Pyrimidines

On November 15, 2012, Matyugina, Elena; Khandazhinskaya, Anastasia; Chernousova, Larisa; Andreevskaya, Sofia; Smirnova, Tatiana; Chizhov, Alexander; Karpenko, Inna; Kochetkov, Sergey; Alexandrova, Ludmila published an article.Product Details of 626-48-2 The title of the article was The synthesis and antituberculosis activity of 5′-nor carbocyclic uracil derivatives. And the article contained the following:

A series of new carbocyclic uracil derivatives, e.g. I, were synthesized and evaluated as potential antituberculosis agents. Racemic hydroxy-cyclopentenyl-5-tetradecynyluracil I completely inhibited the growth of Mycobacterium tuberculosis H37Rv in vitro at a concentration of 10 μg/mL. Individual (+) and (-) isomers of the above uracil derivative were isolated and showed the same level of activity against two strains of Mycobacterium tuberculosis: laboratory sensitive (H37Rv) and drug resistant to five top antituberculosis drugs (MS-115). The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Product Details of 626-48-2

The Article related to drug resistance antituberculosis mycobacterium tuberculosis carbocyclic nucleoside preparation, carbocyclic nucleoside uracil preparation antituberculosis hydroxycyclopentenyltetradecynyluracil mycobacterium tuberculosis antibacterial and other aspects.Product Details of 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 1, 2012, Li, Zhenhua; Wu, Danli; Zhong, Weihui published an article.Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine The title of the article was Facile and efficient cyclization of anthranilonitrile to 2,4-dichloroquinazoline by bis(trichloromethyl) carbonate and catalytic amount triphenylphosphine oxide. And the article contained the following:

2,4-Dichloroquinazolines were synthesized by the cyclization of anthranilonitrile using bis(trichloromethyl)carbonate with the aid of catalytic amount of Ph3PO at 120 °C. This method was also applied to the synthesis of 2,4-dichlorothieno[2,3-d]pyrimidine. The plausible mechanism was presented. The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

The Article related to anthranilonitrile chloromethylcarbonate cyclization phenylphosphine oxide catalyst, aminothiophenonitrile chloromethylcarbonate cyclization phenylphosphine oxide catalyst, chloroquinazoline preparation, chlorothienopyrimidine preparation and other aspects.Safety of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Klinke, Glynis; Richter, Sylvia; Monostori, Peter; Schmidt-Mader, Brigitte; Garcia-Cazorla, Angels; Artuch, Rafael; Christ, Stine; Opladen, Thomas; Hoffmann, Georg F.; Blau, Nenad; Okun, Juergen G. published an article in 2020, the title of the article was Targeted cerebrospinal fluid analysis for inborn errors of metabolism on an LC-MS/MS analysis platform.Quality Control of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione And the article contains the following content:

Laboratory investigations of cerebrospinal fluid (CSF) are essential when suspecting an inborn error of metabolism (IEM) involving neurol. features. Available tests are currently performed on different anal. platforms, requiring a large sample volume and long turnaround time, which often delays timely diagnosis. Therefore, it would be preferable to have an one-instrument targeted multi-metabolite approach. A liquid chromatog.-tandem mass spectrometry (LC-MS/MS) platform, based on two different methods for analyzing 38 metabolites using pos. and neg. electrospray ionisation modes, was established. To allow for platform extension, both methods were designed to use the same CSF sample preparation procedure and to be run on the same separation column (ACE C18-PFP). Assessment of the LC-MS/MS platform methods was first made by anal. validation, followed by the establishment of literature-based CSF cut-off values and reference ranges, and by the measurement of available samples obtained from patients with confirmed diagnoses of aromatic -amino acid decarboxylase deficiency, guanidinoacetate methyltransferase deficiency, ornithine aminotransferase deficiency, cerebral folate deficiency and methylenetetrahydrofolate reductase deficiency. An extendable targeted LC-MS/MS platform was developed for the anal. of multiple metabolites in CSF, thereby distinguishing samples from patients with IEM from non-IEM samples. Reference concentrations for several biomarkers in CSF are provided for the first time. By measurement on a single anal. platform, less sample volume is required (200μL), diagnostic results are obtained faster, and preanal. issues are reduced. LC-MS/MS platform for CSF anal. consisting of two differentially designed methods. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Quality Control of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

The Article related to cerebrospinal fluid inborn error metabolism lcms ms analysis, cerebrospinal fluid, inborn errors of metabolism, inherited metabolic diseases, liquid chromatography coupled to tandem mass spectrometry, reference ranges, targeted metabolomics and other aspects.Quality Control of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On November 30, 2019, Garlito, Borja; Ibanez, Maria; Portoles, Tania; Serrano, Roque; Amlund, Heidi; Lundebye, Anne-Katrine; Sanden, Monica; Berntssen, Marc H. G.; Hernandez, Felix published an article.Formula: C5H6N2O2 The title of the article was LC-MS/MS method for the determination of organophosphorus pesticides and their metabolites in salmon and zebrafish fed with plant-based feed ingredients. And the article contained the following:

The composition of Atlantic salmon feed has changed considerably over the last two decades from being marine-based (fishmeal and fish oil) to mainly containing plant ingredients. Consequently, concern related to traditional persistent contaminants typically associated with fish-based feed has been replaced by other potential contaminants not previously associated with salmon farming. This is the case for many pesticides, which are used worldwide to increase food production, and may be present in plant ingredients. Earlier studies have identified two organophosphorus pesticides, chlorpyrifos-Me and pirimiphos-Me, in plant ingredients used for aquafeed production In the present study, we developed a reliable and sensitive anal. method, based on liquid chromatog. coupled to tandem mass spectrometry, for the determination of these pesticides and their main metabolites in warm water (zebrafish) and cold water (Atlantic salmon) species, where possible differences in metabolites could be expected. The method was tested in whole zebrafish and in different salmon tissues, such as muscle, bile, kidney, fat, and liver. The final objective of this work was to assess kinetics of chlorpyrifos-Me and pirimiphos-Me and their main metabolites in fish tissue, in order to fill the knowledge gaps on these metabolites in fish tissues when fed over prolonged time. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Formula: C5H6N2O2

The Article related to lc ms organophosphorus pesticide bioaccumulation metabolite salmon zebrafish, plant based feed contamination salmo danio chlorpyrifos pirimiphos methyl, atlantic salmon, chlorpyrifos-methyl, lc-ms/ms, metabolites, pirimiphos-methyl, zebrafish and other aspects.Formula: C5H6N2O2

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 2, 2004, Moriya, Minoru; Suzuki, Takao; Ishihara, Akane; Iwaasa, Hisashi; Kanatani, Akio published a patent.Recommanded Product: 5-Phenylpyrimidine-2-carboxylic acid The title of the patent was Preparation of pyrimidine derivatives having 2-aminoquinoline moiety as MCH receptor antagonists. And the patent contained the following:

Title compounds I [R1, R2 = alkyl, etc.; R3, R4, R6, R7 = H, alkyl, etc.; R5 = H, alkyl; R8 = halo, etc.; n = 0-4] were prepared For example, hydrogenation of nitro compound (R)-II followed by acylation with 5-phenylpyrimidine-2-carboxylic acid afforded compound (R)-III. In MCH (melanin concentrating hormone) binding assays, the IC50 value of compound (R)-III was 4.1 nM. Compounds I are claimed useful for the treatment of obesity, diabetes, etc. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Recommanded Product: 5-Phenylpyrimidine-2-carboxylic acid

The Article related to aminoquinoline preparation mch melanin concentrating hormone receptor antagonist, antiobesity aminoquinoline preparation mch melanin concentrating hormone receptor antagonist, antidiabetic agent aminoquinoline preparation mch receptor antagonist and other aspects.Recommanded Product: 5-Phenylpyrimidine-2-carboxylic acid

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Zhang, Yipei; Bello, Anila; Ryan, David K.; Demokritou, Philip; Bello, Dhimiter published an article in 2022, the title of the article was Elevated Urinary Biomarkers of Oxidative Damage in Photocopier Operators following Acute and Chronic Exposures.SDS of cas: 4433-40-3 And the article contains the following content:

Inhalation exposures to nanoparticles (NPs) from printers and photocopiers have been associated with upper airway and systemic inflammation, increased blood pressure, and cases of autoimmune and respiratory disorders. In this study we investigate oxidative stress induced by exposures to copier-emitted nanoparticles using a panel of urinary oxidative stress (OS) biomarkers representing DNA damage (8-hydroxydeoxyguanosine, 8-OHdG; 8-hydroxyguanosine, 8-OHG; 5-hydroxymethyl uracil 5-OHMeU), lipid peroxidation (8-isoprostane; 4-hydroxynonenal, HNE), and protein oxidation biomarkers (o-tyrosine, 3-chlorotyrosine, and 3-nitrotyrosine) under conditions of acute (single 6 h exposure, 9 volunteers, 110 urine samples) and chronic exposures (6 workers, 11 controls, 81 urine samples). Urinary biomarkers were quantified with liquid chromatog.-tandem mass spectrometry after solid phase extraction sample cleanup. 8-OHdG, 8-OHG, 8-isoprostane, and HNE were significantly elevated in both the acute and chronic exposure study participants relative to the controls. In the acute exposure study, the geometric mean ratios post-/pre-exposure were 1.42, 1.10, 2.0, and 2.25, resp. Urinary 8-OHG and HNE increased with time to at least 36 h post-exposure (post-/pre-exposure GM ratios increased to 3.94 and 2.33, resp.), suggesting slower generation and/or urinary excretion kinetics for these biomarkers. In chronically exposed operators, the GM ratios of urinary biomarkers relative to controls ranged from 1.52 to 2.94, depending on the biomarker. O-Tyrosine and 5-OHMeU biomarkers were not significantly different from the controls. 3-chlorotyrosine and 3-nitrotyrosine were not detected in the urine samples. We conclude that NPs from photocopiers induce systemic oxidative stress by damaging DNA, RNA, and lipids. Urinary levels of 8-OHdG, 8-OHG, HNE, and 8-isoprostane were orders of magnitude higher than in nanocomposite processing workers, comparable to nano titanium dioxide and fiberglass manufacturing workers, but much lower than in shipyard welding and carbon nanotube synthesis workers. Biomarkers 8-OHdG, 8-OHG, 8-isoprostane, and HNE appear to be more sensitive and robust urinary biomarkers for monitoring oxidative stress to NPs from photocopiers. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).SDS of cas: 4433-40-3

The Article related to urinary biomarker oxidative damage photocopier operator acute chronic exposure, dna damage, acute exposure, chronic exposure, copier emitted nanoparticles, lipid peroxidation, oxidative stress, oxidative stress biomarkers, reactive oxygen species and other aspects.SDS of cas: 4433-40-3

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kazemnejadi, Milad; Sardarian, Ali Reza; Esmaeilpour, Mohsen published an article in 2019, the title of the article was Introduction of two polyvinyl alcohol resins for efficient solid support Cu-catalyzed N-arylation of α-aminoacids with aryl halides in aqueous media.Category: pyrimidines And the article contains the following content:

In this article, two polyvinyl alc. (PVA)-based resins were prepared by crosslinking of epoxidized PVA-chains using of 4-(4-aminobenzyl)benzenamine as a crosslinker and polymerization of acrylated PVA chains in the another approach. The prepared PVA resins showed well hydrophilic and swelling properties in various organic solvents, which are used in solid-phase organic synthesis (SPOS). Swelling properties of these resins were examined in DMF, THF, water, ethanol, methanol, dichloromethane, and dioxane. Furthermore, the both resins were characterized by FTIR and 1H-NMR and their properties such as epoxy equivalent weight (EEW) of epoxidized PVA and d. of the resins were determined by anal. methods. Then, α-amino acids such as L-aspartic acid, L-leucine, L-alanine, L-serine, L-valine, L-threonine, and L-tyrosine were immobilized on both resins through esterification reaction between these α-amino acids with the present hydroxyl groups on PVA resins, to carry out their solid-phase N-arylation reaction in the presence of CuI as a catalyst in milder and greener conditions than free resin protocols. Hydrolysis of the corresponding N-arylated α-amino acids immobilized on the resins gave the N-arylated α-amino acids in high to excellent yields. © 2019 Wiley Periodicals, Inc.J. Appl. Polym. Sci. 2019, 136, 47597. The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).Category: pyrimidines

The Article related to amino acid arylation solid phase arylhalide green chem swelling, solid support recycling copper arylation polyvinyl alc resin hydrolysis, arylation reaction mechanism copper catalyst, aryl halide cross coupling reaction amino acid copper catalyst and other aspects.Category: pyrimidines

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 30, 2018, Briede, Jacob J.; Deferme, Lize; Wolters, Jarno E. J.; Claessen, Sandra M. H.; van den Beucken, Twan; Wagner, Richard J.; van Breda, Simone G.; Kleinjans, Jos C. S. published an article.Recommanded Product: 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione The title of the article was A cross-omics approach to investigate temporal gene expression regulation by 5-hydroxymethylcytosine via TBH-derived oxidative stress showed involvement of different regulatory kinases. And the article contained the following:

Regulation of DNA methylation plays a crucial role in biol. processes and carcinogenesis. The formation of 5-hydroxymethylcytosine (5hmC) by oxidation of 5-methylcytosine (5mC) has been proposed as an intermediate of active demethylation. However, whether and how active demethylation is regulated by oxidative stress-related processes is not well understood. Here we investigated whether free oxygen radicals are capable of directly forming 5hmC and how this enhanced whole genome gene expression. We applied LC-MS/MS technol. for the anal. of 5mC, 5hmC, 5-formylcytosine (5fC) and 5-hydroxymethyluracyl (5hmU) in HepG2 cells exposed to hydroxyl- and Me radicals, formed by tert-Bu hydroperoxide (TBH) at multiple time points. We observed that TBH is able to induce a significant increase in 5hmC. A detailed evaluation of the hydroxymethylome using a combination of 5hmC-immunoprecipitation and microarrays resulted in the identification of highly dynamic modifications that appear to increase during prolonged oxidant exposure. Analyses of temporal gene expression changes in combination with network anal. revealed different subnetworks containing differentially expressed genes (DEGs) with differentially hydroxyl-methylated regions (DhMRs) in different regulatory kinases enriched with serine-threonine kinases. These serine-threonine kinases compromises MAPK14, RPSK6KA1, RIPK1, and PLK3 and were all previously identified as key-regulators in hepatocarcinogenesis and subject of study for chemotherapeutic interventions. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Recommanded Product: 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

The Article related to gene expression regulation hydroxymethylcytosine tertbutylhydroperoxide oxidative stress regulatory kinase, 5-hydroxymethylcytosine, 5-methylcytosine, differentially expressed genes, hepg2 cells, serine-threonine kinases, tert-butyl hydroperoxide and other aspects.Recommanded Product: 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 30, 1981, Ishikawa, Fumiyoshi; Kosasayama, Akira; Yamaguchi, Hitoshi; Watanabe, Yoshifumi; Saegusa, Junji; Shibamura, Seiichi; Sakuma, Kyoko; Ashida, Shinichiro; Abiko, Yasushi published an article.SDS of cas: 42518-42-3 The title of the article was Cyclic guanidines. 14. Imidazo[1,2-a]thienopyrimidin-2-one derivatives as blood platelet aggregation inhibitors. And the article contained the following:

A series of novel 1,2,3,5-tetrahydroimidazo[1,2-a]thieno[2,3-d]-, and -[3,4-dpyrimidin-2-one derivatives were prepared and tested for the activity of inhibiting platelet aggregation in rats in vitro and ex vivo. They were prepared by the following reactions: NaBH4 reduction of 2,4-dichlorothienopyrimidines, followed by ethoxycarbonylmethylation and successive amination. Most of the compounds were found to be potent inhibitors of blood platelet aggregation. Structure-activity relationships indicated the essential contribution of the lactam structure and lipophilic substituents on the thiophene ring to the effective interaction of the compounds with a receptor site on the platelet. Among the compounds studied, 1,2,3,5,6,7,8,9-octahydro[1]benzothieno[1,2-d]imidazo[1,2-a]pyrimidin-2-one exhibited the most favorable activity. The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).SDS of cas: 42518-42-3

The Article related to cyclic guanidine, imidazothienopyrimidinone preparation blood platelet, thienopyrimidinone imidazo, pyrimidinone imidazothieno, structure blood platelet imidazothienopyrimidinone, reduction ethoxycarbonylmethylation amination dichlorothienopyrimidine and other aspects.SDS of cas: 42518-42-3

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 26, 1998, Rewcastle, Gordon W.; Murray, Donna K.; Elliott, William L.; Fry, David W.; Howard, Curtis T.; Nelson, James M.; Roberts, Billy J.; Vincent, Patrick W.; Showalter, H. D. Hollis; Winters, R. Thomas; Denny, William A. published an article.Formula: C7H3ClFN3 The title of the article was Tyrosine Kinase Inhibitors. 14. Structure-Activity Relationships for Methyl- amino-Substituted Derivatives of 4-[(3-Bromophenyl)amino]-6-(methylamino)- pyrido[3,4-d]pyrimidine (PD 158780), a Potent and Specific Inhibitor of the Tyrosine Kinase Activity of Receptors for the EGF Family of Growth Factors. And the article contained the following:

PD 158780 (I) is a very potent in vitro inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC50 = 0.08 nM), and other members of the erbB family, by competitive binding at the ATP site of these signal transduction enzymes. A series of analogs of PD 158780 bearing solubilizing functions off the 6-methylamino substituent were prepared by reaction of the 6-fluoro derivatives with appropriate amine nucleophiles. These were evaluated for their ability to inhibit the tyrosine phosphorylating action of EGF-stimulated full-length EGFR enzyme and for inhibition of autophosphorylation of the EGFR in A431 human epidermoid carcinoma cells in culture. The most effective analogs were those bearing weakly basic substituents through a secondary amine linkage, which proved water-soluble (>10 mM) and potent (IC50s generally <1 nM). No clear SAR could be discerned for these compounds with respect to amine base strength or the distance of the cationic center from the chromophore, suggesting that 6-substituents are in a favorable area of bulk tolerance in the enzyme binding site. More distinct SAR emerged for the ability of the compounds to inhibit EGFR autophosphorylation in A431 cells, where analogs bearing lipophilic weak bases were preferred. Representative analogs were evaluated for antitumor effectiveness against four in vivo tumor models. Significant in vivo activity was observed in estrogen-dependent MCF-7 breast and A431 epidermoid tumors. Marginal activity was seen in an EGFR-transfected tumor model, suggesting that while this cell line requires EGF for clone formation in soft agar, other growth factors may be able to replace EGF in vivo. Also, activity was seen against the SK-OV-3 ovarian cancer model, which is known to express other EGF receptor family members (although it is not clear whether these are absolutely required for growth in vivo). While substantial growth delays were seen in A431 and MCF-7 tumor models, the treated tumors remained approx. the same size throughout therapy, suggesting that the compounds are cytostatic rather than cytotoxic under these test conditions. It remains to be determined if more prolonged therapy has cytotoxic effects in vivo, resulting in net tumor cell kill. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Formula: C7H3ClFN3

The Article related to pd 158780 analog preparation structure activity, antitumor activity pd 158780 analog preparation, tyrosine kinase inhibitor pd 158780 analog, autophosphorylation inhibitor pd 158780 analog preparation, epidermal growth factor receptor inhibitor preparation and other aspects.Formula: C7H3ClFN3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia