Tag: M.W=100-200

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, Bioscience, Biotechnology, and Biochemistry called Identification, cloning, and sequencing of the genes involved in the conversion of D,L-2-amino-Δ2-thiazoline-4-carboxylic acid to L-cysteine in Pseudomonas sp. strain ON-4a, Author is Ohmachi, Tetsuo; Nishino, Mizuka; Kawata, Maki; Edo, Namiko; Funaki, Hiroko; Narita, Megumi; Mori, Kazuyuki; Tamura, Yoshiharu; Asada, Yoshihiro, the main research direction is Pseudomonas aminothiazoline carboxylate hydrolase gene sequence; carbamoyl amino acid amidase gene sequence Pseudomonas.Recommanded Product: 2150-55-2.

The newly isolated strain Pseudomonas sp. ON-4a converts D,L-2-amino-Δ2-thiazoline-4-carboxylic acid (D,L-ATC) to L-cysteine via N-carbamoyl-L-cysteine. A genomic DNA fragment from this strain containing the gene(s) encoding enzymes that convert D,L-ATC into L-cysteine was cloned in Escherichia coli. Transformants expressing cysteine-forming activity were selected by growth of an E. coli mutant defective in the cysB gene. A pos. clone, denoted CM1, carrying the plasmid pCM1 with an insert DNA of approx. 3.4 kb was obtained, and the nucleotide sequence of a complementing region was analyzed. Anal. of the sequence found two open reading frames, ORF1 and ORF2, which encoded proteins of 183 and 435 amino acid residues, resp. E. coli DH5α harboring pTrCM1, which was constructed by inserting the subcloned sequence into an expression vector, expressed two proteins of 25 kDa and 45 kDa. From the analyses of crude extracts of E. coli DH5α carrying deletion derivatives of pTrCM1 by sodium dodecyl sulfatepolyacrylamide gel electrophoresis and by enzymic activity, it was found that the 25-kDa protein encoded by ORF1 was the enzyme L-2-amino-Δ2-thiazoline-4-carboxylic acid hydrolase, which catalyzes the conversion of D,L-ATC to N-carbamoyl-L-cysteine, and that the 45-kDa protein encoded by ORF2 was the enzyme N-carbamoyl-L-cysteine amidohydrolase, which catalyzes the conversion of N-carbamoyl-L-cysteine to L-cysteine.

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Pyrazine | C4H4N2 – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《4,6-Dichloro- and 4,5,6-trichloropicolinic acid》. Authors are Graf, Roderich.The article about the compound:3-Chloropicolinamidecas:114080-95-4,SMILESS:O=C(N)C1=NC=CC=C1Cl).Category: pyrazines. Through the article, more information about this compound (cas:114080-95-4) is conveyed.

cf. C. A. 25, 2428. Picolinic acid-HCl (200 g.) and 350 cc. SOCl2, gently boiled 10 days, give 30 g. mono-Cl acid, 100 g. di-Cl acid and 30 g. of a mixture of the di- and tri-Cl acids. That the di-Cl acid is the 4,6-Cl2 derivative is shown by the following reactions: The acid chloride and N2H4.H2O in C6H6 give sec-bis(4,6-dichloropicolinic acid) hydrazide, m. above 300°; the Me ester gives 4,6-dichloropicolinic acid hydrazide, m. 154° (benzal derivative, m. 165°); the azide m. 74° and with absolute EtOH yields 4,6-di-chloro-2-carbethoxypyridine, m. 75°; dilute AcOH gives the 2-NH2 derivative (I), m. 108°; with HI I yields a compound, m. 137°, which may be the 6-iodo-4-chloro derivative The Ac derivative of I n. 218-9°. The diazo solution from I in H2SO4 gives 4,6-dichloro-2-hydroxy-pyridine, m. 151°, and in concentrated HCl gives 2,4,6-trichloropyridine, m. 33°; this also results from 2,6-dichloro-4-aminopyridine. Heating the 4,6-Cl2 acid with 80% H2SO4 8 hrs. gives 4-chloro-6-hydroxypicolinic acid (Seyfferth, J. Chem. Soc. 67, 408(1895). 4,5,6-Trichloropicolinic acid (II), crystallizing with 1 mol. H2O, m. 123°, is obtained pure by distillation of the chloride and then of the Me ester, m. 125°; II and HI with some red P, heated 8 hrs. at 150°, give 5-chloropicolinic acid, m. 170°. The amide of II m. 169°; the Ph ester m. 138°. Heating the Me ester with HI and red P 5 hrs. gives 4-iodo-5-chloropicolinic acid, m. 159° (decomposition); refluxed with SOCl2 for 4 hrs., the I is replaced by Cl, giving 4,5-dichloropicolinic acid, crystals with 1 mol. H2O, m. 179-80° (Ost, J. prakt. Chem. 27, 274(1882)). Refluxing the Me ester with 80% H2SO4 4 hrs. gives 4,5-dichloro-6-hydroxypicolinic acid, crystallizing with 1 mol. H2O, m. 284° (decomposition). 3-Chloropicolinic acid, m. 121°; amide, m. 140°.

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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 Cysteine, the main research direction is review cysteine production enzyme.Application of 2150-55-2.

A review with 21 references on the microbial conversion of DL-2-amino-Δ2-thiazoline-4-carboxylic acid  [2150-55-2] to L-cysteine  [52-90-4] and cystine  [56-89-3]; the enzymic synthesis of L-cysteine from β-chloro-L-alanine  [2731-73-9] and Na2S by pyridoxal phosphate-dependent enzymes; and the synthesis of D-cysteine  [921-01-7] by β-chloro-D-alanine dehydrochlorinase  [78990-65-5].

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SDS of cas: 118994-89-1. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Asymmetric Alkyl and Aryl/Azolation of Alkenes via a Single Cu(I) Complex. Author is Ma, Xiaodong; Zhang, Guozhu.

The copper-catalyzed, highly enantioselective alkyl and aryl/azolation of alkenes was reported. The employment of the chiral carbazole-based bisoxazoline (Cbzbox) ligand was critical to the success of this chem. Anionic tridentate ligands improved the reducibility of copper complexes, facilitating alkyl/aryl radical generation and provided good enantiocontrol in the azolation. The three-component coupling reactions featured mild reaction conditions and tolerate broad range of functional groups. This strategy allowed straightforward introduction of valuable azole functionalities into a elaborated mol. system through direct C-H functionalization.

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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: 1827-27-6, is researched, Molecular C5H5FN2, about 2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics, the main research direction is aminoadipic acid glutamate prostate specific membrane antigen theranostic.Formula: C5H5FN2.

The design and synthesis of prostate specific membrane antigen (PSMA) ligands derived from 2-aminoadipic acid, a building block that has not previously been used to construct PSMA ligands, are reported. The effects of both the linker length and of an N-substituent of our PSMA ligands were probed, and X-ray structures of five of these ligands bound to PSMA were obtained. Among the ligands disclosed herein, I showed the highest inhibitory activity for PSMA. As ligand I can readily be radiolabeled since its fluorine atom is adjacent to the nitrogen atom of its pyridine ring, the use of this and related compounds as theranostics can be pursued.

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Application of 1827-27-6. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as IDO1/TDO dual inhibitors. Author is Cui, Guonan; Lai, Fangfang; Wang, Xiaoyu; Chen, Xiaoguang; Xu, Bailing.

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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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 Enzymatic production of L-cysteine from DL-2-amino-Δ2-thiazoline-4-carboxylic acid by Pseudomonas thiazolinophilum: optimal conditions for the enzyme formation and enzymatic reaction.Quality Control of 2-Amino-4,5-dihydrothiazole-4-carboxylic acid.

Cultivation of P. thiazolinophilum AJ 3854 for the production of the enzyme which could form L-cysteine [52-90-4] from DL-2-amino-Δ2-thiazoline-4-carboxylic acid (I) [2150-55-2] and the reaction conditions of this enzyme were investigated. This enzyme was inducible, intracellular, and growth-associated A marked inactivation of enzyme was observed, especially in the growing phase, but could be prevented by 1∼10 mM Mn2+ or by I as inducer at the mid-logarithmic phase. Enzymic degradation of L-cysteine (or L-cystine [56-89-3]) formed from I could be prevented by the addition of hydroxylamine or semicarbazide. Thus, L-cysteine and L-cystine were quant. produced from I. Optimal pH and temperature of enzymic reaction were 8.2 and 42° (2 h), resp. A sigmoidal reaction curve was observed when intact cells were used as enzyme source, but sonic treatment of cells made the curve linear.

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Gopalsamy, Ariamala; Ciszewski, Greg; Shi, Mengxiao; Berger, Dan; Hu, Yongbo; Lee, Frederick; Feldberg, Larry; Frommer, Eileen; Kim, Steven; Collins, Karen; Wojciechowicz, Donald; Mallon, Robert published an article about the compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine( cas:91912-53-7,SMILESS:NC1=CC(C2=CC=NC=C2)=NN1 ).Category: pyrazines. 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:91912-53-7) through the article.

Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This strategy led to the identification of lead compound 9 with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.

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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 LC-MS/MS method development and validation for quantitative analyses of 2-aminothiazoline-4-carboxylic acid – a new cyanide exposure marker in post mortem blood.HPLC of Formula: 2150-55-2.

2-Aminothiazoline-4-carboxylic acid (ATCA) is a hydrogen cyanide metabolite that has been found to be a reliable biomarker of cyanide poisoning, because of its long-term stability in biol. material. There are several methods of ATCA determination; however, they are restricted to extraction on mixed mode cation exchange sorbents. To date, there has been no reliable method of ATCA determination in whole blood, the most frequently used material in forensic anal. This novel method for ATCA determination in post mortem specimen includes protein precipitation, and derivatization of interfering compounds and their later extraction with Et acetate. ATCA was quant. analyzed via HPLC-tandem mass spectrometry with pos. electrospray ionization detection using a hydrophilic interaction liquid chromatog. column. The method satisfied all validation criteria and was tested on the real samples with satisfactory results. Therefore, this anal. approach has been proven to be a tool for measuring endogenous levels of ATCA in post mortem specimens. To conclude, a novel, accurate and sensitive method of ATCA determination in post mortem blood was developed. The establishment of the method provides new possibilities in the field of forensic science.

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Bruni, Fabrizio; Selleri, Silvia; Costanzo, Annarella; Guerrini, Gabriella; Ciciani, Giovanna; Costagli, Camilla; Sacco, Cristiana; Donato, Rosa published an article about the compound: 3-(Pyridin-4-yl)-1H-pyrazol-5-amine( cas:91912-53-7,SMILESS:NC1=CC(C2=CC=NC=C2)=NN1 ).Formula: C8H8N4. 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:91912-53-7) through the article.

A series of pyrazolo[1,5-a]pyrido[3,4-e]pyrimidin-6-ones, I (R1 = H, Me, Ph, 2-furyl, etc., R2 = cyano, CO2Et, H, Ph, NO2, Cl, R3, R4 = H, Me), was prepared by a simple synthetic procedure based on the reaction of hydroxylamine or methoxyamine with 2,3-substituted Et 7-dimethylaminovinyl pyrazolo[1,5-a]pyrimidin-6-carboxylates II. The antimicrobial activity of the obtained compounds was evaluated on a series of standard strains of Gram pos., Gram neg. bacteria and fungi. None of the tested compounds showed significant activity.

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Pyrazine – Wikipedia,
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