Tag: 100-200

Qureshi, Wasay Mohiuddin Shaikh; Pratten, Margaret K. published an article in 2018, the title of the article was Chick embryonic cardiomyocyte micromass system for assessing developmental cardiotoxicity of drugs.Product Details of 626-48-2 And the article contains the following content:

Heart is the first mesodermal organ to develop and is sensitive to life-threatening toxic effects of drugs during development. A number of methods have been devised to study developmental cardiotoxic effects of drugs including micromass system. The micromass system involves the culture of primary embryonic cells and reestablishment of tissue system in vitro. In chick embryonic cardiomyocyte micromass system the chick heart cells are cultured in a small volume at a very high cell d. These cells form synchronized contracting foci. Addition of drugs to this system allows us to study the developmental cardiotoxic effects at mol. level. Using appropriate end points and mol. marker or adopting high-throughput screening, this method can further help to identify and avoid the use of cardiotoxic compounds during development. 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 heart cardiomyocyte micromass system developmental cardiotoxicity vpa bpn, cardiomyocytes, chick, connexin43, developmental toxicology, micromass, reactive oxygen species, teratogens and other aspects.Product Details of 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Starczak, Marta; Zarakowska, Ewelina; Modrzejewska, Martyna; Dziaman, Tomasz; Szpila, Anna; Linowiecka, Kinga; Guz, Jolanta; Szpotan, Justyna; Gawronski, Maciej; Labejszo, Anna; Liebert, Ariel; Banaszkiewicz, Zbigniew; Klopocka, Maria; Foksinski, Marek; Gackowski, Daniel; Olinski, Ryszard published an article in 2018, the title of the article was In vivo evidence of ascorbate involvement in the generation of epigenetic DNA modifications in leukocytes from patients with colorectal carcinoma, benign adenoma and inflammatory bowel disease.Application of 4433-40-3 And the article contains the following content:

Background: A characteristic feature of malignant cells, such as colorectal cancer cells, is a profound decrease in the level of 5-hydroxymethylcytosine, a product of 5-methylcytosine oxidation by TET enzymes. Recent studies showed that ascorbate may upregulate the activity of TET enzymes in cultured cells and enhance formation of their products in genomic DNA. Methods: The study included four groups of subjects: healthy controls (n = 79), patients with inflammatory bowel disease (IBD, n = 51), adenomatous polyps (n = 67) and colorectal cancer (n = 136). The list of analyzed parameters included (i) leukocyte levels of epigenetic DNA modifications and 8-oxo-7,8-dihydro-2′-deoxyguanosine, a marker of oxidatively modified DNA, determined by means of isotope-dilution automated online two-dimensional ultra-performance liquid chromatog. with tandem mass spectrometry, (ii) expression of TET mRNA measured with RT-qPCR, and (iii) chromatog.-determined plasma concentrations of retinol, alpha-tocopherol and ascorbate. Results: Patients from all groups presented with significantly lower levels of 5-methylcytosine and 5-hydroxymethylcytosine in DNA than the controls. A similar tendency was also observed for 5-hydroxymethyluracil level. Patients with IBD showed the highest levels of 5-formylcytosine and 8-oxo-7,8-dihydro-2′-deoxyguanosine of all study subjects, and individuals with colorectal cancer presented with the lowest concentrations of ascorbate and retinol. A pos. correlation was observed between plasma concentration of ascorbate and levels of two epigenetic modifications, 5-hydroxymethylcytosine and 5-hydroxymethyluracil in leukocyte DNA. Moreover, a significant difference was found in the levels of these modifications in patients whose plasma concentrations of ascorbate were below the lower and above the upper quartile for the control group. Conclusions: These findings suggest that deficiency of ascorbate in the blood may be a marker of its shortage in other tissues, which in turn may correspond to deterioration of DNA methylation-demethylation. These observations may provide a rationale for further research on blood biomarkers of colorectal cancer development. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Application of 4433-40-3

The Article related to ascorbate epigenetics dna modification leukocyte carcinoma inflammatory bowel disease, ascorbate, colon polyp, colorectal cancer, dna demethylation, epigenetic dna modifications, ibd and other aspects.Application of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 5, 2015, Saitoh, Morihisa; Yogo, Takatoshi; Kamei, Taku; Tokunaga, Norihito; Ohba, Yusuke; Yukawa, Takafumi published a patent.Application In Synthesis of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride The title of the patent was Preparation of pyridinylpyrrolidinone heterocyclic compounds as tyrosine kinase 2 inhibitors, and preventive and therapeutic methods for autoimmune disease. And the patent contained the following:

The heterocyclic compounds are represented by formula I [ring A = addnl. (un)substituted pyrrolidine; R1, R2, R4 = H, substituent; R3 = H, halo, halo-(un)containing C1-6 alkyl, amino, halo-(un)containing C1-6 alkyl(mono or di-)amino; R5 = H, (un)substituted C1-6 alkyl, (un)substituted C6-14 aryl, (un)substituted aromatic heterocycle, acyl]. Thus, reacting Et cyano(cyclopropyl)acetate (preparation given) with 2-benzyl(2-bromoethyl)carbamate, reacting with sodium hydride to obtain 3-cyclopropyl-2-oxopyrrolidine-3-carbonitrile, separating 3-cyclopropyl-2-oxopyrrolidine-3-carbonitrile by chiral HPLC to prepare (3S)-cyclopropyl-2-oxopyrrolidine-3-carbonitrile, reacting (3S)-cyclopropyl-2-oxopyrrolidine-3-carbonitrile with 2-bromo-4-fluoropyridine, and coupling with 5-(morpholin-4-yl)pyridin-2-amine, gave (3S)-3-cyclopropyl-1-[2-[[5-(morpholin-4-yl)pyridin-2-yl]amino]pyridin-4-yl]-2-oxopyrrolidine-3-carbonitrile with tyrosine kinase 2 (Tyk2) inhibitory activity (1 μM) 99%. Formulations containing I are given. The experimental process involved the reaction of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride(cas: 1187830-46-1).Application In Synthesis of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride

The Article related to pyridinylpyrrolidinone tyk2 inhibitor preparation autoimmune therapeutic psoriasis rheumatoid, arthritis inflammatory sjoegren behcet multiple sclerosis systemic lupus erythematosus and other aspects.Application In Synthesis of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 17, 2020, Gong, Yong; Chen, Lu; Zhang, Wei; Salter, Rhys published an article.Application In Synthesis of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione The title of the article was Transglycosylation in the Modification and Isotope Labeling of Pyrimidine Nucleosides. And the article contained the following:

Transglycosylation of pyrimidine nucleosides is demonstrated in a one-pot synthesis of uridine derivatives under microwave irradiation Inductive activation of 2′,3′,5′-tri-O-acetyl uridine with a 5-nitro group produces a more-reactive glycosyl donor. Under optimized Vorbruggen conditions, the 5-nitrouridine facilitates a reversible nucleobase exchange with a series of 5-substituted uracils. The protocol is also exemplified in a gram-scale reaction under thermal heating. The strategy provides easy access to isotopically labeled uridine. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Application In Synthesis of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

The Article related to vorbruggen nitrouridine nucleobase thermal heating microwave transglycosylation nucleoside, transglycosylation pyrimidine nucleoside isotope labeling synthesis microwave irradiation and other aspects.Application In Synthesis of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 29, 2020, Heymach, John; Robichaux, Jacqulyne; Nilsson, Monique; Jones, Philip; Cross, Jason; Theroff, Jay published a patent.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine The title of the patent was Preparation of pyridopyrimidines as inhibitors of tyrosine kinase for the treatment or prevention of diseases. And the patent contained the following:

The invention relates to preparation of pyridopyrimidines(I) as inhibitors of tyrosine kinase which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of diseases, including cancer. Compounds I wherein A1 is C(R1)or N; A2 is C(R2)or N; A3 is C(R3)or N; Ar1 is aryl or heteroaryl; R1 is halo, CN, OR6, etc.; R2 is H, alkyl, alkoxy; R3 is H or alkyl; R6 is alkyl, H, C(=O)alkyl, are claimed. The example compound II was prepared via 10-step synthetic procedure using 6-fluoropyridin-3-amine as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I can be used in treatment or prevention of HER2- and EGFR-mediated diseases. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

The Article related to enamide pyridopyrimidine preparation tyrosine kinase inhibitor cancer treatment prophylaxis, pyridopyrimidine preparation mutation her2 egfr inhibitor disease treatment prophylaxis and other aspects.Recommanded Product: 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 18, 2015, Lin, Meng-I.; Su, Bo-Han; Lee, Chia-Hsin; Wang, Suz-Ting; Wu, Wen-Chun; Dangate, Prasad; Wang, Shi-Yun; Huang, Wen-I.; Cheng, Ting-Jen; Lin, Olivia A.; Cheng, Yih-Shyun E.; Tseng, Yufeng Jane; Sun, Chung-Ming published an article.Name: 6-Methylpyrimidine-2,4(1H,3H)-dione The title of the article was Synthesis and inhibitory effects of novel pyrimido-pyrrolo-quinoxalinedione analogues targeting nucleoproteins of influenza A virus H1N1. And the article contained the following:

The influenza nucleoprotein (NP) is a single-strand RNA-binding protein and the core of the influenza ribonucleoprotein (RNP) particle that serves many critical functions for influenza replication. NP has been considered as a promising anti-influenza target. A new class of anti-influenza compounds, nucleozin and analogs were reported recently in several laboratories to inhibit the synthesis of influenza macromols. and prevent the cytoplasmic trafficking of the influenza RNP. In this study, pyrimido-pyrrolo-quinoxalinedione (PPQ) analogs as a new class of novel anti-influenza agents are reported. Compound PPQ-581 was identified as a potential anti-influenza lead with EC50 value of 1 μM for preventing virus-induced cytopathic effects. PPQ produces similar anti-influenza effects as nucleozin does in influenza-infected cells. Treatment with PPQ at the beginning of H1N1 infection inhibited viral protein synthesis, while treatment at later times blocked the RNP nuclear export and the appearance of cytoplasmic RNP aggregation. PPQ resistant H1N1 (WSN) viruses were isolated and found to have a NPS377G mutation. Recombinant WSN carrying the S377G NP is resistant to PPQ in anti-influenza and RNA polymerase assays. The WSN virus with the NPS377G mutation also is devoid of the PPQ-mediated RNP nuclear retention and cytoplasmic aggregation. The NPS377G expressing WSN virus is not resistant to the reported NP inhibitors nucleozin. Similarly, the nucleozin resistant WSN viruses are not resistant to PPQ, suggesting that PPQ targets a different site from the nucleozin-binding site. The results also suggest that NP can be targeted through various binding sites to interrupt the crucial RNP trafficking, resulting in influenza replication inhibition. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Name: 6-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to preparation quinoxalinedione nucleoprotein antiviral influenza virus, anti-influenza, influenza nucleoprotein, pyrimido-pyrrolo-quinoxalinedione (ppq), rna-dependent rna polymerase and other aspects.Name: 6-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 1, 2021, Chen, Lishi; Deng, Shanbin; Fang, Yuchan; Zhong, Yanmei; Wang, Yandong; Tang, Wenjing; Zhang, Biting; Du, Mengjiao; Chuqin Yu published an article.Synthetic Route of 4433-40-3 The title of the article was Serum metabonomic study of the effects of Huofeitong tablet on rats with COPD. And the article contained the following:

Chronic obstructive pulmonary disease (COPD) is a common respiratory disease. The Huofeitong tablet (HFTT), a Chinese compound medicine, exhibits an unambiguous therapeutic effect on COPD. However, the mechanism of its therapeutic effect on COPD is unclear. This study aimed to investigate the effect of HFTT on COPD and its mechanism. The changes in pulmonary function and the inflammatory factors in rats were determined via histopathol. and bronchoalveolar lavage fluid. The mechanism of HFTT in COPD treatment was revealed using UPLC-Q-TOF-MS/MS and multivariate statistical anal. Results showed that after HFTT treatment, the lung function began to recover, the lung tissue improved, and the TNF-α and IL-6 levels decreased, suggesting that HFTT had a therapeutic effect on COPD. In addition, 12 potential biomarkers, including malonate, urea-1-carboxylate, pyruvate, L-cysteate, glutathione, 2-deoxy-α-D-ribose1-phosphate, 3-fumarylpyruvate, 3-maleylpyruvate, 2-inosose, urate, allantoin, and inosine were screened. They associated with COPD development and concentrated in glutathione metabolism, glyoxylate and dicarboxylate metabolism, secondly concentrated in pyruvate metabolism, glycolysis/gluconeogenesis, pentose phosphate pathway, citrate cycle, glycine, serine and threonine metabolism, inositol phosphate, and purine metabolism This study contributes to the development and application of HFTT in COPD treatment and provides a theor. basis for COPD diagnosis, prevention, and treatment. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Synthetic Route of 4433-40-3

The Article related to huofeitong antiinflammatory agent chronic obstructive pulmonary disease, biomarkers, chronic obstructive pulmonary disease, huofeitong tablet, metabolism, pathway, uplc-q-tof-ms/ms and other aspects.Synthetic Route of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 17, 2005, Edwards, Paul John; Gibson, Karl Richard; Mantell, Simon John; Maw, Graham Nigel; Poinsard, Cedric published a patent.COA of Formula: C7H3ClFN3 The title of the patent was Preparation of azaquinazoline derivatives for treating pain. And the patent contained the following:

The title 6-amino-7-azaquinazolines I [X = a bond, alkylene; R1 = (un)substituted cycloalkyl, cycloalkyl fused to (hetero)cycloalkyl, heterocycloalkyl; R2 = OR4, NR4R5; R4 = alkyl, cycloalkyl, etc.; R5 = H, alkyl, cycloalkyl; or NR4R5 = aziridinyl, azetidinyl, piperidinyl, etc.], useful in the treatment of pain, were prepared and formulated. Thus, reacting cycloheptyl-(6-fluoropyrido[3,4-d]pyrimidin-4-yl)amine (preparation given) with piperidin-4-ol afforded I [X = a bond; R1 = cycloheptyl; R2 = 4-hydroxypiperidin-1-yl]. The exemplified compounds I were tested in mGluR1 assay and were found to have an IC50 of 10 μM or less. The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).COA of Formula: C7H3ClFN3

The Article related to azaquinazoline preparation analgesic glutamate receptor metabotropic mglur1 antagonist, azaquinazolinamine preparation analgesic glutamate receptor metabotropic mglur1 antagonist and other aspects.COA of Formula: C7H3ClFN3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Cawrse, Brian M.; Lapidus, Rena S.; Cooper, Brandon; Choi, Eun Yong; Seley-Radtke, Katherine L. published an article in 2018, the title of the article was Anticancer Properties of Halogenated Pyrrolo[3,2-d]pyrimidines with Decreased Toxicity via N5 Substitution.Synthetic Route of 626-48-2 And the article contains the following content:

Halogenated pyrrolo[3,2-d]pyrimidine analogs have shown antiproliferative activity in recent studies, with cell accumulation occurring in the G2/M stage without apoptosis. However, the mechanism of action and pharmacokinetic (PK) profile of these compounds has yet to be determined To investigate the PK profile of these compounds, a series of halogenated pyrrolo[3,2-d]pyrimidine compounds was synthesized and first tested for activity in various cancer cell lines followed by a mouse model. EC50 values ranged from 0.014 to 14.5 μM, and maximum tolerated doses (MTD) in mice were between 5 and 10 mg kg-1. This indicates a wide variance in activity and toxicity that necessitates further study. To decrease toxicity, a second series of compounds was synthesized with N5-alkyl substitutions in an effort to slow the rate of metabolism, which was thought to be leading to the toxicity. The N-substituted compounds demonstrated comparable cell line activity (EC50 values between 0.83-7.3 μM) with significantly decreased toxicity (MTD=40 mg kg-1). Finally, the PK profile of the active N5-substituted compound shows a plasma half-life of 32.7 min, and rapid conversion into the parent unsubstituted analog. Together, these data indicate that halogenated pyrrolo[3,2-d]pyrimidines present a promising lead into potent antiproliferative agents with tunable activity and toxicity, and rapid metabolism The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Synthetic Route of 626-48-2

The Article related to antitumor halogenated pyrrolo pyrimidine preparation toxicity pharmacokinetics prodrug, anticancer, antiproliferative, prodrugs, pyrrolopyrimidines, triple-negative breast cancer and other aspects.Synthetic Route of 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ramana, M. M. V.; Pawar, Sanjay C. published an article in 2015, the title of the article was A novel and expedient synthesis of 1,3-dialkyl-6-methylpyrimidinediones.Application of 626-48-2 And the article contains the following content:

A series of 1,3-dialkyl-6-methylpyrimidinediones I [R = Me, Et, n-Pr, i-Pr, n-Bu, s-Bu] was synthesized via double Chapman rearrangement of 2,4-dialkoxy-6-methylpyrimidines under conventional heating as well as microwave irradiation 2,4-Dialkoxy-6-methylpyrimidines were prepared by condensation of 2,4-dichloro-6-methylpyrimidine with various alcs. Microwave-assisted method with the advantages of reduced reaction times and better reaction yields, provided a simpler and environmentally friendly alternative for conventional procedures. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Application of 626-48-2

The Article related to dialkyl pyrimidinedione preparation green chem, dialkoxy pyrimidine preparation double chapman rearrangement microwave irradiation, dichloro pyrimidine aliphatic alc condensation and other aspects.Application of 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia