Day: January 5, 2023

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

Regioselective N-alkylation with alcohols for the preparation of 2-(N-alkylamino)quinazolines and 2-(N-alkylamino)pyrimidines was written by Li, Feng;Chen, Lin;Kang, Qikai;Cai, Jianguang;Zhu, Guangjun. And the article was included in New Journal of Chemistry in 2013.Name: 4,6-Diphenylpyrimidin-2-amine This article mentions the following:

In the presence of the [Cp*IrCl₂]₂/NaOH system, the direct N-alkylation of 2-aminoquinazolines and 2-aminopyrimidines with alcs. afforded the N-exo-substituted 2-(N-alkylamino)quinazolines and 2-(N-alkylamino)pyrimidines with 71-96% yields and complete regioselectivities. The protocol is highly attractive because of easily available starting materials, high atom efficiency and environmental friendliness. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Name: 4,6-Diphenylpyrimidin-2-amine).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) 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. 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.Name: 4,6-Diphenylpyrimidin-2-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Profiling of the spatiotemporal distribution, risks, and prioritization of antibiotics in the waters of Laizhou Bay, northern China was written by Lu, Shuang;Lin, Chunye;Lei, Kai;Xin, Ming;Gu, Xiang;Lian, Maoshan;Wang, Baodong;Liu, Xitao;Ouyang, Wei;He, Mengchang. And the article was included in Journal of Hazardous Materials in 2022.Computed Properties of C11H12N4O3S This article mentions the following:

We investigated the spatiotemporal distributions, risks, and prioritization of 15 widely used antibiotics in Laizhou Bay (LZB). Water samples (145) were collected from LZB and its estuaries and analyzed. Twelve antibiotics, with total concentrations of 241-1450 and 69-289 ng L^-1 in estuarine water and seawater, resp., were detected, with the contributions of norfloxacin, ciprofloxacin, and amoxicillin exceeding 70%. Amoxicillin was firstly determined, which contributed to 20% and 46% of the total antibiotics during summer and spring, resp. Higher antibiotic concentrations were observed in the sea located adjacent to aquaculture bases and the Yellow River Estuary, which are significantly influenced by mariculture and riverine inputs, resp. Veterinary antibiotics showed higher total concentrations in summer compared to spring, indicating a higher degree of their usage in mariculture in summer. The antibiotic mixtures posed high risk to algae and low to medium risks to crustaceans and fish. Amoxicillin and norfloxacin were identified as high-risk pollutants. Addnl., amoxicillin and ciprofloxacin showed medium to high resistance development risks. Previous studies on antibiotics in the LZB did not determined amoxicillin and thus underestimated antibiotic contamination, ecol. risk, and resistance development risk. Amoxicillin, norfloxacin, and ciprofloxacin should be prioritized in risk management. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Computed Properties of C11H12N4O3S).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) 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. 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.Computed Properties of C11H12N4O3S

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia