Tag: M.W=100-200

Related Products of 91912-53-7. 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: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine, is researched, Molecular C8H8N4, CAS is 91912-53-7, about Novel pyrazolopyrimidines as highly potent B-Raf inhibitors.

A novel series of pyrazolo[1,5-a]pyrimidines bearing a 3-hydroxyphenyl group at C(3) and substituted tropanes at C(7) have been identified as potent B-Raf inhibitors. Exploration of alternative functional groups as a replacement for the C(3) phenol demonstrated indazole to be an effective isostere. Several compounds possessing substituted indazole residues, such as 4e, 4p, and 4r, potently inhibited cell proliferation at submicromolar concentrations in the A375 and WM266 cell lines, and the latter two compounds also exhibited good therapeutic indexes in cells.

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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: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Bioconversion of D,L-ATC to L-cysteine using whole cells.Computed Properties of C4H6N2O2S.

In the conversion of D,L-2-amino-Δ2-thiazoline-4-carboxylic acid (D,L-ATC) to L-cysteine using Pseudomonas species CU6, the effects of surfactants on whole cells and the stabilities of cell-free enzyme solution and continuous reactor packed with immobilized whole cells were investigated. The enzymic reaction was minimal by whole cells without the addition of surfactants, whereas it was well carried out with SDS or Triton X-100 and was comparable to the reaction using a cell-free enzyme solution The enzyme activity of the cell-free solution decreased 50% after 7 h of storage at 30°, but not under anaerobic conditions with sparging nitrogen gas. On the other hand, there were no effects of nitrogen gas in a continuous reactor using immobilized whole cells. Hydroxylamine, an inhibitor of L-cysteine desulfhydrase, lowered the enzyme stability.

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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 Highly Enantioselective Mukaiyama Aldol Reactions Catalyzed by a Chiral Oxazaborolidinium Ion: Total Synthesis of (-)-Inthomycin C, Author is Senapati, Bidyut Kumar; Gao, Lizhu; Lee, Sung Il; Hwang, Geum-Sook; Ryu, Do Hyun, the main research direction is enantioselective synthesis beta hydroxy ester Mukaiyama aldol reaction aldehyde; inthomycin c enantioselective synthesis Mukaiyama aldol reaction.Electric Literature of C6H7NO3.

A cationic oxazaborolidinium-catalyzed asym. Mukaiyama aldol reaction of (1-methoxy-2-methyl-propenyloxy)-trimethylsilane with various aldehydes including α,β-disubstituted acroleins has been developed in high yields and enantioselectivities. The synthetic utility of this methodol. was demonstrated in the first short synthesis of naturally occurring inthomycin C (I) in high enantio-purity.

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Computed Properties 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 RECiQ: A Rapid and Easy Method for Determining Cyanide Intoxication by Cyanide and 2-Aminothiazoline-4-carboxylic Acid Quantification in the Human Blood Using Probe Electrospray Ionization Tandem Mass Spectrometry. Author is Hisatsune, Kazuaki; Murata, Tasuku; Ogata, Koretsugu; Hida, Minemasa; Ishii, Akira; Tsuchihashi, Hitoshi; Hayashi, Yumi; Zaitsu, Kei.

In this study, we developed a rapid and easy method to determine cyanide (CN) intoxication by quantification of CN and 2-aminothiazoline-4-carboxylic acid (ATCA), which is a new and reliable indicator of CN exposure, in the human blood using probe electrospray ionization tandem mass spectrometry (PESI/MS/MS) named RECiQ. For CN, we applied the previously reported one-pot derivatization method using 2,3-naphthalene-dialdehyde and taurine, which can directly derivatize CN in the blood. The anal. conditions of the CN derivatization were optimized as a 10 min reaction time at room temperature In contrast, ATCA could be directly detected in the blood by PESI/MS/MS. We developed quant. methods for the derivatized CN and ATCA using an internal standard method and validated them using quality control samples, demonstrating that the linearities of each calibration curve were greater than 0.995, and intra- and interday precisions and accuracies were 5.1-15 and 1.1-14%, resp. Moreover, the lower limit of detections for CN and ATCA were 42 and 43 ng/mL, resp. Finally, we applied RECiQ to three postmortem blood specimens obtained from victims of fire incidents, which resulted in the successful quantification of CN and ATCA in all samples. As PESI/MS/MS can be completed within 0.5 min, and the sample volume requirement of RECiQ is only 2μL of blood, these methods are useful not only for the rapid determination of CN exposure but also for the estimation of the CN intoxication levels during an autopsy.

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Quality Control of Ethyl oxazole-5-carboxylate. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Selective Inhibition of Collagen Prolyl 4-Hydroxylase in Human Cells. Author is Vasta, James D.; Andersen, Kristen A.; Deck, Kathryn M.; Nizzi, Christopher P.; Eisenstein, Richard S.; Raines, Ronald T..

Collagen is the most abundant protein in animals. Its overproduction is associated with fibrosis and cancer metastasis. The stability of collagen relies on posttranslational modifications, the most prevalent being the hydroxylation of collagen strands by collagen prolyl 4-hydroxylases (CP4Hs). Catalysis by CP4Hs enlists an iron cofactor to convert proline residues to 4-hydroxyproline residues, which are essential for the conformational stability of mature collagen. Et 3,4-dihydroxybenzoate (EDHB) is commonly used as a “”P4H”” inhibitor in cells, but suffers from low potency, poor selectivity, and off-target effects that cause iron deficiency. Dicarboxylates of 2,2′-bipyridine are among the most potent known CP4H inhibitors but suffer from a high affinity for free iron. A screen of biheteroaryl compounds revealed that replacing one pyridyl group with a thiazole moiety retains potency and enhances selectivity. A diester of 2-(5-carboxythiazol-2-yl)pyridine-5-carboxylic acid is bioavailable to human cells and inhibits collagen biosynthesis at concentrations that neither cause general toxicity nor disrupt iron homeostasis. These data anoint a potent and selective probe for CP4H and a potential lead for the development of a new class of antifibrotic and antimetastatic agents.

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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: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Optimization of bioconversion conditions for manufacturing L-cysteine from DL-2-amino-Δ2-thiazoline-4-carboxylic acid with immobilized cells based on response surface analysis.Quality Control of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

The conversion conditions for manufacturing L-cysteine using immobilized cells were optimized by using SAS software combined with the methods of Plackett-Burman design and response surface methodol. The cells were immobilized by calcium alginate embedding method. The optimum levels of three important factors were determined as follows: the volume of immobilized cell was 25.5 mL, the concentration of DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) was 1.0 mass%, and the proliferation time of immobilized cells was 12.9 h. Experiments showed that the average enzyme activity could reach 934 U/mL at optimized conditions for five batches, with an increase of 38.9% compared with that before the optimization. After the immobilized cells were utilized for 4 times, the conversion rate could be still over 91.0% of the initial value.

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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: 2150-55-2, is researched, Molecular C4H6N2O2S, about N-carbamoyl-L-cysteine as an intermediate in the bioconversion from D,L-2-amino-Δ2-thiazoline-4-carboxylic acid to L-cysteine by Pseudomonas sp. ON-4a, the main research direction is Pseudomonas carbamoylcysteine; 2-amino-Δ 2-thiazoline-4-carboxylic acid (ATC); L-cysteine; N-carbamoyl-L-cysteine (L-NCC); Pseudomonas species; bioconversion.COA of Formula: C4H6N2O2S.

The authors investigated the conversion of D,L-2-amino-Δ2-thiazoline-4-carboxylic (D,L-ATC) to L-cysteine with Pseudomonas sp. ON-4a, an ATC-assimilating bacterium. Cysteine and N-carbamoylcysteine (NCC), but not S-carbamoylcysteine (SCC), were produced from D,L-ATC by a cell-free extract from the strain. These products were isolated from the reaction mixture and then identified as the L-form. Similar results were obtained with P. putida AJ3865 and unidentified strain TG-3, an ATC-assimilating bacteria. It became clear that L-NCC is an intermediate in the conversion of D,L-ATC to L-cysteine in these Pseudomonas strains. Furthermore, it was suggested that these bacteria have L-ATC hydrolase and L-NCC amidohydrolase.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Kinetics of the cyanide-cystine reaction》. Authors are Gawron, Oscar; Fernando, Joseph.The article about the compound:2-Amino-4,5-dihydrothiazole-4-carboxylic acidcas:2150-55-2,SMILESS:O=C(C1N=C(N)SC1)O).Safety of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. Through the article, more information about this compound (cas:2150-55-2) is conveyed.

The kinetics of the cystine-cyanide reaction was studied in 0.04M KOH at pH 12.5 by a spectrophotometric method. The reaction was bimol., with cyclization of the thiocyanato product much faster than the reverse reaction. Activation parameters at 35° were: Ea, 16.8 kcal./mole; ΔH*, 16.1 kcal./mole; and ΔS*, -7.4 e.u. The entropy of activation was about the same as that for the cyanide-S8 reaction but about 20 e.u. less than that for the cystine-SO3–reaction; this indicated the activated complex for cystine-SO3– is more crowded than that for cystine-CN-.

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Ito, Masahiro; Tanaka, Toshio; Cary, Douglas R.; Iwatani-Yoshihara, Misa; Kamada, Yusuke; Kawamoto, Tomohiro; Aparicio, Samuel; Nakanishi, Atsushi; Imaeda, Yasuhiro published the article 《Discovery of Novel 1,4-Diacylpiperazines as Selective and Cell-Active eIF4A3 Inhibitors》. Keywords: diacyl piperazine derivative preparation eIF4A3 inhibitor structure cancer.They researched the compound: Ethyl oxazole-5-carboxylate( cas:118994-89-1 ).Safety of Ethyl oxazole-5-carboxylate. 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:118994-89-1) here.

Eukaryotic initiation factor 4A3 (eIF4A3), a member of the DEAD-box RNA helicase family, is one of the core components of the exon junction complex (EJC). The EJC is known to be involved in a variety of RNA metabolic processes typified by nonsense-mediated RNA decay (NMD). In order to identify mol. probes to investigate the functions and therapeutic relevance of eIF4A3, a search for selective eIF4A3 inhibitors was conducted. Through the chem. optimization of 1,4-diacylpiperazine derivatives identified via high-throughput screening (HTS), we discovered the first reported selective eIF4A3 inhibitor 53a exhibiting cellular NMD inhibitory activity. A surface plasmon resonance (SPR) biosensing assay ascertained the direct binding of 53a and its analog 52a to eIF4A3 and revealed that the binding occurs at a non-ATP binding site. Compounds 52a and 53a represent novel mol. probes for further study of eIF4A3, the EJC, and NMD.

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Electric Literature of C4H6N2O2S. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Cyanide Toxicokinetics: The Behavior of Cyanide, Thiocyanate and 2-Amino-2-Thiazoline-4-Carboxylic Acid in Multiple Animal Models. Author is Bhandari, Raj K.; Oda, Robert P.; Petrikovics, Ilona; Thompson, David E.; Brenner, Matthew; Mahon, Sari B.; Bebarta, Vikhyat S.; Rockwood, Gary A.; Logue, Brian A..

Cyanide causes toxic effects by inhibiting cytochrome c oxidase, resulting in cellular hypoxia and cytotoxic anoxia, and can eventually lead to death. Cyanide exposure can be verified by direct anal. of cyanide concentrations or analyzing its metabolites, including thiocyanate (SCN-) and 2-amino-2-thiazoline-4-carboxylic acid (ATCA) in blood. To determine the behavior of these markers following cyanide exposure, a toxicokinetics study was performed in three animal models: (i) rats (250-300 g), (ii) rabbits (3.5-4.2 kg) and (iii) swine (47-54 kg). Cyanide reached a maximum in blood and declined rapidly in each animal model as it was absorbed, distributed, metabolized and eliminated. Thiocyanate concentrations rose more slowly as cyanide was enzymically converted to SCN-. Concentrations of ATCA did not rise significantly above the baseline in the rat model, but rose quickly in rabbits (up to a 40-fold increase) and swine (up to a 3-fold increase) and then fell rapidly, generally following the relative behavior of cyanide. Rats were administered cyanide s.c. and the apparent half-life (t1/2) was determined to be 1,510 min. Rabbits were administered cyanide i.v. and the t1/2 was determined to be 177 min. Swine were administered cyanide i.v. and the t1/2 was determined to be 26.9 min. The SCN- t1/2 in rats was 3,010 min, but was not calculated in rabbits and swine because SCN- concentrations did not reach a maximum The t1/2 of ATCA was 40.7 and 13.9 min in rabbits and swine, resp., while it could not be determined in rats with confidence. The current study suggests that cyanide exposure may be verified shortly after exposure by determining significantly elevated cyanide and SCN- in each animal model and ATCA may be used when the ATCA detoxification pathway is significant.

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