Day: January 6, 2023

Efficient coupling of 2-halopyrimidines to 2,2′-bipyrimidines was written by Nasielski, J.;Standaert, A.;Nasielski-Hinkens, R.. And the article was included in Synthetic Communications in 1991.Recommanded Product: 2-Bromo-4,6-dimethylpyrimidine This article mentions the following:

Pyrimidines I (R = H, Me, Ph; R¹ = Br, Cl) have been dimerized to the corresponding 2,2′-bipyrimidines in good yields by Tiecco’s method using NiCl₂, PPh₃ and Zn in DMF. In the experiment, the researchers used many compounds, for example, 2-Bromo-4,6-dimethylpyrimidine (cas: 16879-39-3Recommanded Product: 2-Bromo-4,6-dimethylpyrimidine).

2-Bromo-4,6-dimethylpyrimidine (cas: 16879-39-3) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Recommanded Product: 2-Bromo-4,6-dimethylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Occurrence and distribution of antibiotics and antibiotic resistance genes in the guts of shrimp from different coastal areas of China was written by Li, Wei;Li, Yaying;Zheng, Ningguo;Ge, Chaorong;Yao, Huaiying. And the article was included in Science of the Total Environment in 2022.Formula: C11H12N4O3S This article mentions the following:

With the continuous increase in shrimp (Litopenaeus vannamei) aquaculture production, the widespread use of antibiotics as a means of preventing and treating diseases has adversely affected the environment, animal health and symbiotic microorganisms in gut environments. At the same time, antibiotic resistance genes (ARGs) are widespread in aquaculture and pose a great threat to aquatic organisms and humans. Therefore, in the present study, the occurrence and distribution of 17 antibiotics, ARGs and mobile genetic elements (MGEs) were detected in the guts of shrimp collected from 12 coastal regions of China. The results showed that sulfadiazine, ciprofloxacin and norfloxacin were detectable in the guts of L. vannamei at all sampling sites. Sul1, sul2, floR and intI-1 were also detected in the guts of L. vannamei at all sampling sites. The total relative abundances of ARGs and MGEs were significantly pos. correlated according to Pearson correlation anal. Sulfonamide resistance genes (sul1 and sul2) were significantly pos. correlated with intI-1. These results indicated that MGEs could increase the risk of horizontal gene transfer of ARGs in a gut environment. MGEs are the most important factors promoting the spread of ARGs. Correlation anal. showed that sulfadiazine was significantly pos. correlated with sul1 and sul2 and that fluoroquinolone antibiotics were significantly pos. correlated with floR, indicating that antibiotics could induce the production of ARGs. Network anal. indicated that Iamia and Alkaliphilus species may harbor the most antibiotic resistance genes, and these bacteria were closely related to the proliferation and spread of ARGs in a gut environment. Antibiotic use and the spread of ARGs in mariculture systems may have neg. effects on shrimp and human health. The use of antibiotics should be strictly regulated to control contaminants in mariculture systems, including pathogens and ARGs, thereby reducing potential risks to human health. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Formula: C11H12N4O3S).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Formula: C11H12N4O3S

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Detection of active groups in alkylpyrimidines. Study of the mobility of hydrogen by hydrogen-deuterium isotope exchange. I. Qualitative kinetics was written by Dizabo, Pierre;Monier, Jean C.;Pompon, Alain. And the article was included in Journal of Labelled Compounds in 1971.Electric Literature of C6H9N3 This article mentions the following:

Me groups bound to heterocyclic rings exchange H for D. This exchange is studied for alkyl or aminoalkylpyrimidines in acid. The qual. results obtained as a function of acidity, substituent location, and temperature confirm the reaction mechanism proposed by Brown except in the case of 2-amino-4,6-dimethylpyrimidine. In the experiment, the researchers used many compounds, for example, 4,5-Dimethylpyrimidin-2-amine (cas: 1193-74-4Electric Literature of C6H9N3).

4,5-Dimethylpyrimidin-2-amine (cas: 1193-74-4) 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.Electric Literature of C6H9N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Dual Inhibitors of 8-Oxoguanine Surveillance by OGG1 and NUDT1 was written by Tahara, Yu-ki;Kietrys, Anna M.;Hebenbrock, Marian;Lee, Yujeong;Wilson, David L.;Kool, Eric T.. And the article was included in ACS Chemical Biology in 2019.Product Details of 20090-58-8 This article mentions the following:

Oxidative damage in DNA is one of the primary sources of mutations in the cell. The activities of repair enzymes 8-oxoguanine DNA glycosylase (OGG1) and human MutT Homolog 1 (NUDT1 or MTH1), which work together to ameliorate this damage, are closely linked to mutagenesis, genotoxicity, cancer, and inflammation. Here we have undertaken the development of small-mol. dual inhibitors of the two enzymes as tools to test the relationships between these pathways and disease. The compounds preserve key structural elements of known inhibitors of the two enzymes, and they were synthesized and assayed with recently developed luminescence assays of the enzymes. Further structural refinement of initial lead mols. yielded compound 5 (I) (SU0383) with IC50 (NUDT1) = 0.034μM, IC50 (OGG1) = 0.49μM. I displayed low toxicity in two human cell lines at 10μM. Experiments confirm the ability of I to increase sensitivity of tumor cells to oxidative stress. Dual inhibitors of these two enzymes are expected to be useful in testing multiple hypotheses regarding the roles of 8-oxo-dG in multiple disease states. In the experiment, the researchers used many compounds, for example, 4-Chloro-5-methylpyrimidin-2-amine (cas: 20090-58-8Product Details of 20090-58-8).

4-Chloro-5-methylpyrimidin-2-amine (cas: 20090-58-8) 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. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Product Details of 20090-58-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Palladium-catalyzed cross-coupling reaction of 2- and/or 5-substituted 4,6-dichloropyrimidines with arylboronic acids was written by Tumkevicius, S.;Dodonova, J.;Baskirova, I.;Voitechovicius, A.. And the article was included in Journal of Heterocyclic Chemistry in 2009.Quality Control of 4,6-Diphenylpyrimidin-2-amine This article mentions the following:

The Suzuki-Miyaura reaction of some 4,6-dichloropyrimidines bearing methylthio-, methyl-, amino-, cyano-, formyl-, and nitro groups in positions 2 and/or 5 of the pyrimidine ring with arylboronic acids has been investigated. Influence of palladium catalyst, ligand, base, and solvent on the reaction outcome was studied. The reaction was found to give the corresponding 4,6-diarylpyrimidines in reasonable yields using Pd(OAc)₂/PPh₃/K₃PO₄ or Pd(PPh₃)₂Cl₂/K₃PO₄ as catalyst systems. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Quality Control of 4,6-Diphenylpyrimidin-2-amine).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Quality Control of 4,6-Diphenylpyrimidin-2-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The coloration reaction mechanism of 6-aminouracil derivatives with Ehrlich reagent and its application to the colorimetric determination method. II was written by Nakashima, Kenichiro. And the article was included in Yakugaku Zasshi in 1977.Product Details of 54030-56-7 This article mentions the following:

6-Amino-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine (I) [1004-40-6] and its N- or S-substituted derivatives are hydrolyzed by p-toluenesulfonic acid or HCl to the corresponding barbiturates. These barbiturates condense with the Ehrlich reagent [100-10-7] in the presence of an acid catalyst to afford stable benzylidene compounds These reactions were found to be almost quant. The optimal exptl. conditions were also established for using the above reactions for the quant. colorimetric determination of I derivatives In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Product Details of 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Product Details of 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Occurrence and variations of pharmaceuticals and personal-care products in rural water bodies: A case study of the Taige Canal (2018-2019) was written by Jiang, Xinshu;Zhu, Yongqing;Liu, Liquan;Fan, Xueqi;Bao, Yixiang;Deng, Shanshan;Cui, Yunxia;Cagnetta, Giovanni;Huang, Jun;Yu, Gang. And the article was included in Science of the Total Environment in 2021.Related Products of 1220-83-3 This article mentions the following:

A systematic monitoring campaign of pharmaceuticals and personal-care products (PPCPs) was performed in the Taige Canal basin, which is located in a rural area of the Yangtze River Delta. A total of 55 out of 61 monitored PPCPs were detected, with concentrations up to 647 ng/L. The maximum concentrations of 75% of monitored antibiotics and 80% of non-antibiotics were above the median values of previously reported maximum concentrations in China, indicating that the basin is heavily contaminated. It is estimated that the PPCP mass flow of the Taige Canal (0.06-0.58 kg/day) entering into Lake Taihu is similar to that of the influent of a wastewater treatment plant. Anal. of the seasonal variation shows that, during the wet season, the average total concentration of sulfonamides was 8 and 11 times that of the normal season and dry season, resp. The concentration of sulfachlorpyridazine accounted for 40.37% of total antibiotics, suggesting heavy pollution from the animal-breeding industry in this area. The PPCP mass flow rates observed in 2019 were lower than those of 2018 in the same season, and this interannual variation is mainly attributable to water pollution controls in the watershed. Combined anal. of ordination and clustering indicates that the distribution of PPCPs in the Taige Canal is affected by the confluence with Yong’an River and human activities such as water pollution control. Water-sediment distribution anal. demonstrates that the sediment-water distribution coefficients of quinolone and macrolide were higher than those of sulfonamide, lincosamide and chloramphenicol. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Related Products 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. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Related Products of 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Tetrahydro-3H-pyrazolo[4,3-a]phenanthridine-based CDK inhibitor was written by Opoku-Temeng, Clement;Dayal, Neetu;Hernandez, Delmis E.;Naganna, N.;Sintim, Herman O.. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2018.Quality Control of 2-Methoxypyrimidine-5-carbaldehyde This article mentions the following:

Cyclin-dependent kinases have emerged as important targets for cancer therapy. HSD992, containing a novel scaffold based on the tetrahydro-3H-pyrazolo[4,3-a]phenanthridine core, inhibits CDK2/3 but not other CDKs and also potently inhibits several cancer cell lines. In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1Quality Control of 2-Methoxypyrimidine-5-carbaldehyde).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Quality Control of 2-Methoxypyrimidine-5-carbaldehyde

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

CsOH/γ-Al₂O₃: a heterogeneous reusable basic catalyst for one-pot synthesis of 2-amino-4,6-diaryl pyrimidines was written by Ramana, Amey Nimkar M. M. V.;Betkar, Rahul;Ranade, Prasanna;Mundhe, Balaji. And the article was included in New Journal of Chemistry in 2016.HPLC of Formula: 40230-24-8 This article mentions the following:

New strategy for a one-pot synthesis of 2-amino-4,6-diaryl pyrimidines using CsOH/γ-Al₂O₃ as a heterogeneous, reusable basic catalyst was presented. Developed synthetic protocol for pyrimidines was a one-pot three-component reaction of acetophenone, aromatic aldehydes and guanidine hydrochloride in ethanol. Characterization of the catalyst CsOH/γ-Al₂O₃ was performed by using FT-IR, XRD, TG-DTA, SEM, BET surface area and CO₂-TPD anal. techniques. Anal. data prove that the catalyst had excellent reusability and also indicated their good thermal stability. 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 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.HPLC of Formula: 40230-24-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor was written by Borsari, Chiara;Rageot, Denise;Dall’Asen, Alix;Bohnacker, Thomas;Melone, Anna;Sele, Alexander M.;Jackson, Eileen;Langlois, Jean-Baptiste;Beaufils, Florent;Hebeisen, Paul;Fabbro, Doriano;Hillmann, Petra;Wymann, Matthias P.. And the article was included in Journal of Medicinal Chemistry in 2019.Name: 4-Dimethoxymethylpyrimidin-2-ylamine This article mentions the following:

The mechanistic target of rapamycin (mTOR) plays a pivotal role in growth and tumor progression and is an attractive target for cancer treatment. ATP-competitive mTOR kinase inhibitors (TORKi) have the potential to overcome limitations of rapamycin derivatives in a wide range of malignancies. Herein, we exploit a conformational restriction approach to explore a novel chem. space for the generation of TORKi. Structure-activity relationship (SAR) studies led to the identification of compound 12b with a ∼450-fold selectivity for mTOR over class I PI3K isoforms. Pharmacokinetic studies in male Sprague Dawley rats highlighted a good exposure after oral dosing and a min. brain penetration. CYP450 reactive phenotyping pointed out the high metabolic stability of 12b. These results identify the tricyclic pyrimido-pyrrolo-oxazine moiety as a novel scaffold for the development of highly selective mTOR inhibitors for cancer treatment. In the experiment, the researchers used many compounds, for example, 4-Dimethoxymethylpyrimidin-2-ylamine (cas: 165807-05-6Name: 4-Dimethoxymethylpyrimidin-2-ylamine).

4-Dimethoxymethylpyrimidin-2-ylamine (cas: 165807-05-6) 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-Dimethoxymethylpyrimidin-2-ylamine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia