Month: April 2022

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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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

COA of Formula: C4H5N3. 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: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Discovery, synthesis and optimization of an N-alkoxy indolylacetamide against HIV-1 carrying NNRTI-resistant mutations from the Isatis indigotica root. Author is Xu, Chengbo; Xin, Yijing; Chen, Minghua; Ba, Mingyu; Guo, Qinglan; Zhu, Chenggen; Guo, Ying; Shi, Jiangong.

From an aqueous decoction of the traditional Chinese medicine “”ban lan gen”” (the Isatis indigotica root), an antiviral natural product I [R1 = Me; R2 = 2-CO2Me; n = 1] was isolated as an NNRTI (non-nucleoside reverse transcriptase inhibitor) (EC50 = 3.40μM). Its novel structure was determined as Me (1-methoxy-1H-indol-3-yl)acetamidobenzoate I [R1 = Me; R2 = 2-CO2Me; n = 1] by spectroscopic data and confirmed by single crystal X-ray diffraction. Through synthesis and structure-activity relationship (SAR) investigation of compound I [R1 = Me; R2 = 2-CO2Me; n = 1] and 57 new derivatives I [R1 = Me, n-Pr, Bn, etc.; R2 = Ph, 2-ClC6H4, 2-pyridyl, etc.; n = 1,2,3] (24 with EC50 values of 0.06-8.55μM), two optimized derivatives I [R1 = n-Pr, n-Bu; R2 = 3-chloro-4-pyridyl; n = 1] (EC50: 0.06μM and 0.06μM) having activity comparable to that of NVP (EC50 = 0.03μM) were obtained. Further evaluation verified that compounds I [R1 = n-Pr, n-Bu; R2 = 3-chloro-4-pyridyl; n = 1] were RT DNA polymerase inhibitors and exhibited better activities and drug resistance folds compared to NVP against seven NNRTI-resistant strains carrying different mutations. Especially, compound I [R1 = n-Bu; R2 = 3-chloro-4-pyridyl; n = 1] (EC50 = 0.43μM) was more active to the L100I/K103N double-mutant strain as compared to both NVP (EC50 = 0.76μM) and EFV (EC50 = 1.08μM). The mol. docking demonstrated a possible binding pattern between compound I [R1 = n-Bu; R2 = 3-chloro-4-pyridyl; n = 1] and RT and revealed activity mechanism of compound I [R1 = n-Bu; R2 = 3-chloro-4-pyridyl; n = 1] against the NNRTI-resistant strains.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Singh, Baljinder; Diaz-Gonzalez, Rosario; Ceballos-Perez, Gloria; Rojas-Barros, Domingo I.; Gunaganti, Naresh; Gillingwater, Kirsten; Martinez-Martinez, Maria Santos; Manzano, Pilar; Navarro, Miguel; Pollastri, Michael P. published an article about the compound: 4-Aminopyrimidine( cas:591-54-8,SMILESS:C1=CN=CN=C1N ).Formula: C4H5N3. 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:591-54-8) through the article.

Human African trypanosomiasis (HAT), or sleeping sickness, is caused by the protozoan parasite Trypanosoma brucei and transmitted through the bite of infected tsetse flies. The disease is considered fatal if left untreated. To identify new chemotypes against Trypanosoma brucei, previously we identified 797 potent kinase-targeting inhibitors grouped into 59 clusters plus 53 singleton compounds with at least 100-fold selectivity over HepG2 cells. From this set of hits, a cluster of diaminopurine-derived compounds was identified. Herein, we report our medicinal chem. investigation involving the exploration of structure-activity and structure-property relationships around one of the high-throughput screening (HTS) hits, N2-(thiophen-3-yl)-N6-(2,2,2-trifluoroethyl)-9H-purine-2,6-diamine (1, NEU-1106). This work led to the identification of a potent lead compound (4aa, NEU-4854) with improved in vitro absorption, distribution, metabolism, and excretion (ADME) properties, which was progressed into proof-of-concept translation of in vitro antiparasitic activity to in vivo efficacy.

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Reference:
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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Reference:
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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Reference:
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: 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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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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.Lee, H. H.; Palmer, B. D.; Wilson, W. R.; Denny, W. A. researched the compound: 4-Bromo-1-methyl-2-nitro-1H-imidazole( cas:121816-79-3 ).Category: pyrazines.They published the article 《Synthesis and hypoxia-selective cytotoxicity of a 2-nitroimidazole mustard》 about this compound( cas:121816-79-3 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: chloroethylaminonitroimidazole preparation hypoxia selective cytotoxicity; nitroimidazole mustard preparation hypoxia selective cytotoxicity; imidazole chloroethylaminonitro preparation hypoxia selective cytotoxicity. We’ll tell you more about this compound (cas:121816-79-3).

A four-step synthesis of 5-[N,N-bis(2-chloroethyl)amino]-1-methyl-2-nitroimidazole from 1-methyl-2-nitroimidazole is described. This compound showed similar hypoxia-selective cytotoxicity to the dinitrobenzamide mustard SN 23862 in UV4 cells (ca. 40-fold), and superior selectivity (>7-fold) in repair-competent AA8 cells.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthetic Route of C4H5N3. 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: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Synthetic Strategies of Pyrimidine-Based Scaffolds as Aurora Kinase and Polo-like Kinase Inhibitors. Author is Jadhav, Mrunal; Sankhe, Kaksha; Bhandare, Richie R.; Edis, Zehra; Bloukh, Samir Haj; Khan, Tabassum Asif.

A review. Small mols. containing heterocyclic moieties have attracted considerable interest for designing new antitumor agents. Of these, the pyrimidine ring system is found in multitude of drug structures, and being the building unit of DNA and RNA makes it an attractive scaffold for the design and development of anticancer drugs. Currently, 22 pyrimidine-containing entities are approved for clin. use as anticancer drugs by the FDA. An exhaustive literature search indicates several publications and more than 59 patents from the year 2009 onwards on pyrimidine derivatives exhibiting potent antiproliferative activity. These pyrimidine derivatives exert their activity via diverse mechanisms, one of them being inhibition of protein kinases. Aurora kinase (AURK) and polo-like kinase (PLK) are protein kinases involved in the regulation of the cell cycle. Within the numerous pyrimidine-based small mols. developed as anticancer agents, this review focuses on the pyrimidine fused heterocyclic compounds modulating the AURK and PLK proteins in different phases of clin. trials as anticancer agents. This article aims to provide a comprehensive overview of synthetic strategies for the preparation of pyrimidine derivatives and their associated biol. activity on AURK/PLK. It will also present an overview of the synthesis of the heterocyclic-2-aminopyrimidine, 4-aminopyrimidine and 2,4-diaminopyrimidine scaffolds, and one of the pharmacophores in AURK/PLK inhibitors is described systematically.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Tshala-Katumbay, Desire D.; Ngombe, Nadege N.; Okitundu, Daniel; David, Larry; Westaway, Shawn K.; Boivin, Michael J.; Mumba, Ngoyi D.; Banea, Jean-Pierre published an article about the compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid( cas:2150-55-2,SMILESS:O=C(C1N=C(N)SC1)O ).HPLC of Formula: 2150-55-2. 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:2150-55-2) through the article.

A review. Threats by fundamentalist leaders to use chem. weapons have resulted in renewed interest in cyanide toxicity. Relevant insights may be gained from studies on cyanide mass intoxication in populations relying on cyanogenic cassava as the main source of food. In these populations, sublethal concentrations (up to 80 μmol/l) of cyanide in the blood are commonplace and lead to signs of acute toxicity. Long-term toxicity signs include a distinct and irreversible spastic paralysis, known as konzo, and cognition deficits, mainly in sequential processing (visual-spatial anal.) domains. Toxic culprits include cyanide (mitochondrial toxicant), thiocyanate (AMPA-receptor chaotropic cyanide metabolite), cyanate (protein-carbamoylating cyanide metabolite), and 2-iminothiazolidine-4-carboxylic acid (seizure inducer). Factors of susceptibility include younger age, female gender, protein-deficient diet, and, possibly, the gut functional metagenome. The existence of uniquely exposed and neurol. affected populations offers invaluable research opportunities to develop a comprehensive understanding of cyanide toxicity and test or validate point-of-care diagnostic tools and treatment options to be included in preparedness kits in response to cyanide-related threats.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem