Category: 84807-09-0

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

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

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

HPLC of Formula: 84807-09-0On September 12, 2002 ,《Synthesis and Molecular Modeling of New 1-Aryl-3-[4-arylpiperazin-1-yl]-1-propane Derivatives with High Affinity at the Serotonin Transporter and at 5-HT1A Receptors》 was published in Journal of Medicinal Chemistry. The article was written by Orus, Lara; Perez-Silanes, Silvia; Oficialdegui, Ana-M.; Martinez-Esparza, Javier; Del Castillo, Juan-C.; Mourelle, Marisa; Langer, Thierry; Guccione, Salvatore; Donzella, Giuseppina; Krovat, Eva M.; Poptodorov, Konstantin; Lasheras, Berta; Ballaz, Santiago; Hervias, Isabel; Tordera, Rosa; Del Rio, Joaquin; Monge, Antonio. The article contains the following contents:

It has been proposed that 5-HT1A receptor antagonists augment the antidepressant efficacy of selective serotonin (5-HT) reuptake inhibitors. In a search toward new and efficient antidepressants, 1-(aryl)-3-[4-arylpiperazin-1-yl]-1-propane mol. hybrids were designed, synthesized, and evaluated for 5-HT reuptake inhibition and 5-HT1A receptor affinity. The design was based in coupling structural moieties related to inhibition of serotonin reuptake, such as benzo[b]thiophene derivatives to arylpiperazines, typical 5-HT1A receptor ligands. In binding studies, several compounds showed affinity at the 5-HT transporter and at 5-HT1A receptors. Mol. modeling studies predicted the pharmacophore elements required for high affinity binding and the features that enable to discriminate between agonist, partial agonist, or antagonist action at 5-HT1A receptors and 5-HT transporter inhibition. Solvent interactions in desolvation prior to the binding step along with enthalpy and entropy compensations might be responsible to explain agonist, partial agonist, and antagonist character. Hydrogen-bonding capability seems to be important to break hydrogen interhelical hydrogen bonds or alternatively to form other bonds upon ligand binding. Partial agonists and antagonists are unable to do this as the full agonist, which interacts closely by long-range forces or directly. The compounds showing the higher affinity at both the 5-HT transporter (Ki<50 nM) and the 5-HT1A receptors (Ki<20 nM) were further explored for their ability to stimulate [35S]GTPγS binding or to antagonize 8-hydroxy-2-di-n-propylamino-tetralin (8-OH-DPAT)-stimulated [35]GTPγS binding to rat hippocampal membranes, an index of agonist/antagonist action at 5-HT1A receptors, resp. Functional characterization was performed by measuring the antagonism to 8-OH-DPAT-induced hypothermia in mice. The experimental process involved the reaction of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0HPLC of Formula: 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.HPLC of Formula: 84807-09-0

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

Zhou, Dahui; Zhou, Ping; Evrard, Deborah A.; Meagher, Kristin; Webb, Michael; Harrison, Boyd L.; Huryn, Donna M.; Golembieski, Jeannette; Hornby, Geoffrey A.; Schechter, Lee E.; Smith, Deborah L.; Andree, Terrance H.; Mewshaw, Richard E. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Studies toward the discovery of the next generation of antidepressants. Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives》.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole The author mentioned the following in the article:

Based on the previously reported discovery lead, 3-(cis-4-(4-(1H-indol-4-yl)piperazin-1-yl)cyclohexyl)-5-fluoro-1H-indole (2), a series of related arylpiperazin-4-yl-cyclohexyl indole analogs were synthesized then evaluated as 5-HT transporter inhibitors and 5-HT1A receptor antagonists. The investigation of the structure-activity relationships revealed the optimal pharmacophoric elements required for activities in this series. The best example from this study (I) exhibited equal binding affinities at 5-HT transporter (Ki = 4.9 nM), 5-HT1A receptor (Ki = 6.2 nM) and functioned as a 5-HT1A receptor antagonist. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole)

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.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole

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

Application of 84807-09-0On May 9, 2013 ,《Biophysical Fragment Screening of the β1-Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design》 appeared in Journal of Medicinal Chemistry. The author of the article were Christopher, John A.; Brown, Jason; Dore, Andrew S.; Errey, James C.; Koglin, Markus; Marshall, Fiona H.; Myszka, David G.; Rich, Rebecca L.; Tate, Christopher G.; Tehan, Benjamin; Warne, Tony; Congreve, Miles. The article conveys some information:

Biophys. fragment screening of a thermostabilized β1-adrenergic receptor (β1AR) using surface plasmon resonance (SPR) enabled the identification of moderate affinity, high ligand efficiency (LE) arylpiperazine hits 7 and 8. Subsequent hit to lead follow-up confirmed the activity of the chemotype, and a structure-based design approach using protein-ligand crystal structures of the β1AR resulted in the identification of several fragments that bound with higher affinity, including indole 19 and quinoline 20. In the first example of GPCR crystallog. with ligands derived from fragment screening, structures of the stabilized β1AR complexed with 19 and 20 were determined at resolutions of 2.8 and 2.7 Å, resp. After reading the article, we found that the author used 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Application of 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.Application of 84807-09-0

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

Name: 4-(Piperazin-1-yl)-1H-indoleOn May 9, 2013 ,《Structure-Based Fragment Screening Is Demonstrated To Be a Practical Lead Discovery Method for a Representative G-Protein-Coupled Receptor》 appeared in Journal of Medicinal Chemistry. The author of the article were Stevens, Benjamin D.. The article conveys some information:

A review. In this paper the author discusses the work of Christopher et al. who described a successful approach leading to the discovery of structurally novel β1 adrenoreceptor ligands driven exclusively by biophys. methods. A work that highlights the promise of such technol. for utilization in future GPCR lead discovery programs andprovides an appealing alternative to traditional approaches forreceptors where structural stabilization is possible. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Name: 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).Name: 4-(Piperazin-1-yl)-1H-indole

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

Zajdel, Pawel; Kos, Tomasz; Marciniec, Krzysztof; Satala, Grzegorz; Canale, Vittorio; Kaminski, Krzysztof; Holuj, Malgorzata; Lenda, Tomasz; Koralewski, Robert; Bednarski, Marek; Nowinski, Leszek; Wojcikowski, Jacek; Daniel, Wladyslawa A.; Nikiforuk, Agnieszka; Nalepa, Irena; Chmielarz, Piotr; Kusmierczyk, Justyna; Bojarski, Andrzej J.; Popik, Piotr published an article on February 10 ,2018. The article was titled 《Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects》, and you may find the article in European Journal of Medicinal Chemistry.Quality Control of 4-(Piperazin-1-yl)-1H-indole The information in the text is summarized as follows:

Currently used antipsychotics are characterized by multireceptor mode of action. While antagonism of dopamine D2 receptors is responsible for the alleviation of “”pos.”” symptoms of schizophrenia and the effects at other, particularly serotonergic receptors are necessary for their addnl. therapeutic effects, there is no consensus regarding an “”ideal”” target engagement. Here, a detailed SAR anal. in a series of 45 novel azinesulfonamides of cyclic amine derivatives, involving the aryl-piperazine/piperidine pharmacophore, central alicyclic amine and azinesulfonamide groups has led to the selection of (S)-4-((2-(2-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)isoquinoline (62). The polypharmacol. profile of 62, characterized by partial 5-HT1AR agonism, 5-HT2A/5-HT7/D2/D3R antagonism, and blockade of SERT, reduced the “”pos.””-like, and “”neg.””-like symptoms of psychoses. Compound 62 produced no catalepsy, demonstrated a low hyperprolactinemia liability and displayed pro-cognitive effects in the novel object recognition task and attentional set-shifting test. While association of in vitro features with the promising in vivo profile of 62 is still not fully established, its clin. efficacy should be verified in further stages of development. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Quality Control of 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).Quality Control of 4-(Piperazin-1-yl)-1H-indole

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

Product Details of 84807-09-0On September 1, 2018 ,《Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Anglin, Justin; Zavareh, Reza Beheshti; Sander, Philipp N.; Haldar, Daniel; Mullarky, Edouard; Cantley, Lewis C.; Kimmelman, Alec C.; Lyssiotis, Costas A.; Lairson, Luke L.. The article contains the following contents:

Pancreatic ductal adenocarcinoma (PDAC) is a lethal malignancy that is extremely refractory to the therapeutic approaches that have been evaluated to date. Recently, it has been demonstrated that PDAC tumors are dependent upon a metabolic pathway involving aspartate aminotransferase 1, also known as glutamate-oxaloacetate transaminase 1 (GOT1), for the maintenance of redox homeostasis and sustained proliferation. As such, small mol. inhibitors targeting this metabolic pathway may provide a novel therapeutic approach for the treatment of this devastating disease. To this end, from a high throughput screen of ∼800,000 mols., 4-(1H-indol-4-yl)-N-phenylpiperazine-1-carboxamide was identified as an inhibitor of GOT1. Mouse pharmacokinetic studies revealed that potency, rather than inherent metabolic instability, would limit immediate cell- and rodent xenograft-based experiments aimed at validating this potential cancer metabolism-related target. Medicinal chem.-based optimization resulted in the identification of multiple derivatives with >10-fold improvements in potency, as well as the identification of a tryptamine-based series of GOT1 inhibitors.4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Product Details of 84807-09-0) 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.Product Details of 84807-09-0

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

Zhang, Bo-Sheng; Li, Yuke; Zhang, Zhe; An, Yang; Wen, Yu-Hua; Gou, Xue-Ya; Quan, Si-Qi; Wang, Xin-Gang; Liang, Yong-Min published an article in Journal of the American Chemical Society. The title of the article was 《Synthesis of C4-Aminated Indoles via a Catellani and Retro-Diels-Alder Strategy》.Category: piperazines The author mentioned the following in the article:

Highly functionalized 4-aminoindoles were synthesized via the three-component cross-coupling of o-iodoaniline, N-benzoyloxyamines, and norbornadiene. The Catellani and retro-Diels-Alder strategy was used in this domino process. o-Iodoaniline, with electron-donating and sterically hindered protecting groups, made the reaction selective toward o-C-H amination. On the basis of d. functional theory calculations, the intramol. Buchwald coupling of this reaction underwent a dearomatization and a 1,3-palladium migration process. The reasons for the control of the chem. selectivity by the protecting groups are given. Moreover, synthetic applications toward 4-piperazinylindole and a GOT1 inhibitor were realized. After reading the article, we found that the author used 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Category: piperazines)

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