Tag: M.W=100-200

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: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201.Reference of 3-(Pyridin-4-yl)-1H-pyrazol-5-amine.

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 | 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: 2150-55-2, is researched, SMILESS is O=C(C1N=C(N)SC1)O, Molecular C4H6N2O2SJournal, Article, Toxicology Mechanisms and Methods called Spectrophotometric analysis of the cyanide metabolite 2-aminothiazoline-4-carboxylic acid (ATCA), Author is Baskin, Steven I.; Petrikovics, Ilona; Platoff, Gennady E.; Rockwood, Gary A.; Logue, Brian A., the main research direction is cyanide metabolite aminothiazoline carboxylic acid preparation spectrophotometry.Application of 2150-55-2.

Methods of directly evaluating cyanide levels are limited by the volatility of cyanide and by the difficulty of establishing steady-state cyanide levels with time. We investigated the measurement of a stable, toxic metabolite, 2-aminothiazoline-4-carboxylic acid (ATCA), in an attempt to circumvent the challenge of directly determining cyanide concentrations in aqueous media. This study was focused on the spectrophotometric ATCA determination in the presence of cyanide, thiocyanate (SCN-), cysteine, rhodanese, thiosulfate, and other sulfur donors. The method involves a thiazolidine ring opening in the presence of p-(hydroxy-mercury)-benzoate, followed by the reaction with diphenylthiocarbazone (dithizone). The product is spectrophotometrically analyzed at 625 nm in CCl4. The calibration curve was linear with a regression line of Y = 0.0022x (R2 = 0.9971). Interference of cyanide antidotes with the method was determined Cyanide, thiosulfate, butanethiosulfonate (BTS), and rhodanese did not appreciably interfere with the anal., but SCN- and cysteine significantly shifted the standard curve. This sensitive spectrophotometric method has shown promise as a substitute for the measurement of the less stable cyanide.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Organic Letters called The Kondrat’eva Reaction in Flow: Direct Access to Annulated Pyridines, Author is Lehmann, Johannes; Alzieu, Thibaut; Martin, Rainer E.; Britton, Robert, which mentions a compound: 118994-89-1, SMILESS is O=C(C1=CN=CO1)OCC, Molecular C6H7NO3, Recommanded Product: Ethyl oxazole-5-carboxylate.

A continuous flow inverse-electron-demand Kondrat’eva reaction has been developed that provides direct access to cycloalka[c]pyridines from unactivated oxazoles and cycloalkenes. The cycloadditions of both unactivated alkenes and deactivated oxazoles are promoted in continuous flow at elevated temperatures and pressures (230 °C, 750psi). E.g., reaction of 5-phenyloxazole and cyclopentene in presence of TFA gave 55% 4-phenyl-6,7-dihydro-5H-cyclopenta[c]pyridine (I). Annulated pyridines obtained by this one-step process are valuable scaffolds for medicinal chem.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Design, Synthesis, and Structure-Activity Relationship of Indole-3-glyoxylamide Libraries Possessing Highly Potent Activity in a Cell Line Model of Prion Disease, published in 2009-12-10, which mentions a compound: 1827-27-6, Name is 5-Amino-2-fluoropyridine, Molecular C5H5FN2, Safety of 5-Amino-2-fluoropyridine.

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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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Shipin Kexue (Beijing, China) called Effect of dissolved oxygen on production of L-cysteine synthetase by Pseudomonas sp. TS1138, Author is Huai, Lihua; Chen, Ning, which mentions a compound: 2150-55-2, SMILESS is O=C(C1N=C(N)SC1)O, Molecular C4H6N2O2S, Name: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

Pseudomonas sp. TS1138 has potential to produce L-cysteine synthetase through asym. hydrolysis of DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC). The effect of dissolved oxygen level on the production of L-cysteine synthetase was investigated in shake flasks or 7 L bioreactor. The results indicated that the cell growth and the production of L-cysteine synthetase were inhibited at low dissolved oxygen level. Although cell growth was improved at the high dissolved oxygen level, the inhibition against production of L-cysteine synthetase was still observed in shake flasks. In 7 L bioreactor, dissolved oxygen concentration controlled at more than 30% was helpful for improving the cell growth and the production of L-cysteine synthetase through regulating agitation rate and air flow rate during the middle and late stage.

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Pyrazine – Wikipedia,
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Name: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Synthesis and study of the anti-inflammatory properties of some pyrazolo[1,5-a]pyrimidine derivatives. Author is Bruni, Fabrizio; Costanzo, Annarella; Selleri, Silvia; Guerrini, Gabriella; Fantozzi, Roberto; Pirisino, Renato; Brunelleschi, Sandra.

A series of pyrazolo[1,5-a]pyrimidin-7-ones I (R = bromophenyl, methoxyphenyl, thienyl, pyridyl, cyclohexyl, Bu, iso-Pr, nitrophenyl, aminophenyl hydrochloride, and ethylpyridinium iodide) were synthesized to evaluate in vivo and in vitro effects induced by structural modifications at the 2 position of 4,7-dihydro-4-ethyl-2-phenylpyrazolo[1,5-a]pyrimidin-7-one (FPP028). This substance, which has been previously studied, is a weak inhibitor of prostaglandin biosynthesis and a nonacid analgesic and anti-inflammatory agent devoid of ulcerogenic properties. To gain more insight into the mechanism of action of this class of compounds, several in vivo tests were carried out, such as carrageenan-induced rat paw edema and pleurisy. In vitro tests include some studies of leukocyte functions, such as superoxide production and myeloperoxidase release. In vitro effects on arachidonic acid-, ADP, and platelet-activating factor-induced platelet aggregation were also studied. Different anti-inflammatory activities were observed, depending on the nature of substituents at the 2 position; these differences are probably linked to the capacity of these compounds to inhibit leukotrienes and/or prostaglandin biosynthesis with different selectivity. 4,7-Dihydro-4-ethyl-2(2-thienyl)pyrazolo[1,5-a]pyrimidin-7-one proved to be the most interesting compound of the novel synthesized series, showing powerful pharmacol. activity in vivo as well as in vitro, together with very weak acute toxicity.

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Pyrazine – Wikipedia,
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Synthetic Route of 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 Simultaneous analysis of 28 urinary VOC metabolites using ultra high performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry (UPLC-ESI/MSMS). Author is Alwis, K. Udeni; Blount, Benjamin C.; Britt, April S.; Patel, Dhrusti; Ashley, David L..

Volatile organic compounds (VOCs) are ubiquitous in the environment, originating from many different natural and anthropogenic sources, including tobacco smoke. Long-term exposure to certain VOCs may increase the risk for cancer, birth defects, and neurocognitive impairment. Therefore, VOC exposure is an area of significant public health concern. Urinary VOC metabolites are useful biomarkers for assessing VOC exposure because of non-invasiveness of sampling and longer physiol. half-lives of urinary metabolites compared with VOCs in blood and breath. We developed a method using reversed-phase ultra high performance liquid chromatog. (UPLC) coupled with electrospray ionization tandem mass spectrometry (ESI/MSMS) to simultaneously quantify 28 urinary VOC metabolites as biomarkers of exposure. We describe a method that monitors metabolites of acrolein, acrylamide, acrylonitrile, benzene, 1-bromopropane, 1,3-butadiene, carbon-disulfide, crotonaldehyde, cyanide, N,N-dimethylformamide, ethylbenzene, ethylene oxide, propylene oxide, styrene, tetrachloroethylene, toluene, trichloroethylene, vinyl chloride and xylene. The method is accurate (mean accuracy for spiked matrix ranged from 84 to104%), sensitive (limit of detection ranged from 0.5 to 20 ng mL-1) and precise (the relative standard deviations ranged from 2.5 to 11%). We applied this method to urine samples collected from 1203 non-smokers and 347 smokers and demonstrated that smokers have significantly elevated levels of tobacco-related biomarkers compared to non-smokers. We found significant (p < 0.0001) correlations between serum cotinine and most of the tobacco-related biomarkers measured. These findings confirm that this method can effectively quantify urinary VOC metabolites in a population exposed to volatile organics There are many compounds similar to this compound(2150-55-2)Synthetic Route of C4H6N2O2S. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Comparison of cyanide exposure markers in the biofluids of smokers and non-smokers. Author is Vinnakota, Chakravarthy V.; Peetha, Naga S.; Perrizo, Mitch G.; Ferris, David G.; Oda, Robert P.; Rockwood, Gary A.; Logue, Brian A..

Cyanide is highly toxic and is present in many foods, combustion products (e.g. cigarette smoke), industrial processes, and has been used as a terrorist weapon. In this study, cyanide and its major metabolites, thiocyanate and 2-amino-2-thiazoline-4-carboxylic acid (ATCA), were analyzed from various human biofluids of smokers (low-level chronic cyanide exposure group) and non-smokers to gain insight into the relationship of these biomarkers to cyanide exposure. The concentrations of each biomarker tested were elevated for smokers in each biofluid. Significant differences (p < 0.05) were found for thiocyanate in plasma and urine, and ATCA showed significant differences in plasma and saliva. Addnl., biomarker concentration ratios, correlations between markers of cyanide exposure, and other statistical methods were performed to better understand the relationship between cyanide and its metabolites. Of the markers studied, the results indicate plasma ATCA, in particular, showed excellent promise as a biomarker for chronic low-level cyanide exposure. In addition to the literature in the link below, there is a lot of literature about this compound(2-Amino-4,5-dihydrothiazole-4-carboxylic acid)Recommanded Product: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, illustrating the importance and wide applicability of this compound(2150-55-2).

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Product Details of 2150-55-2. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Continuous L-cysteine production using immobilized cell reactors and product extractors. Author is Ryu, Ok Hee; Ju, Jae Yeong; Shin, Chul Soo.

Methods to improve the stability of L-cysteine-producing enzymes from Pseudomonas sp. M-38, both as whole cells and as immobilized cells, were investigated for the production of L-cysteine from DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC). Among the 3 L-cysteine-producing enzymes, only L-ATC hydrolase was unstable. However, the stability of L-ATC hydrolase was significantly enhanced by the addition of 20% sorbitol. In continuous L-cysteine production, >60% of the initial activity of L-ATC hydrolase remained after 1000 h at 37° with 40% sorbitol and at 30° with 20% sorbitol. A system involving a cascade of processes using 2 packed-bed reactors with immobilized cells and 2 L-cysteine extractors with the ion-exchange resin Dowex 50W was developed to reduce product inhibition and unreacted substrate. The overall productivity of the system was 43% higher than for 2 reactors without an ion-exchange extractor.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthetic Route of C5H5FN2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Synthesis of 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones via directed lithiation of 2-substituted 5-aminopyridine derivatives.

Directed lithiation of Boc or pivaloyl derivatives of 2-substituted 5-aminopyridines I (R = Cl, F, OMe, R1 = COnCMe3, X = H, n = 1, 2) with BuLi-TMEDA in di-Et ether at -10°C gave 4-lithio derivatives which were quenched with CO2 to give the analogous C-4 carboxylic acids I (X = CO2H). Hydrolysis of the protecting groups with either TFA or aqueous KOH gave 2-substituted 5-aminopyridine-4-carboxylic acids I (R1 = H, X = CO2H) which were converted to 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones II by reaction with formamide or, more optionally, formamidine acetate. Boc protected aminopyridines provided the best overall results, with synthesis of these derivatives best achieved by direct reaction of the aminopyridine with di-tert-Bu dicarbonate in the absence of added base.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem