Month: October 2022

In 2022,Wangngae, Sirilak; Chansaenpak, Kantapat; Weeranantanapan, Oratai; Piyanuch, Pornthip; Sumphanapai, Thitima; Yamabhai, Montarop; Noisa, Parinya; Lai, Rung-Yi; Kamkaew, Anyanee published an article in Scientific Reports. The title of the article was 《Effect of morpholine and charge distribution of cyanine dyes on cell internalization and cytotoxicity》.Application In Synthesis of 1-Methylpiperazine The author mentioned the following in the article:

To improve the potency of Heptamethine cyanines (Hcyanines) in cancer research, we designed and synthesized two novel Hcyanines based theranostic probes, IR794-Morph and IR794-Morph-Mpip, to enhance cancer cell internalization and targeting. In acidic conditions that resemble to tumor environment, both IR794 derivatives exhibited broad NIR absorption band (704-794 nm) and fluorescence emission (798-828 nm) that is suitable for deep seated tumor imaging. Moreover, in vitro study revealed that IR794-Morph-Mpip exhibited better cancer targetability towards various cancer cell lines under physiol. and slightly acidic conditions compared to normal cells. IR794-Morph-Mpip was fast internalized into the cancer cells within the first 5 min and mostly localized in lysosomes and mitochondria. In addition, the internalized signal was brighter when the cells were in the hypoxic environment. Furthermore, cellular uptake mechanism of both IR794 dyes, investigated via flow cytometry, revealed that endocytosis through OATPs receptors and clathrin-mediated endocytosis were the main routes. Moreover, IR794-Morph-Mpip, displayed anti-cancer activity towards all tested cancer cell types with IC50 below 7 μM (at 6 h incubation), which is approx. three times lower than that of the normal cells. Therefore, increasing protonated cites in tumor environment of Hcyanines together with incorporating morpholine in the mol. can enhance structure-inherent targeting of these dyes. The results came from multiple reactions, including the reaction of 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

The author of 《New phenolic Mannich bases with piperazines and their bioactivities》 were Gul, Halise Inci; Tugrak, Mehtap; Gul, Mustafa; Mazlumoglu, Sertac; Sakagami, Hiroshi; Gulcin, Ilhami; Supuran, Claudiu T.. And the article was published in Bioorganic Chemistry in 2019. Safety of 1-Methylpiperazine The author mentioned the following in the article:

New Mannich bases, 2-(4-hydroxy-3-methoxy-5-((substituted piperazin-1-yl)methyl)benzylidene)-2,3-dihydro-1H-inden-1-ones I [R = Me, Ph, benzyl, etc.] were synthesized with the reaction of vanillin derived chalcone compound (2-(4-hydroxy-3-methoxybenzylidene)indan-1-one), paraformaldehyde and suitable amine in 1:1.2:1 mol ratios. Compounds I were evaluated in terms of cytotoxic/anticancer and CA inhibitory effects. According to the results obtained, the compounds I [R = Ph, 3-trifluoromethylphenyl] had the highest potency selectivity expression (PSE) values (60.6 and 19.2, resp.). On the other hand, the compounds I [R = benzyl] (Ki = 209.6 ± 70.2 pM) and [R = 3-methoxyphenyl] (Ki = 342.66 ± 63.72 pM) had the lowest Ki values in CA inhibition experiments towards hCA I and hCA II, resp. In conclusion, the compounds I [R = phenyl] (with cytotoxic/anticancer activity), I [R = benzyl] (with hCA I inhibiting activity) and I [R = 3-methoxyphenyl] (with hCA II inhibiting activity) can be leading compounds of the study for further designs and evaluations. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Safety 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..Safety of 1-Methylpiperazine

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

《Multi-cationic aminopyrene-based labeling tags for oligosaccharide analysis by capillary electrophoresis-mass spectrometry》 was published in Analytica Chimica Acta in 2020. These research results belong to Krenkova, Jana; Liskova, Marcela; Cmelik, Richard; Vigh, Gyula; Foret, Frantisek. Name: 1-Methylpiperazine The article mentions the following:

In this work, new multicationic aminopyrene-based labeling tags were designed and synthesized for oligosaccharide anal. by capillary electrophoresis-mass spectrometry (CE-MS). The starting compound, 8-aminopyrene-1,3,6-trisulfonic acid trisodium salt, was modified in order to form a sulfonamide derivative having three tertiary amines in the label structure. The sulfonamide derivative was further methylated to generate three permanently charged quaternary ammonium moieties on the label. The synthesized labels were characterized by NMR, IR, UV/Vis, fluorescence spectroscopy and mass spectrometry. Furthermore, the labels were applied for maltooligosaccharide standards as well as N-linked glycans labeling via reductive amination and followed by CE-MS anal. The CE-MS anal. of maltooligosaccharides labeled by these newly synthesized labels provided the sub-micromolar limit of detection based on the extracted ion electropherogram signals. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Name: 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..Name: 1-Methylpiperazine

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

Computed Properties of C5H12N2In 2020 ,《Design, synthesis, antimicrobial activity and molecular docking studies of some novel di-substituted sulfonylquinoxaline derivatives》 was published in Bioorganic Chemistry. The article was written by Ammar, Yousry A.; Farag, Awatef A.; Ali, Abeer M.; Ragab, Ahmed; Askar, Ahmed A.; Elsisi, Doaa M.; Belal, Amany. The article contains the following contents:

Compound I [R = Cl] was prepared via reaction of o-phenylene diamine with oxalic acid followed by chlorosulfonation with excess chlorosulfonic acid. A series of new sulfonylquinoxaline derivatives I [R = 3-MeOC6H4, 1-piperidyl, 2-(cyanomethyl)benzimidazol-1-yl, etc.] were obtained upon reacting compound I [R = Cl] with different types of amines. Compound II [R1 = R2 = Cl] was reacted with different secondary amines yielded mono and di secondary aminoquinoxaline derivatives II [R1 = 1-piperidyl, 4-methylpiperazin-1-yl, morpholino; R2 = Cl, morpholino, NHNH2, etc.] depending on the reactivity difference of the two chlorine atoms. Hydrazinolysis of compound II [R1 = 1-piperidyl, 4-methylpiperazin-1-yl, morpholino; R2 = Cl] furnished hydrazino quinoxaline derivatives II [R1 = 1-piperidyl, 4-methylpiperazin-1-yl, morpholino; R2 = NHNH2]. Addnl. triazolo and pyrazolyl quinoxaline derivatives III and IV [R3 = 5-OH-3-Me-pyrazol-1-yl, 2-[(2,5-diphenylpyrazol-3-yl)methylene]hydrazino] were obtained through the reaction of compound II [R1 = 1-piperidyl; R2 = NHNH2] with Ph isothiocyanate, formylpyrazole and Et acetoacetate. All the synthesized compounds were screened for their antibacterial and antifungal activities. Compounds II [R1 = 1-piperidyl, R2 = Cl; R1 = R2 = 4-methylpiperazin-1-yl; R1 = 1-piperidyl, R2 = 4-methylpiperazin-1-yl; R1 = 4-methylpiperazin-1-yl, R2 = 1-piperidyl; R1 = morpholino, R2 = 4-methylpiperazin-1-yl; R1 = morpholino, R2 = NHNH2] showed good to moderate antimicrobial activity against the tested Gram-pos., Gram-neg. bacteria and fungi with MIC values ranging from 2.44 to 180.14μM. Their MBC values were also evaluated using the same tested microorganisms. Moreover, screening against multi-drug resistant strains revealed the promiscuity of these new derivatives, especially compound II [R1 = 1-piperidyl, R2 = Cl] that showed comparable antibacterial activity (MIC 4.91-9.82μM) with Norfloxacin (MIC 2.44-9.80μM). Furthermore, these compounds were evaluated as DNA Gyrase inhibitors and the obtained results were in the range of 15.69-23.72μM. Mol. docking studies of the promising derivatives into DNA Gyrase binding site proved the usefulness of hybridizing quinoxaline scaffold with SO2 and morpholine moieties as a hopeful strategy in designing new DNA Gyrase binding mols. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Computed Properties 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..Computed Properties of C5H12N2

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

《Anticancer potential of new 3-nitroaryl-6-(N-methyl)piperazin-1,2,4-triazolo[3,4-a]phthalazines targeting voltage-gated K+ channel: Copper-catalyzed one-pot synthesis from 4-chloro-1-phthalazinyl-arylhydrazones》 was written by Romero, Angel H.; Sojo, Felipe; Arvelo, Francisco; Calderon, Christian; Morales, Alvaro; Lopez, Simon E.. Recommanded Product: 1-MethylpiperazineThis research focused ontriazolophthalazine preparation anticancer mol docking potassium channel; 1,2,4-triazolo-phthalazine; Anticancer activity; CH oxidative cyclization; Molecular docking; Nitro-substitution; Potassium-channel. The article conveys some information:

A series of six 3-aryl-6-(N-methylpiperazin)-1,2,4-triazolo[3,4-a]phthalazines were prepared through a facile and efficient one-pot copper-catalyzed procedure from 4-chloro-1-phthalazinyl-arylhydrazones with relatively good yields (62-83%). The one-pot copper-catalytic procedure consists of two simultaneous reactions: (i) a direct intramol. dehydrogenative cyclization between ylidenic carbon and adjacent pyrazine nitrogen to form 1,2,4-triazolo ring and, (ii) a direct N-amination on carbon-chlorine bond. Then, an in vitro anticancer evaluation was performed for the synthesized compounds against five selected human cancer cells (A549, MCF-7, SKBr3, PC-3 and HeLa). The nitro-derivatives were significantly more active against cancer strains than against the rest of tested compounds Specifically, compound I was identified as the most promising anticancer agent with significant biol. responses and low relative toxicities on human dermis fibroblast. The cytotoxic effect of compound I was more significant on PC3, MCF-7 and SKBr3 cancer cells with low-micromolar IC50 value ranging from 0.11 to 0.59μM, superior to Adriamycin drug. Mechanistic exptl. and theor. studies demonstrated that compounds I act as a K+ channel inhibitor in cancer models. Further mol. docking studies suggest that the EGFR Tyrosine Kinase enzyme may be a potential target for the most active 3-aryl-6-(N-methylpiperazin)-1,2,4-triazolo[3,4-a]phthalazines. In the part of experimental materials, we found many familiar compounds, such as 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

《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

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 《A novel water-soluble perylenetetracarboxylic diimide as a fluorescent pH probe: Chemosensing, biocompatibility and cell imaging》 were Georgiev, Nikolai I.; Said, Awad I.; Toshkova, Reneta A.; Tzoneva, Rumiana D.; Bojinov, Vladimir B.. And the article was published in Dyes and Pigments in 2019. Quality Control of 1-Methylpiperazine The author mentioned the following in the article:

Herein the authors pay attention to the design, synthesis and sensor activity of a novel biocompatible perylene-3,4,9,10-tetracarboxylic diimide (PDI) pH-probe in water. The synthesized compound shows selective fluorescence signaling properties as a function of pH (pKa value of 6.35±0.02) which makes the probe suitable for pH determination in the physiol. range. Thus prepared water soluble fluorescent system demonstrate low cytotoxicity to L929 cell lines from 330 μM to 1.3 μM and cell permeability in the lower concentration range. That findings show the high potential of the newly prepared PDI probe for monitoring of pH variations in bio-samples. The experimental process involved the reaction of 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

Application In Synthesis of 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acidOn May 9, 2008 ,《Spectral correlation of high-performance liquid chromatography-diode array detection data from two independent chromatographic runs》 appeared in Journal of Chromatography A. The author of the article were Li, Wei; Hu, Chang-qin. The article conveys some information:

A novel qual. anal. method for peak tracking in impurity profiling control by the correlation of spectra was established. Two-dimensional (2D) standard spectrochromatog. data produced by HPLC with diode array detection (HPLC-DAD) were compared with sample data to develop two-dimensional chromatog. spectral correlative maps. Taking full advantage of separation efficiency of HPLC and spectral specificity of the analytes, the method was successfully used to recognize impurities in quinolone antibacterials, when in combination with relative retention times (RRTs). For the comparison of spectra was expanded to three-dimensional space, simultaneous identification of the chromatog. peaks can be obtained rapidly without preparation and injection of a reference solution, even when the mobile phase changed or the peaks of multi-component samples overlapped. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid(cas: 182868-72-0Application In Synthesis of 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid)

1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid(cas: 182868-72-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).Application In Synthesis of 1-Cyclopropyl-8-ethoxy-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

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