Pyrimidines

Synthesis and biological research of 2-aryl-4-morpholino-6-triazolylpyrimidine derivatives as antitumor PI3K inhibitors was written by Yang, Xiu-li;Wang, Tian-cai;Lin, Sen;Fan, Hou-xing. And the article was included in Jingxi Huagong in 2014.Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine This article mentions the following:

In order to find more active antitumor PI3K inhibitors, pyrimidine-2,4-diol was used as raw material to go through chlorination by POCl₃, coupling with morpholine, then iodine generation, which was followed by Sonogashira coupling to remove the trimethylsilyl in order to get the triazolyl intermediate. Finally, the intermediate went through Suzuki coupling to give 2-aryl-4-morpholino-6-triazolylpyrimidine 14-27. Their structures were confirmed by ¹HNMR and LC-MS. The in vitro anti-proliferative activity assay against A2780 was carried out by MTT detection method, and the results showed that, at the test concentration of 10μmol/L, the compounds 14 and 25 were more potent than clin. candidates GDC-0941 and BEZ-235, the inhibition rate of which reached 76.7% and 77.2%, resp. Furthermore, the results of pharmacokinetic study suggested that compound 25 was desirable: t_1/2 = 3.2 h, and AUC_0-∞ was 34,193 (ng·h)/mL. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Recommanded Product: 4-(2-Chloropyrimidin-4-yl)morpholine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Impacts of farmland application of antibiotic-contaminated manures on the occurrence of antibiotic residues and antibiotic resistance genes in soil: A meta-analysis study was written by Zhang, Yu;Cheng, Dengmiao;Xie, Jun;Zhang, Yuting;Wan, Yu;Zhang, Yueqiang;Shi, Xiaojun. And the article was included in Chemosphere in 2022.Application of 1220-83-3 This article mentions the following:

Meta-anal. of 94 published studies was conducted to explore the impacts of farmland application of antibiotic-contaminated manures on antibiotic concentrations and ARG abundances in manure-amended soil. Forty-nine antibiotics were reported, in which chlortetracycline, oxytetracycline, doxycycline, tetracycline, enrofloxacin, ciprofloxacin and norfloxacin were the most prevalent and had relatively high concentrations The responses of ARG and mobile genetic element (MGE) abundances to farmland application of antibiotic-contaminated manures varied considerably under different management strategies and environmental settings. On average, compared to unamended treatments, farmland application of antibiotic-contaminated manures significantly increased the total ARG and MGE abundances by 591% and 351%, resp. (P < 0.05). Of all the included ARG classes, the largest increase was found for sulfonamide resistance genes (1121%), followed by aminoglycoside (852%) and tetracycline (763%) resistance genes. Correlation anal. suggested that soil organic carbon (SOC) was significantly neg. correlated with antibiotic concentrations in manured soil (P < 0.05) due to the formation of covalent bonds and nonextractable residues. Soil silt content was significantly pos. correlated with antibiotic concentration (P < 0.05), which was attributed to greater sorption capacities. The ARG abundances were significantly pos. correlated with soil silt content, antibiotic concentrations, mean annual temperature, SOC, MGEs and soil pH (P < 0.05), suggesting that changes in these factors may shape the ARG profiles. Collectively, these findings advanced our understanding of the occurrence of antibiotics and ARGs in manure-amended soil and potential factors affecting them and will contribute to better management of these contaminants in future agricultural production In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Application of 1220-83-3).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Application of 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Health effects and risks associated with the occurrence of pharmaceuticals and their metabolites in marine organisms and seafood was written by Madikizela, Lawrence Mzukisi;Ncube, Somandla. And the article was included in Science of the Total Environment in 2022.HPLC of Formula: 1220-83-3 This article mentions the following:

Pharmaceuticals and their metabolites are continuously invading the marine environment due to their input from the land such as their disposal into the drains and sewers which is mostly followed by their transfer into wastewater treatment plants (WWTPs). Their incomplete removal in WWTPs introduces pharmaceuticals into oceans and surface water. To date, various pharmaceuticals and their metabolites have been detected in marine environment. Their occurrence in marine organisms raises concerns regarding toxic effects and development of drug resistant genes. Therefore, it is crucial to review the health effects and risks associated with the presence of pharmaceuticals and their metabolites in marine organisms and seafood. This is an important study area which is related to the availability of seafood and its quality. Hence, this study provides a critical review of the information available in literature which relates to the occurrence and toxic effects of pharmaceuticals in marine organisms and seafood. This was initiated through conducting a literature search focussing on articles investigating the occurrence and effects of pharmaceuticals and their metabolites in marine organisms and seafood. In general, most studies on the monitoring of pharmaceuticals and their metabolites in marine environment are conducted in well developed countries such as Europe while research in developing countries is still limited. Pharmaceuticals present in freshwater are mostly found in seawater and marine organisms. Furthermore, the toxicity caused by different pharmaceutical mixtures was observed to be more severe than that of individual compounds In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3HPLC of Formula: 1220-83-3).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.HPLC of Formula: 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Regioselectivity studies of sydnone cycloaddition reactions of azine-substituted alkynes was written by Foster, Robert S.;Jakobi, Harald;Harrity, Joseph P. A.. And the article was included in Tetrahedron Letters in 2011.Synthetic Route of C6H4N2 This article mentions the following:

The synthesis of azine-substituted pyrazoles by a sydnone cycloaddition strategy is described. Incorporation of a 3-pyridyl moiety at the sydnone N-atom has little effect on either reactivity or regioselectivity, however, 2-ethynyl-pyridine and -pyrimidine undergo cycloaddition with surprisingly poor levels of regiocontrol. A rationale for the observed regiochem. trends and potential routes for improving selectivities are discussed. In the experiment, the researchers used many compounds, for example, 2-Ethynylpyrimidine (cas: 37972-24-0Synthetic Route of C6H4N2).

2-Ethynylpyrimidine (cas: 37972-24-0) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Synthetic Route of C6H4N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Three Efficient Methods for Preparation of Coelenterazine Analogues was written by Shakhmin, Anton;Hall, Mary P.;Walker, Joel R.;Machleidt, Thomas;Binkowski, Brock F.;Wood, Keith V.;Kirkland, Thomas A.. And the article was included in Chemistry – A European Journal in 2016.Reference of 90905-32-1 This article mentions the following:

The growing popularity of bioluminescent assays has highlighted the need for coelenterazine analogs possessing properties tuned for specific applications. However, the structural diversity of known coelenterazine analogs has been limited by current syntheses. Known routes for the preparation of coelenterazine analogs employ harsh reaction conditions that limit access to many substituents and functional groups. Novel synthetic routes reported here establish simple and robust methods for synthesis and investigation of structurally diverse marine luciferase substrates. Specifically, these new routes allow synthesis of coelenterazine analogs containing various heterocyclic motifs and substituted aromatic groups with diverse electronic substituents at the R² position. Interesting analogs described herein were characterized by their physicochem. properties, bioluminescent half-life, light output, polarity and cytotoxicity. Some of the analogs represent leads that can be utilized in the development of improved bioluminescent systems. In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1Reference of 90905-32-1).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Reference of 90905-32-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Inclusion complexation of 2-aminopyrimidines with β-cyclodextrin, physico-chemical and nuclear magnetic spectroscopic studies was written by Sumitha Celin, T.;Nagarajan, S.. And the article was included in Materials Science-Poland in 2014.HPLC of Formula: 40230-24-8 This article mentions the following:

Inclusion complexation of 2-aminopyrimidines with β-cyclodextrin was studied in the solid state by IR spectroscopy, differential scanning calorimetry (DSC) and SEM. The aminopyrimidine-β-CD complexes were also investigated in a solution by NMR spectral techniques (¹H-NMR and ¹³C-NMR). Qual. modifications in the position and number of peaks or bands obtained from spectral methods as well as thermal anal. indicated the inclusion. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8HPLC of Formula: 40230-24-8).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.HPLC of Formula: 40230-24-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014 was written by Pike, Kurt G.;Malagu, Karine;Hummersone, Marc G.;Menear, Keith A.;Duggan, Heather M. E.;Gomez, Sylvie;Martin, Niall M. B.;Ruston, Linette;Pass, Sarah L.;Pass, Martin. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2013.Product Details of 938443-20-0 This article mentions the following:

The optimization of a potent and highly selective series of dual mTORC1 and mTORC2 inhibitors is described. An initial focus on improving cellular potency while maintaining or improving other key parameters, such as aqueous solubility and margins over hERG IC₅₀, led to the discovery of the clin. candidate AZD8055. Further optimization, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clin. candidate AZD2014. In the experiment, the researchers used many compounds, for example, 2,4,7-Trichloropyrido[2,3-d]pyrimidine (cas: 938443-20-0Product Details of 938443-20-0).

2,4,7-Trichloropyrido[2,3-d]pyrimidine (cas: 938443-20-0) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Product Details of 938443-20-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors was written by Thakur, Ashish;Tawa, Gregory J.;Henderson, Mark J.;Danchik, Carina;Liu, Suiyang;Shah, Pranav;Wang, Amy Q.;Dunn, Garrett;Kabir, Md.;Padilha, Elias C.;Xu, Xin;Simeonov, Anton;Kharbanda, Surender;Stone, Richard;Grewal, Gurmit. And the article was included in Journal of Medicinal Chemistry in 2020.Application of 20090-58-8 This article mentions the following:

A series of quinazolin-4-one based hydroxamic acids was rationally designed and synthesized as novel dual PI3K/HDAC inhibitors by incorporating an HDAC pharmacophore into a PI3K inhibitor (Idelalisib) via an optimized linker. Several of these dual inhibitors were highly potent (IC₅₀ < 10 nM) and selective against PI3Kγ, δ and HDAC6 enzymes and exhibited good antiproliferative activity against multiple cancer cell lines. The lead compound 48c, induced necrosis in several mutant and FLT3-resistant AML cell lines and primary blasts from AML patients, while showing no cytotoxicity against normal PBMCs, NIH3T3, and HEK293 cells. Target engagement of PI3Kδ and HDAC6 by 48c was demonstrated in MV411 cells using the cellular thermal shift assay (CETSA). Compound 48c showed good pharmacokinetics properties in mice via i.p. administration and provides a means to examine the biol. effects of inhibiting these two important enzymes with a single mol., either in vitro or in vivo. In the experiment, the researchers used many compounds, for example, 4-Chloro-5-methylpyrimidin-2-amine (cas: 20090-58-8Application of 20090-58-8).

4-Chloro-5-methylpyrimidin-2-amine (cas: 20090-58-8) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Application of 20090-58-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Cooperative ruthenium complex catalyzed multicomponent synthesis of pyrimidines was written by Maji, Milan;Kundu, Sabuj. And the article was included in Dalton Transactions in 2019.Related Products of 40230-24-8 This article mentions the following:

A new set of 2-(2-benzimidazolyl) pyridine ligand based air and moisture stable ruthenium complexes were synthesized and characterized. The catalytic behaviors of these complexes were evaluated towards the multicomponent synthesis of highly substituted pyrimidines directly from various amidines, primary alcs., and secondary alcs. Among all the metal complexes, 2-hydroxypyridine and benzimidazole fragments containing complex I showed the best reactivity in this reaction. In addition, the N-H proton of benzimidazole and the hydroxyl group of pyridine played a critical role in enhancing catalytic activity. Several control experiments and mechanistic studies were carried out to understand this multicomponent synthesis of pyrimidines using complex I. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Related Products of 40230-24-8).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Related Products of 40230-24-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hydrogen peroxide mediated formation of heteroaryl ethers from pyridotriazol-1-yloxy heterocycles and arylboronic acids was written by Bardhan, Sujata;Tabei, Keiko;Wan, Zhao-Kui;Mansour, Tarek S.. And the article was included in Tetrahedron Letters in 2009.Recommanded Product: 5-Bromo-2-phenoxypyrimidine This article mentions the following:

Pyridotriazol-1-yloxypyrimidine reacts with arylboronic acids under palladium-free, Cs₂CO₃, (0.8%) H₂O₂, and DME conditions to produce heteroaryl ethers in good yields comparable to the oxidative palladium-catalyzed reaction. The yields of aryl ethers from pyridotriazol-1-yloxyquinazoline with (0.8%) H₂O₂ were modest. Hydrogen peroxide is superior to dioxygen as an oxidant in these reactions. In the experiment, the researchers used many compounds, for example, 5-Bromo-2-phenoxypyrimidine (cas: 257280-25-4Recommanded Product: 5-Bromo-2-phenoxypyrimidine).

5-Bromo-2-phenoxypyrimidine (cas: 257280-25-4) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. A Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones enables an efficient and facile synthesis of structurally important pyrimidines via a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization.Recommanded Product: 5-Bromo-2-phenoxypyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia