Category: Pyrazines

On August 31, 1983, Vekemans, J.; Pollers-Wieers, C.; Hoornaert, G. published an article.SDS of cas: 87486-34-8 The title of the article was A new synthesis of substituted 2(1H)-pyrazinones. And the article contained the following:

The hydrohalides of 2-sec-aminoalkanenitriles on treatment with oxalyl halides in o-Cl2C6H4 at 80-100° give 3,5-dihalo-2(1H)-pyrazinones, e.g. I, of which the 3-halo substituent is easily replaced by nucleophiles. A reaction mechanism for the pyrazinone synthesis is proposed. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).SDS of cas: 87486-34-8

The Article related to pyrazinone, aminoalkanenitrile cyclization oxalyl chloride, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On May 10, 2013, Crawford, James John; Ortwine, Daniel Fred; Wei, Binqing; Young, Wendy B. published a patent.Recommanded Product: 87486-34-8 The title of the patent was Heteroarylpyridone and azapyridone compounds as inhibitors of BTK activity and their preparation. And the patent contained the following:

The invention relates to heteroarylpyridone and azapyridone compounds of formula I and stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathol. conditions, are disclosed. Compounds of formula I wherein X1is CR1 and N; X2 is CR2 and N; X3 is CR3 and N, where one or two of X1 – X2 are N; R1, R2 and R4 are independently H, F, Cl, NH2, etc.; R4 is H, F, Cl, CN, CH2OH, etc.; R5 is (un)substituted C6-20 aryl, C3-12 carbocyclyl, C1-20 heteroaryl, etc.; R6 is H, Me, Et, etc.; R7 is (un)substituted tricyclic azacyclyl; Y1 and Y2 are independently CH and N, provided that not both of Y1 and Y2 are N; and stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their BTK inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.132 μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Recommanded Product: 87486-34-8

The Article related to heteroarylpyridone azapyridone preparation btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On June 7, 2007, Mulvihill, Kristen Michelle; Castelhano, Arlindo L. published a patent.Category: pyrazines The title of the patent was Process for the preparation of substituted imidazo[1,5-a]pyrazines. And the patent contained the following:

The title compounds [I; X = Cl, Br, I; e.g., 3-(1-bromo-8-chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone] are prepared by the halogenation of 3-(8-chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone with either N-chloro-, N-bromo-, or N-iodosuccinimide (e.g., NBS) in a compatible solvent (e.g., DMF) at 0-60°. The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).Category: pyrazines

The Article related to bromochloroimidazopyrazinylcyclobutanone preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrazines

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On February 17, 2022, Chen, Yi published a patent.SDS of cas: 87486-34-8 The title of the patent was Preparation of heterocyclic compounds as BTK inhibitors, and dosage form compositions comprising an inhibitor of BTK and mutants thereof. And the patent contained the following:

Provided herewith are pharmaceutical tablet compositions comprising an organic acid (such as fumaric acid) and a compound of formula I, or an N-oxide thereof, solvate, polymorph, tautomer, stereoisomer, an isotopic form, or a prodrug of said compound of formula I or N-oxide thereof: wherein the compound of formula I is an inhibitor of Bruton’ s tyrosine kinase. Compounds of formula I wherein Q3 is 5-membered heteroaryl; m and n are independently 0, 1, 2, 3 and 4; R1 and R5 are independently H, D, alkyl,spiroalkyl, alkenyl, etc.; and their tablet compositions comprising organic acids, N-oxides, polymorphs, tautomers, stereoisomers, isotopic forms, and prodrugs, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were formulated as tablets and tested for pharmacokinetic properties (data given). The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).SDS of cas: 87486-34-8

The Article related to heterocyclyl preparation btk inhibitor dosage form, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On August 1, 2022, Aguinaga Martinez, Maite V.; Jozicova, Natali; Dusek, Jan; Horstkotte, Burkhard; Pavek, Petr; Miro, Manuel; Sklenarova, Hana published an article.Synthetic Route of 55779-48-1 The title of the article was Real-time monitoring of Metridia luciferase release from cells upon interaction with model toxic substances by a fully automatic flow setup – A proof of concept. And the article contained the following:

This manuscript reports on a fully automatic sequential injection system incorporating a 3D printed module for real-time monitoring of the release of Metridia luciferase from a modified liver epithelial cell line. To this end, a simple and effective approach for the automation of flash-type chemiluminescence assays was developed. The 3D printed module comprised an apical and a basal compartment that enabled monitoring membrane processes on both sides of the cell monolayer aimed at elucidating the direction of luciferase release. A natural release was observed after transfection with the luciferase plasmid by online measurement of the elicited light from the reaction of the synthesized luciferase with the coelenterazine substrate. Model substances for acute toxicity from the group of cholic acids – chenodeoxycholic and deoxycholic acids – were applied at the 1.0 and 0.5 mmol L-1 levels. The tested cholic acids caused changes in cell membrane permeability that was accompanied by an increased luciferase release. The obtained kinetic profiles were evaluated based on the delay between the addition of the toxic substance and the increase of the chemiluminescence signal. All experiments were carried out in a fully automatic system in ca. 5 min per sample in 30 min intervals and no manual interventions were needed for a sampling period of at least 6 h. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Synthetic Route of 55779-48-1

The Article related to metridia luciferase liver epithelial cell toxicity chemiluminescence, 3d-printing, automation, cell toxicity, metridia luciferase, real-time monitoring, sequential injection analysis and other aspects.Synthetic Route of 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Nguyen, Hieu T. H.; Bouteau, Francois; Mazars, Christian; Kuse, Masaki; Kawano, Tomonori published an article in 2019, the title of the article was Enhanced elevations of hypo-osmotic shock-induced cytosolic and nucleic calcium concentrations in tobacco cells by pretreatment with dimethyl sulfoxide.Category: pyrazines And the article contains the following content:

DMSO (DMSO) is a dipolar aprotic solvent widely used in biol. assays. Here, we observed that DMSO enhanced the hypo-osmotically induced increases in the concentration of Ca2+ in cytosolic and nucleic compartments in the transgenic cell-lines of tobacco (BY-2) expressing aequorin. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Category: pyrazines

The Article related to calcium dimethyl sulfoxide aequorin nicotiana cell suspension cytosol nucleus, cytosolic calcium concentration, dimethyl sulfoxide, hypo-osmotic shock, nucleic calcium concentration and other aspects.Category: pyrazines

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Bakayan, Adil; Picaud, Sandrine; Malikova, Natalia P.; Tricoire, Ludovic; Lambolez, Bertrand; Vysotski, Eugene S.; Peyrieras, Nadine published an article in 2020, the title of the article was RedquorinXS mutants with enhanced calcium sensitivity and bioluminescence output efficiently report cellular and neuronal network activities.Synthetic Route of 55779-48-1 And the article contains the following content:

Considerable efforts have been focused on shifting the wavelength of aequorin Ca2+-dependent blue bioluminescence through fusion with fluorescent proteins. This approach has notably yielded the widely used GFP-aequorin (GA) Ca2+ sensor emitting green light, and tdTomato-aequorin (Redquorin), whose bioluminescence is completely shifted to red, but whose Ca2+ sensitivity is low. In the present study, the screening of aequorin mutants generated at twenty-four amino acid positions in and around EF-hand Ca2+-binding domains resulted in the isolation of six aequorin single or double mutants (AequorinXS) in EF2, EF3, and C-terminal tail, which exhibited markedly higher Ca2+ sensitivity than wild-type aequorin in vitro. The corresponding Redquorin mutants all showed higher Ca2+ sensitivity than wild-type Redquorin, and four of them (RedquorinXS) matched the Ca2+ sensitivity of GA in vitro. RedquorinXS mutants exhibited unaltered thermostability and peak emission wavelengths. Upon stable expression in mammalian cell line, all RedquorinXS mutants reported the activation of the P2Y2 receptor by ATP with higher sensitivity and assay robustness than wt-Redquorin, and one, RedquorinXS-Q159T, outperformed GA. Finally, wide-field bioluminescence imaging in mouse neocortical slices showed that RedquorinXS-Q159T and GA similarly reported neuronal network activities elicited by the removal of extracellular Mg2+. Our results indicate that RedquorinXS-Q159T is a red light-emitting Ca2+ sensor suitable for the monitoring of intracellular signaling in a variety of applications in cells and tissues, and is a promising candidate for the transcranial monitoring of brain activities in living mice. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Synthetic Route of 55779-48-1

The Article related to redquorinxs mutant calcium sensitivity bioluminescence cellular neuronal network, bret, gpcr assay, aequorin, bioluminescence, calcium sensor, mutagenesis, neuronal network imaging and other aspects.Synthetic Route of 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On December 1, 2019, Pinto da Silva, Luis; Nunez-Montenegro, Ara; Magalhaes, Carla M.; Ferreira, Paulo J. O.; Duarte, Diana; Gonzalez-Berdullas, Patricia; Rodriguez-Borges, Jose E.; Vale, Nuno; Esteves da Silva, Joaquim C. G. published an article.HPLC of Formula: 55779-48-1 The title of the article was Single-molecule chemiluminescent photosensitizer for a self-activating and tumor-selective photodynamic therapy of cancer. And the article contained the following:

While photodynamic therapy is known for significant advantages over conventional cancer therapies, its dependence on light has limited it to treating tumors on or just under the skin or on the outer lining of organs/cavities. Herein, we have developed a single-mol. photosensitizer capable of intracellular self-activation and with potential tumor-selectivity due to a chemiluminescent reaction involving only a cancer marker. Thus, the photosensitizer is directly chemiexcited to a triplet excited state capable of generating singlet oxygen, without requiring either a light source or any catalyst/co-factor. Cytotoxicity assays involving the photosensitizer show significant toxicity toward tumor cells, even better than reference drugs, while not inducing toxicity toward normal cells. This work provides a proof-of-concept for a novel type of photosensitizer that eliminates the current restrictions that photodynamic therapy presents regarding tumor size and localization. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).HPLC of Formula: 55779-48-1

The Article related to chemiluminescent photosensitizer cancer pdt photodynamic therapy, breast cancer, cancer, chemiluminescence, coelenterazine, photodynamic therapy, photosensitizer, prostate cancer and other aspects.HPLC of Formula: 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On July 1, 2019, Yang, Jianhong; Du, Jiatian; Huang, Chong; Wang, Tianqi; Huang, Luyi; Yang, Shengyong; Li, Linli published an article.COA of Formula: C5H4Br2N2O The title of the article was Discovery of 5-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrazin-2(1H)-one derivatives as new potent PB2 inhibitors. And the article contained the following:

PB2 is an important subunit of influenza RNA-dependent RNA polymerase (RdRP) and has been recognized as a promising target for the treatment of influenza. We herein report the discovery of a new series of PB2 inhibitors containing the skeleton 5-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrazin-2(1H)-one. Compound I is the most potent one, which showed KD values of 0.11 μM and 0.19 μM in surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) assays, resp. In antiviral activity and cellular cytotoxicity assays, compound I showed an EC50 value of 1.025 μM and a CC50 value greater than 100 μM. Mol. docking was also used to predict the binding mode of I with PB2. Collectively, this study provides a promising lead compound for subsequent anti-influenza drug discovery targeting PB2. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).COA of Formula: C5H4Br2N2O

The Article related to fluoropyrrolopyridinyl pyrazinone preparation pb2 inhibitor antiinfluenza antiviral activity, influenza a virus, pb2, small molecule inhibitor, structure-activity relationship and other aspects.COA of Formula: C5H4Br2N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Zenchak, Jessica R.; Palmateer, Brandon; Dorka, Nicolai; Brown, Tariq M.; Wagner, Lina-Marie; Medendorp, William E.; Petersen, Eric D.; Prakash, Mansi; Hochgeschwender, Ute published an article in 2020, the title of the article was Bioluminescence-driven optogenetic activation of transplanted neural precursor cells improves motor deficits in a Parkinson′s disease mouse model.SDS of cas: 55779-48-1 And the article contains the following content:

The need to develop efficient therapies for neurodegenerative diseases is urgent, especially given the increasing percentages of the population living longer, with increasing chances of being afflicted with conditions like Parkinson′s disease (PD). A promising curative approach toward PD and other neurodegenerative diseases is the transplantation of stem cells to halt and potentially reverse neuronal degeneration. However, stem cell therapy does not consistently lead to improvement for patients. Using remote stimulation to optogenetically activate transplanted cells, we attempted to improve behavioral outcomes of stem cell transplantation. We generated a neuronal precursor cell line expressing luminopsin 3 (LMO3), a luciferase-channelrhodopsin fusion protein, which responds to the luciferase substrate coelenterazine (CTZ) with emission of blue light that in turn activates the opsin. Neuronal precursor cells were injected bilaterally into the striatum of homozygous aphakia mice, which carry a spontaneous mutation leading to lack of dopaminergic neurons and symptoms of PD. Following transplantation, the cells were stimulated over a period of 10 days by intraventricular injections of CTZ. Mice receiving CTZ demonstrated significantly improved motor skills in a rotarod test compared to mice receiving vehicle. Thus, bioluminescent optogenetic stimulation of transplanted neuronal precursor cells shows promising effects in improving locomotor behavior in the aphakia PD mouse model and encourages further studies to elucidate the mechanisms and long-term outcomes of these beneficial effects. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).SDS of cas: 55779-48-1

The Article related to bioluminescence optogenetic neural precursor cell parkinson disease mouse, pitx3, chemogenetic, embryonic stem cells, luminopsin, multielectrode array, neural differentiation and other aspects.SDS of cas: 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem