki published their research in Scientific Reports on December 31 ,2019. The article was titled 《Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic beta cells》.Related Products of 70006-24-5 The article contains the following contents:

Clin. use of olanzapine frequently causes severe hyperglycemia as an adverse effect. In this study, we elucidated mechanisms by which olanzapine reduced insulin secretion using the hamster pancreatic beta cell line HIT-T15. Reverse transcriptional-PCR anal. revealed expression of dopamine (D2, D3 and D4), serotonin (5-HT2A, 5-HT2B, 5-HT2C, and 5-HT6), and histamine (H1 and H2) receptors in HIT-T15 cells. Olanzapine decreased insulin secretion from HIT-T15 cells at clin. relevant concentrations (64-160 nM). A dopamine D2 agonist, D3 antagonist, and D4 antagonist suppressed insulin secretion, whereas a D2 antagonist and D3 agonist increased it. A serotonin 5-HT2B agonist slightly increased insulin secretion, while a 5-HT2C antagonist slightly decreased it. Our results suggest that dopamine (D2, D3 and D4), serotonin (5-HT2B and 5-HT2C), and histamine (H1 and H2) receptors, which are expressed on pancreatic beta cells, directly modulate insulin secretion from pancreatic beta -cells. Thus, olanzapine may induce hyperglycemia in clin. settings by suppressing insulin secretion from beta cells through inhibition of dopamine D3, serotonin 5-HT2B and 5-HT2C, and histamine H1 receptors. In addition to this study using Abt-724, there are many other studies that have used Abt-724(cas: 70006-24-5Related Products of 70006-24-5) was used in this study.

Abt-724(cas: 70006-24-5) 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).Related Products of 70006-24-5

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

The author of 《Novel practical deprotection of N-Boc compounds using fluorinated alcohols》 were Choy, Jason; Jaime-Figueroa, Saul; Jiang, Laurence; Wagner, Paul. And the article was published in Synthetic Communications in 2008. Recommanded Product: 4-(Piperazin-1-yl)-1H-indole The author mentioned the following in the article:

The thermolytic deprotection of N-Boc compounds was accomplished using F3CCH2OH or (F3C)2CHOH as solvents. Even though the cleavage of the tert-butylcarbamate (Boc) group can be achieved at solvent reflux temperature, the deprotection process was significantly accelerated under microwave-assisted conditions. The practicality of this methodol. was demonstrated on alkyl, aryl, and heteroaromatic N-Boc-amines. In the experiment, the researchers used many compounds, for example, 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Recommanded Product: 4-(Piperazin-1-yl)-1H-indole)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) 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: 4-(Piperazin-1-yl)-1H-indole

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

SDS of cas: 84807-09-0On October 1, 2005 ,《Automated Microflow NMR: Routine Analysis of Five-Microliter Samples》 was published in Analytical Chemistry. The article was written by Jansma, Ariane; Chuan, Tiffany; Albrecht, Robert W.; Olson, Dean L.; Peck, Timothy L.; Geierstanger, Bernhard H.. The article contains the following contents:

A microflow CapNMR probe double-tuned for 1H and 13C was installed on a 400-MHz NMR spectrometer and interfaced to an automated liquid handler. Individual samples dissolved in DMSO-d6 are submitted for NMR anal. in vials containing as little as 10 μL of sample. Sets of samples are submitted in a low-volume 384-well plate. Of the 10 μL of sample per well, as with vials, 5 μL is injected into the microflow NMR probe for anal. For quality control of chem. libraries, 1D NMR spectra are acquired under full automation from 384-well plates on as many as 130 compounds within 24 h using 128 scans per spectrum and a sample-to-sample cycle time of ∼11 min. Because of the low volume requirements and high mass sensitivity of the microflow NMR system, 30 nmol of a typical small mol. is sufficient to obtain high-quality, well-resolved, 1D proton or 2D COSY NMR spectra in ∼6 or 20 min of data acquisition time per experiment, resp. Implementation of pulse programs with automated solvent peak identification and suppression allow for reliable data collection, even for samples submitted in fully protonated DMSO. The automated microflow NMR system is controlled and monitored using web-based software. The experimental process involved the reaction of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0SDS of cas: 84807-09-0)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.SDS of cas: 84807-09-0

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

《Identification of Aminoimidazole and Aminothiazole Derivatives as Src Family Kinase Inhibitors》 was written by Francini, Cinzia Maria; Fallacara, Anna Lucia; Artusi, Roberto; Mennuni, Laura; Calgani, Alessia; Angelucci, Adriano; Schenone, Silvia; Botta, Maurizio. Recommanded Product: 127116-19-2 And the article was included in ChemMedChem in 2015. The article conveys some information:

Src family kinases (SFKs) are a family of non-receptor tyrosine kinases (TKs) implicated in the regulation of many cellular processes. The aberrant activity of these TKs has been associated with the growth and progression of cancer. In particular, c-Src is overexpressed or hyperactivated in a variety of solid tumors and is most likely a strong promoting factor for the development of metastasis. Herein, the synthesis of new 4-aminoimidazole and 2-aminothiazole derivatives and their in vitro biol. evaluation are described for their potential use as SFK inhibitors. Initially, 2-aminothiazole analogs of dasatinib and 4-aminoimidazole derivatives were synthesized and tested against the SFKs Src, Fyn, Lyn, and Yes. Five hits were identified as the most promising compounds, with Ki values in the range of 90-480 nM. A combination of mol. docking, homol. modeling, and mol. dynamics were then used to investigate the possible binding mode of such compounds within the ATP binding site of the SFKs. Finally, the antiproliferative activities of the best candidates were evaluated against SH-SY5Y and K562 cell lines. Compound 3 b [2-(4-{2-methyl-6-[(5-phenylthiazol-2-yl)amino]pyrimidin-4-yl}piperazin-1-yl)ethanol] was found to be the most active inhibitor. After reading the article, we found that the author used 2-(4-(6-Chloro-2-methylpyrimidin-4-yl)piperazin-1-yl)ethanol(cas: 127116-19-2Recommanded Product: 127116-19-2)

2-(4-(6-Chloro-2-methylpyrimidin-4-yl)piperazin-1-yl)ethanol(cas: 127116-19-2) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Recommanded Product: 127116-19-2

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

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

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