Category: Pyrazines

Related Products of 591-54-8. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Racemization-free synthesis of dipeptide, amide and ester by oxalyl chloride and catalytic triphenylphosphine oxide. Author is Ren, Ji-Wei; Tong, Meng-Nan; Zhao, Yu-Fen; Ni, Feng.

An efficient triphenylphosphine oxide (Ph3PO) catalyzed amidation and esterification reaction for rapid synthesis of a series of dipeptides, amides and esters under mild condition is described. This reaction is applicable to challenging couplings of hindered carboxylic acid with low nucleophilic amine or alc., giving products in good yields (67-90%) without any racemization. This system employs highly reactive intermediate Ph3PCl2 as activator of carboxylate, in a catalytic manner, and drive the reaction to complete in short reaction time (less than 10 min). It has the advantages of good functional group tolerance, broad substrate scope and good atom-economy. A 100 mmol scale reaction with good yield shed light on its potential for industrial application. A plausible mechanism is proposed based on 31P NMR monitor of reaction process.

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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Study on L-cystine conversion technology by Pseudomonas putida TS1138, published in 2008-01-20, which mentions a compound: 2150-55-2, mainly applied to Pseudomonas cystine cysteine, COA of Formula: C4H6N2O2S.

A technol. of L-cystine production was studied in this paper, which included microbial enzymic conversion of DL-2-amino-Δ2-thiazoline-4- carboxylic acid (DL-ATC) to L-cysteine, subsequent oxidization of L-cysteine to L-cystine and its purification The cells of Pseudomonas putida TS1138 could be repetitively used as the enzyme sources to convert the substrate DL-ATC to L-cysteine. After being oxidized by 2% dimethy-sulfoxide (DMSO), L-cystine could be harvested and further purified by the pos. ion-exchange resin 001*7. High Performance Liquid Chromatog. (HPLC) identified the purified L-cystine as having a total recovery of 78.55% and purity of 99.12%. This study demonstrated an efficient and convenient method for L- cystine production, which overcame the instability of enzymes, troublesome procedures and high cost of enzyme immobilization as contrasted to the traditional method. All in all, it provides a new approach for industrial production of L- cystine as well as L-cysteine.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about A Two-Stage Iterative Process for the Synthesis of Poly-oxazoles.Related Products of 118994-89-1.

Methodol. has been developed to prepare bis-oxazoles via a two-stage iterative process. The sequence begins with C(2)-chlorination of a lithiated oxazole using hexachloroethane. Generation of the C(2)-C(4′) bond by SNAr substitution with TosMIC anion, followed by conversion to the heterocycle in a one-pot reaction with glyoxylic acid monohydrate, affords the desired bis-oxazole in good yield and purity. The two-stage process allows for efficient synthesis of a tris-oxazole and the iterative preparation of a tetra-oxazole.

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Recommanded Product: 5-Amino-2-fluoropyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Design, synthesis of novel celastrol derivatives and study on their antitumor growth through HIF-1α pathway. Author is Shang, Fan-Fan; Wang, Jing Ying; Xu, Qian; Deng, Hao; Guo, Hong-Yan; Jin, Xuejun; Li, Xiaoting; Shen, Qing-Kun; Quan, Zhe-Shan.

Four series of hypoxia-inducible factor-1 alpha (HIF-1α) functioning derivatives stemming from modifications to the C-29 carboxyl group of celastrol were designed and synthesized, and their anticancer activities were evaluated. To address the structure and activity relationship of each derivative, extensive structural changes were made. HRE luciferase reporter assay demonstrated that 12 modified compounds showed superior HIF-1α inhibitory activity. Among them, quinolin-7-yloxy derivative I exhibited the best features: first, it had the strongest HIF-1α inhibitory activity (IC50 = 0.05μM, 5-fold higher than that of celastrol), and second, it possessed lower cytotoxicity (22-fold lower, I 16.85μM vs. celastrol 0.76μM). Thus, the safety factor of C6 was about 112 times higher than that of celastrol. Western blot assay indicated that I may inhibit the expression of HIF-1α protein in cells. Addnl., I hindered tumor cell cloning, migration and induced cell apoptosis. It is worth mentioning that in the mouse tumor xenograft model, I (10 mg/kg) displayed good antitumor activity in vivo, showing a better inhibition rate (74.03%) than the reference compound 5-fluorouracil (inhibition rate, 59.58%). However, the celastrol treatment group experienced collective death after four doses of the drug. Moreover, I minimally affected the mouse weight, indicating that its application in vivo has little toxic effect. H&E staining experiments show that it could also exacerbate the degree of tumor cell damage. The results of water solubility experiment show that the solubility of I is increased by 1.36 times than that of celastrol. In conclusion, I is a promising antitumor agent through the HIF-1α pathway.

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Pyrazine – Wikipedia,
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Formula: C4H6N2O2S. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Progress on enzymatic synthesis of L-cysteine from DL-ATC by Pseudomonas sp.. Author is Wu, Min; Chen, Wei-qing; Wang, Pu; He, Jun-yao.

A review. The microbial transformation method for L-cysteine production shows evident advantages, because of its short cycle time, low cost, high region and stereoselectivity, easy control of reaction condition, and environment-friendly. Recently, studies on the bioconversion of DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) to L-cysteine by intracellular enzymes were reported. The research progresses on L-cysteine production by microbial bioconversion, especially Pseudomonas sp., or its crude enzyme extract are summarized. The applications of immobilization technol. in the biotransformation of DL-ATC to L-cysteine are introduced. The genetically engineered bacteria and the study progresses of L-cysteine desulfhydrase were also discussed.

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HPLC of Formula: 1827-27-6. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Solvent and substituent effects on fluorine-19 chemical shifts in some 5-substituted 2-fluoropyridines. Author is Giam, Choo-Seng; Lyle, James L..

The 19F NMR chem. shifts of several 5-substituted 2-fluoropyridines in 4 widely different solvents have been measured. The effects of solvents and substituents on the shifts paralleled those in the benzene series with certain modifications.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about A general route to the Streptomyces-derived inthomycin family: the first synthesis of (+)-inthomycin B.Safety of Ethyl oxazole-5-carboxylate.

A concise, convergent and stereocontrolled synthesis of (+)-inthomycin B (I), based on the Stille coupling of a stannyl-diene with an oxazole vinyl iodide unit, is described. The asym. center was introduced using the Kiyooka ketene acetal/amino acid-derived oxazaborolidinone procedure.

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Pyrazine – Wikipedia,
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Name: 4-Aminopyrimidine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Design, synthesis and biological evaluation of pyridone-aminal derivatives as MNK1/2 inhibitors. Author is Yuan, Xinrui; Wu, Hanshu; Bu, Hong; Zheng, Peiyuan; Zhou, Jinpei; Zhang, Huibin.

Excessive phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) plays a major role in the dysregulation of mRNA translation and the activation of tumor cell signaling. eIF4E is exclusively phosphorylated by mitogen-activated protein kinase interacting kinases 1 and 2 (MNK1/2) on Ser209. So, MNK1/2 inhibitors could decrease the level of p-eIF4E and regulate tumor-associated signaling pathways. A series of pyridone-aminal derivatives were synthesized and evaluated as MNK1/2 inhibitors. Several compounds exhibited great inhibitory activity against MNK1/2 and selected compounds showed moderate to excellent anti-proliferative potency against hematol. cancer cell lines. In particular, compound 42i (MNK1 IC50 = 7.0 nM; MNK2 IC50 = 6.1 nM) proved to be the most potent compound against TMD-8 cell line with IC50 value of 0.91 μM. Furthermore, 42i could block the phosphorylation level of eIF4E in CT-26 cell line, and 42i inhibited the tumor growth of CT-26 allograft model significantly. These results indicated that compound 42i was a promising MNK1/2 inhibitor for the potent treatment of colon cancer.

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Electric Literature of C5H5FN2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Design, Synthesis, and Structure-Activity Relationship of Indole-3-glyoxylamide Libraries Possessing Highly Potent Activity in a Cell Line Model of Prion Disease. Author is Thompson, Mark J.; Borsenberger, Vinciane; Louth, Jennifer C.; Judd, Katie E.; Chen, Beining.

Transmissible spongiform encephalopathies (TSEs) are a family of invariably fatal neurodegenerative disorders for which no effective curative therapy currently exists. We report here the synthesis of a library of indole-3-glyoxylamides and their evaluation as potential antiprion agents. A number of compounds demonstrated submicromolar activity in a cell line model of prion disease together with a defined structure-activity relationship, permitting the design of more potent compounds that effected clearance of scrapie in the low nanomolar range. Thus, the indole-3-glyoxylamides described herein constitute ideal candidates to progress to further development as potential therapeutics for the family of human prion disorders.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 591-54-8, is researched, Molecular C4H5N3, about Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents, the main research direction is arylalkyl methylacridinium preparation antibacterial SAR mol docking; 9-Arylalkyl-10-methylacridinium derivatives; Antibacterial activity; Design and synthesis; FtsZ inhibitor; Structure-activity relationships.Name: 4-Aminopyrimidine.

With the increasing incidence of antibiotic resistance, new antibacterial agents having novel mechanisms of action hence are in an urgent need to combat infectious diseases caused by multidrug-resistant (MDR) pathogens. Four novel series of substituted 9-arylalkyl-10-methylacridinium derivatives as FtsZ inhibitors were designed, synthesized and evaluated for their antibacterial activities against various Gram-pos. and Gram-neg. bacteria. The results demonstrated that they exhibited broad-spectrum activities with substantial efficacy against MRSA and VRE, which were superior or comparable to the berberine, sanguinarine, linezolid, ciprofloxacin and vancomycin. In particular, the most promising compound I showed rapid bactericidal properties, which avoid the emergence of drug resistance. However, I showed no inhibitory effect on Gram-neg. bacteria but biofilm formation study gave possible answers. Further target identification and mechanistic studies revealed that I functioned as an effective FtsZ inhibitor to alter the dynamics of FtsZ self-polymerization, which resulted in termination of the cell division and caused cell death. Further cytotoxicity and animal studies demonstrated that I not only displayed efficacy in a murine model of bacteremia in vivo, but also no significant hemolysis to mammalian cells. Overall, this compound with novel skeleton could serve as an antibacterial lead of FtsZ inhibitor for further evaluation of drug-likeness.

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Pyrazine – Wikipedia,
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