Tag: M.W=100-200

Recommanded Product: 118994-89-1. 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: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Discovery of Novel 1,4-Diacylpiperazines as Selective and Cell-Active eIF4A3 Inhibitors. Author is Ito, Masahiro; Tanaka, Toshio; Cary, Douglas R.; Iwatani-Yoshihara, Misa; Kamada, Yusuke; Kawamoto, Tomohiro; Aparicio, Samuel; Nakanishi, Atsushi; Imaeda, Yasuhiro.

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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Quality Control of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. 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: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Enzymatic characteristics in the bioconversion of D,L-ATC to L-cysteine. Author is Ryu, Ok Hee; Shin, Chul Soo.

The bioconversion of DL-2-aminothiazoline-4-carboxylic acid (I) to L-cysteine (II) was investigated. After the intracellular enzyme of a Pseudomonas species was inducibly formed by addition of I in the middle of culture, the cells were isolated and treated with sonication to prepare the crude enzyme solution I was the only isomeric form of the amino acid produced from I and its production could be enhanced several 10-fold by addition of Mn2+ which was required as a cofactor in the enzymic reaction. In addition, this reaction suffered from feedback inhibition of II. On the other hand, since a II-decomposing enzyme coexisted in the crude enzyme solution, most of the II formed disappeared in the absence of its inhibitor. However, hydroxylamine was a potent inhibitor which could successfully prevent the decomposition of II.

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Pyrazine – Wikipedia,
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Safety of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. 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 Cloning, expression, and identification of genes involved in the conversion of DL-2-amino-Δ2-thiazoline-4-carboxylic acid to L-cysteine via S-carbamyl-L-cysteine pathway in Pseudomonas sp. TS1138. Author is Yu, Yangsheng; Liu, Zhong; Liu, Chunqin; Li, Yang; Jin, Yongjie; Yang, Wenbo; Bai, Gang.

Two novel genes (tsB, tsC) involved in the conversion of DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) to L-cysteine through S-carbamyl-L-cysteine (L-SCC) pathway were cloned from the genomic DNA library of Pseudomonas sp. TS1138. The recombinant proteins of these two genes were expressed in Escherichia coli BL21, and their enzymic activity assays were performed in vitro. It was found that the tsB gene encoded an L-ATC hydrolase, which catalyzed the conversion of L-ATC to L-SCC, while the tsC gene encoded an L-SCC amidohydrolase, which showed the catalytic ability to convert L-SCC to L-cysteine. These results suggest that tsB and tsC play important roles in the L-SCC pathway and L-cysteine biosynthesis in Pseudomonas sp. TS1138, and that they have potential applications in the industrial production of L-cysteine.

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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 biological evaluation of indole-2-carboxylic acid derivatives as IDO1/TDO dual inhibitors, published in 2020-02-15, which mentions a compound: 1827-27-6, Name is 5-Amino-2-fluoropyridine, Molecular C5H5FN2, Product Details of 1827-27-6.

Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are involved in the key steps of tryptophan metabolism and are potential new targets for tumor immunotherapy. In this work, a variety of indole-2-carboxylic acid derivatives I (R1 = H, 7-F, NHAc, etc.; X = NH, NMe, S; Y = NH, S, -NHCH2-, etc.; Ar = 4-F-3-Cl-C6H3, 4-F-3-OMe-C6H3, 3-Cl-3-OMe-C6H3, etc.) were synthesized, and their inhibitory activities against both enzymes along with structure-activity relationships were investigated. As a result, a number of 6-acetamido-indole-2-carboxylic acid derivatives were found to be potent dual inhibitors with IC50 values at low micromolar levels. Among them, compound I (R1 = 6-NHAc, X = N, Y = NH, Ar = 3,4-di-F-C6H3) was the most potent inhibitor with an IC50 value of 1.17μM for IDO1, and 1.55μM for TDO, resp. In addition, a para-benzoquinone derivative II, resulted from the oxidation of compound I (R1 = 6-NHEt, X = NH, Y = NH, Ar = 4-F-3-Cl-C6H3), was also identified and it showed strong inhibition against the two enzymes with IC50 values at the double digit nanomolar level. Using mol. docking and mol. dynamic simulations, authors predicted the binding modes of this class of compounds within IDO1 and TDO binding pocket. The results provide insights for further structural optimization of this series of IDO1/TDO dual inhibitors.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Palladium-catalyzed deamidative arylation of azoles with arylamides through a tandem decarbonylation-C-H functionalization, the main research direction is azole arylamide palladium chemoselective regioselective deamidative arylation; aryl azole preparation; chemoselective regioselective deamidative arylation catalyst palladium.Safety of Ethyl oxazole-5-carboxylate.

A highly chemo-, regio-selective, and efficient palladium-catalyzed deamidative arylation of azoles with arylamides, as an aryl metal equivalent, has been developed. The reaction proceeds smoothly to generate the corresponding products in good yields via a tandem decarbonylation-C-H activation.

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Pyrazine – Wikipedia,
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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 Enhanced biocatalytic production of L-cysteine by Pseudomonas sp. B-3 with in situ product removal using ion-exchange resin.SDS of cas: 2150-55-2.

Bioconversion of DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) catalyzed by whole cells of Pseudomonas sp. was successfully applied for the production of L-cysteine. It was found, however, like most whole-cell biocatalytic processes, the accumulated L-cysteine produced obvious inhibition to the activity of biocatalyst and reduced the yield. To improve L-cysteine productivity, an anion exchange-based in situ product removal (ISPR) approach was developed. Several anion-exchange resins were tested to select a suitable adsorbent used in the bioconversion of DL-ATC for the in situ removal of L-cysteine. The strong basic anion-exchange resin 201 × 7 exhibited the highest adsorption capacity for L-cysteine and low adsorption for DL-ATC, which is a favorable option. With in situ addition of 60 g L-1 resin 201 × 7, the product inhibition can be reduced significantly and 200 mmol L-1 of DL-ATC was converted to L-cysteine with 90.4 % of yield and 28.6 mmol L-1 h-1 of volumetric productivity. Compared to the bioconversion without the addition of resin, the volumetric productivity of L-cysteine was improved by 2.27-fold using ISPR method.

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Pyrazine – Wikipedia,
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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid( cas:2150-55-2 ) is researched.Name: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.Yang, Bo; Liu, Zhigang; Deng, Bei; Zeng, Yulei; Hu, Jiajun; Li, Weilin; Hu, Zheng published the article 《Isolation and genetic improvement of Pseudomonas sp. strain HUT-78, capable of enzymatic production of L-cysteine from DL-2-amino-Δ2-thiazoline-4-carboxylic acid》 about this compound( cas:2150-55-2 ) in Journal of General and Applied Microbiology. Keywords: cysteine production Pseudomonas fermentation mutagenesis genetic engineering; aminothiazolinecarboxylate hydrolase carbamoylcysteine amidohydrolase Pseudomonas. Let’s learn more about this compound (cas:2150-55-2).

Microorganisms able to bioconvert DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) into L-cysteine were originally isolated from 10 soil samples with DL-ATC as the sole nitrogen source. Ninety-seven L-cysteine-producing bacterial strains were screened out and obtained in pure culture. Among them, a strain, designated as HUT-78, was selected as the best producer, with a molar bioconversion rate of 60%. Based on the 16S rRNA gene sequence anal., this isolate was placed within the genus Pseudomonas. A novel mutant of this strain with a significantly reduced activity of L-cysteine desulfhydrase, a L-cysteine-decomposing enzyme, was derived by UV-mutagenesis. This mutant, designated as mHUT-78, exhibited a 42% increase in L-cysteine producing activity. Moreover, the bioconversion reactions in both the parent and the mutant strain were significantly accelerated by co-overexpression of the two key enzymes, AtcB and AtcC, involved in the bioconversion reaction.

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Pyrazine – Wikipedia,
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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 One-pot synthesis of DL-2-amino-2-thiazoline-4-carboxylic acid, the main research direction is chloropropionic acid reaction thiourea; aminothiazoline carboxylic acid preparation.Quality Control of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

DL-2-Amino-2-thiazoline-4-carboxylic acid was prepared in one-pot reaction from 2,3-dichloropropionic acid. Not only the procedure was simplified, but also the yield was increased from less than 63% recorded to 93%.

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Pyrazine – Wikipedia,
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Computed Properties of C4H6N2O2S. 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: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Quantification of 2-aminothiazoline-4-carboxylic acid as a reliable marker of cyanide exposure using chemical derivatization followed by liquid chromatography-tandem mass spectrometry.

In this research, we have developed a novel and simple liquid chromatog. coupled with electrospray ionization-tandem mass spectrometry (LC/ESI-MS/MS) method for quantification of 2-aminothiazoline-4-carboxylic acid (ATCA), which is produced by the direct reaction of cyanide (CN) with endogenous cystine. In forensic science, detection of CN is important because CN is a poison that is often used for murder or suicide, in addition to being produced by the thermal decomposition of natural or synthetic materials. However, because CN disappears rapidly from body tissue, ATCA is thought to be a more reliable indicator of CN exposure. For the method reported herein, human blood samples (20μL) were subjected to protein precipitation followed by derivatization with 4-bromoethyl-7-methoxycoumarin. Blood spiked with ATCA at concentrations ranging from 50 to 1500 ng/mL was used to prepare a calibration curve (lower limit of quantification; 50 ng/mL, lower limit of detection; 25 ng/mL). Our method uses chem. derivatization, so unlike previously reported methods, it does not require tedious pretreatment procedures, hydrophilic interaction liquid chromatog. columns, or specialized equipment. In addition, our method allows for repeatable and accurate quantification of ATCA, with intra- and inter-assay coefficients of variation of below 5.0% and below 6.0%, resp. We used the method to analyze ATCA in postmortem human blood samples, including samples from people who had intentionally ingested CN or were fire victims. Blood ATCA concentrations were higher among people who had ingested CN or were fire victims than among people in a control group (P < 0.0001). The data reported herein demonstrate that our LC/ESI-MS/MS method can be used to detect and quantify ATCA in postmortem blood samples and that CN exposure strongly affects ATCA concentration, providing a useful tool for detection of CN poisoning. Although many compounds look similar to this compound(2150-55-2)Computed Properties of C4H6N2O2S, numerous studies have shown that this compound(SMILES:O=C(C1N=C(N)SC1)O), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

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Rewcastle, Gordon W.; Denny, William A.; Winters, R. Thomas; Colbry, Norman L.; Showalter, H. D. Hollis published the article 《Synthesis of 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones via directed lithiation of 2-substituted 5-aminopyridine derivatives》. Keywords: pyridopyrimidinone preparation; pyrimidinone pyrido preparation; aminopyridine lithiation carboxylation.They researched the compound: 5-Amino-2-fluoropyridine( cas:1827-27-6 ).Synthetic Route of C5H5FN2. 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:1827-27-6) here.

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,
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