Pyrazines

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Studies on the relation between 2-iminothiazolidine-4-carboxylic acid and the thiocyanate metabolism in the guinea pig, the main research direction is iminothiazolidine carboxylate metabolism; thiocyanate iminothiazolidine carboxylate metabolite.Recommanded Product: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

In vitro and in vivo experiments have been carried out to elucidate the metabolism of 2-iminothiazolidine-4-carboxylic acid (I) [2150-55-2]. By using I-35S, the formation. of 35SCN as well as of 35S-containing I metabolites could be excluded. As compared to the findings from control animals, the serum SCN levels determined in guinea pigs after oral administration of I were unchanged.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Huang, Huazhang; Nishi, Kosuke; Tsai, Hsing-Ju; Hammock, Bruce D. published an article about the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F ).Recommanded Product: 1827-27-6. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:1827-27-6) through the article.

Fatty acid amide hydrolase (FAAH) is a pharmaceutical target whose inhibition may lead to valuable therapeutics. Sensitive substrates for high-throughput assays are crucial for the rapid-screening FAAH inhibitors. Here we describe the development of novel and highly sensitive fluorescent assays for FAAH based on substituted aminopyridines. Examining the relationship between the structure and the fluorescence of substituted aminopyridines suggested that a methoxy group in the para position relative to the amino group in aminopyridines greatly increased the fluorescence (i.e., quantum yields approach unity). These novel fluorescent reporters had a high Stokes’ shift of 94 nm, and their fluorescence in buffer systems increased with pH values from neutral to basic. Fluorescent substrates with these reporters displayed a very low fluorescent background and high aqueous solubility Most importantly, fluorescent assays for FAAH based on these substrates were at least 25 times more sensitive than assays using related compounds with published colorimetric or fluorescent reporters. This property results in shorter assay times and decreased protein concentrations in the assays. Such sensitive assays will facilitate distinguishing the relative potency of powerful inhibitors of FAAH. When these fluorescent substrates were applied to human liver microsomes, results suggested that there was at least one amide hydrolase in addition to FAAH that could hydrolyze long-chain fatty acid amides. These results show that these fluorescent substrates are very valuable tools in FAAH activity assays including screening inhibitors by high-throughput assays instead of using the costly and labor-intensive radioactive ligands. Potential applications of novel fluorescent reporters are discussed.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Quality Control of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Microbial enzyme conversion of L-cysteine and L-cystine. Author is Liu, Zhong; Yang, Wenbo; Bai, Gang; Tian, Wang; Jin, Yongjie.

Pseudomonas sp. TS1138 isolated from soil samples was able to form L-cysteine from DL-2-Amiuo-δ2-Thiazoline-4-Carboxylic Acid (DL-ATC) after cultured 16 h. The optimum carbon and nitrogen sources of strain growth and enzyme formation are glucose and urea. This enzyme was induced by DL-ATC. The product was identified to be L-Cysteine based on thin layer chromatog., optical rotation and HPLC studies.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Sano, Konosuke; Eguchi, Chikahiko; Yasuda, Naohiko; Mitsugi, Koji published the article 《Metabolic pathway of L-cysteine formation from DL-2-amino-Δ2-thiazoline-4-carboxylic acid by Pseudomonas》. Keywords: aminothiazolinecarboxylate metabolism Pseudomonas cysteine.They researched the compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid( cas:2150-55-2 ).Recommanded Product: 2150-55-2. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:2150-55-2) here.

DL-2-Amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) was completely converted to L-cysteine by intact cells or homogenates of P. thiazolinophilum. S-Carbamylcysteine was the actual intermediate of ATC hydrolysis. P. desmolytica Hydrolyzed only 50% of DL-ATC, but completely converted L-ATC into L-cysteine, suggesting that the organism had no ATC-racemizing enzyme and that ATC is racemized by an enzyme in P. thiazolinophilum. A proposed pathway from D-ATC to L-cysteine in P.thiazolinophilum is presented.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine(SMILESS: NC1=CC(C2=CC=NC=C2)=NN1,cas:91912-53-7) is researched.Name: 5-Amino-2-fluoropyridine. The article 《Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:91912-53-7).

Interleukin-12 (IL-12) and IL-23 are proinflammatory cytokines and therapeutic targets for inflammatory and autoimmune diseases, including inflammatory bowel diseases, psoriasis, rheumatoid arthritis, and multiple sclerosis. The authors describe the discovery of APY0201, a unique small mol. IL-12/23 production inhibitor, from activated macrophages and monocytes, and demonstrate ameliorated inflammation in an exptl. model of colitis. Through a chem. proteomics approach using a highly sensitive direct nanoflow LC-MS/MS system and bait compounds equipped with the FLAG epitope associated regulator of PIKfyve (ArPIKfyve) was detected. Further study identified its associated protein phosphoinositide kinase, FYVE finger-containing (PIKfyve), as the target protein of APY0201, which was characterized as a potent, highly selective, ATP-competitive PIKfyve inhibitor that interrupts the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3,5)P2. These results elucidate the function of PIKfyve kinase in the IL-12/23 production pathway and in IL-12/23-driven inflammatory disease pathologies to provide a compelling rationale for targeting PIKfyve kinase in inflammatory and autoimmune diseases.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Zhang, Pei; Jiang, Mei-Yan; Le, Mei-Ling; Zhang, Bei; Zhou, Qian; Wu, Yinuo; Zhang, Chen; Luo, Hai-Bin published an article about the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F ).Name: 5-Amino-2-fluoropyridine. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:1827-27-6) through the article.

Phosphodiesterase-9 (PDE9) is a promising target for the treatment of Alzheimer’s disease (AD). To discover efficient PDE9 inhibitors with good metabolic stability and solubility, a series of novel pyrazolopyrimidinone derivatives were designed with the assistance of mol. docking and dynamics simulations. All the fourteen synthesized compounds gave excellent inhibition ratio against PDE9 at 10 nM. Compound (R)-N-(1H-benzo[d]imidazol-5-yl)-2-((1-cyclopentyl-4-oxo-4,5-dihydro-1H-pyrazolo [3,4-d]pyrimidin-6-yl)amino)propanamide with the IC50 of 2.0 nM against PDE9, showed good metabolic stability (t1/2 of 57 min) in the RLM as well as good solubility (195 mg/L). The anal. on binding modes of targeted compounds may provide insight for further structural modification.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 118994-89-1, is researched, SMILESS is O=C(C1=CN=CO1)OCC, Molecular C6H7NO3Journal, Article, Research Support, Non-U.S. Gov’t, Organic Letters called Direct arylation of oxazoles at C2. a concise approach to consecutively linked oxazoles, Author is Flegeau, Emmanuel Ferrer; Popkin, Matthew E.; Greaney, Michael F., the main research direction is substituted oxazole derivative preparation; oxazole aryl iodide cross coupling palladium; teroxazolecarboxylate preparation.COA of Formula: C6H7NO3.

The synthesis of bis- and trisoxazoles via direct arylation is discussed. A variety of aryl groups can be installed at the 2-position of 5-aryl and 5-carboxy-substituted oxazoles under mild conditions using palladium catalysis on water. The direct arylation method can be extended to the synthesis of bis- and trisoxazoles if 2-triisopropylsilyl-4-iodooxazole is used as the electrophile in the arylation.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Reference of 5-Amino-2-fluoropyridine. 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: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides. Author is Demjen, Andras; Alfoeldi, Robert; Angyal, Aniko; Gyuris, Mario; Hackler, Laszlo Jr.; Szebeni, Gabor J.; Woelfling, Janos; Puskas, Laszlo G.; Kanizsai, Ivan.

The synthesis and in vitro cytotoxic characteristics of new imidazo[1,2-b]pyrazole-7-carboxamides were investigated. Following a hit-to-lead optimization exploiting 2D and 3D cultures of MCF-7 human breast, 4T1 mammary gland, and HL-60 human promyelocytic leukemia cancer cell lines, a 67-membered library was constructed and the structure-activity relationship (SAR) was determined Seven synthesized analogs exhibited sub-micromolar activities, from which compound 63 (2-(tert-Butyl)-N-(4-fluorophenyl)-3-((2,4,4-trimethylpentan-2-yl)amino)-1H-imidazo[1,2-b]pyrazole-7-carboxamide) exerted the most significant potency with a remarkable HL-60 sensitivity (IC50 = 0.183 μM).

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: 4-Aminopyrimidine. 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 Design, synthesis, molecular docking and cytotoxic activity of novel urea derivatives of 2-amino-3-carbomethoxythiophene. Author is Vikram, Venugopalarao; Penumutchu, Srinivasa R.; Vankayala, Raviraj; Thangudu, Suresh; Amperayani, Karteek Rao; Parimi, Umadevi.

An efficient feasible route for the one-pot synthesis of novel series of urea derivatives (2a-2j) from 2-amino-3-carbomethoxythiophene (1) via in situ isocyanate has been developed, and their corresponding anticancer activities were accomplished. The series of urea derivatives were characterized by using 1H, 13C NMR and mass spectroscopic anal. The cytotoxic activities were evaluated against human cervical (HeLa) and human lung (NCI-H23) cancer cell lines. These studies revealed satisfactory activity for some of the compounds, which could potentially serve as lead compounds for drug discovery and development. Furthermore, mol. docking studies supported in identifying the potential binding sites between the urea derivatives and eukaryotic ribonucleotidereductase (RR). High ambiguity driven docking (HADDOCK) modeling was specifically employed to determine the model complex of RR and urea derivatives The proposed model has provided a deep insight into the mol. level interactions of RR-urea model complexes in understanding the exact pharmacophore for designing highly potent RR inhibitors. Overall, the present work has shed light in developing a feasible and robust approach for the synthesis of novel urea derivatives of 2-amino-3-carbomethoxythiophene and identified a part of mol. structure that is responsible for a specific biol. interaction leading to potential anticancer activities. Graphic abstract: We report herein, the exptl. design, synthesis and characterization of a novel series of urea derivatives of 2-amino-3carbomethoxythiophene with pyrimidine amine and benzyl amine analogs as both derivatives which exhibited potential antitumor activity via one pot synthesis and subsequently studied the structure activity relationships (SAR), and anticancer activities. The docking studies identified a part of molecularstructure that is responsible for a specific biol. interaction leading to the destruction of cancer cells.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Study on L-cystine conversion technology by Pseudomonas putida TS1138, the main research direction is Pseudomonas cystine cysteine.Quality Control of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

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.

After consulting a lot of data, we found that this compound(2150-55-2)Quality Control of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem