Day: October 26, 2022

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

Referemce:
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

Referemce:
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

Referemce:
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

On October 26, 2020, Curti, Claudio; Rassu, Gloria; Lombardo, Marco; Zambrano, Vincenzo; Pinna, Luigi; Battistini, Lucia; Sartori, Andrea; Pelosi, Giorgio; Zanardi, Franca published an article.Application of 626-48-2 The title of the article was Unlocking Access to Enantiopure Fused Uracils by Chemodivergent [4+2] Cross-Cycloadditions: DFT-Supported Homo-Synergistic Organocatalytic Approach. And the article contained the following:

The discovery of chem. methods enabling the construction of carbocycle-fused uracils which embody a three-dimensional and functional-group-rich architecture is a useful tool in medicinal chem. oriented synthesis. In this work, an unprecedented amine-catalyzed [4+2] cross-cycloaddition is documented; it involves remotely enolizable 6-methyluracil-5-carbaldehydes and β-aryl enals, and chemoselectively produces two novel bicyclic and tricyclic fused uracil chemotypes in good yields with a maximum level of enantiocontrol. In-depth mechanistic investigations and control experiments support an intriguing homo-synergistic organocatalytic approach, where the same amine organocatalyst concomitantly engages both aldehyde partners in a stepwise eliminative [4+2] cycloaddition, whose vinylogous iminium ion intermediate product may diverge-depending upon conditions-to either bicyclic targets by hydrolysis or tricyclic products by a second homo-synergistic trienamine-mediated stepwise [4+2] cycloaddition 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 uracil cinnamaldehyde chemoselective regioselective diastereoselective enantioselective organocatalysis cycloaddition, carbocycle fused uracil stereoselective preparation, asymmetric synthesis, cycloaddition, fused-ring systems, heterocycles, organocatalysis and other aspects.Application of 626-48-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Jakubiec, Dominika; Przypis, Lukasz; Suwinski, Jerzy W.; Walczak, Krzysztof Z. published an article in 2017, the title of the article was Synthesis of 5-hetaryluracil derivatives via 1,3-dipolar cycloaddition reaction.Synthetic Route of 4433-40-3 And the article contains the following content:

1,3-Dipolar cycloaddition was applied for the synthesis 5-hetaryluracil derivatives where substituted uracils played the role of 1,3-dipoles or dipolarophiles. Treatment of the nitrile oxide derived from 5-formyluracil and substituted alkenes gave the appropriate 5-(4,5-dihydroisoxazol-3-yl)pyrimidine-2,4(1H,3H)-diones, which by oxidation with N-bromosuccinimide were transformed into appropriate 5-(isoxazol-3-yl)uracils. When 5-cyanouracil was used as a dipolarophile in the reaction with nitrile oxides, generated from aromatic aldoximes, several 5-(1,2,4-oxadiazol-5-yl)uracils were obtained. An alternative reaction of 5-formyluracil with an excess of nitriles in the presence of cerium ammonium nitrate as an oxidant gave 1,2,4-oxadiazol-3-yl derivatives in moderate yields. 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 dioxopyrimidinyl aldoxime preparation alkene regioselective dipolar cycloaddition, dihydroisoxazolyl uracil preparation, nitrile dioxopyrimidinyl aldoxime dipolar cycloaddition, oxadiazoyl uracil preparation, phenyl aldoxime cyanouracil dipolar cycloaddition and other aspects.Synthetic Route of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 1, 2017, Woodring, Jennifer L.; Bachovchin, Kelly A.; Brady, Kimberly G.; Gallerstein, Mitchell F.; Erath, Jessey; Tanghe, Scott; Leed, Susan E.; Rodriguez, Ana; Mensa-Wilmot, Kojo; Sciotti, Richard J.; Pollastri, Michael P. published an article.COA of Formula: C8H10BrN3O The title of the article was Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation. And the article contained the following:

Human African trypanosomiasis (HAT) is a deadly disease in need of new chemotherapeutics that can cross into the central nervous system. The authors previously reported the discovery of (NEU-617), a small mol. with activity against T. brucei bloodstream proliferation. Further optimization of NEU-617 to improve the physicochem. properties (LogP, LLE, [1], and MPO score) [2] have led us to twelve sub-micromolar compounds, most importantly the headgroup variants I and II, and the linker variant III. Although these 3 compounds had reduced potency compared to NEU-617, they all had improved LogP, LLE and MPO scores. Cross-screening these analogs against other protozoan parasites uncovered IV with potent activity towards T. brucei, T. cruzi and L. major, while four others compounds showed activity towards P. falciparum D6. This reinforces the effectiveness of lead repurposing for the discovery of new protozoan disease therapeutics. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).COA of Formula: C8H10BrN3O

The Article related to anilinoquinazoline trypanosome inhibitor antimalarial malaria trypanosomiasis trypanosomicide, human african trypanosomiasis, leishmania major, neglected tropical disease, plasmodium falciparum, target class repurposing, trypanosoma brucei, trypanosoma cruzi and other aspects.COA of Formula: C8H10BrN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 1, 2020, Semenov, Vyacheslav E.; Zueva, Irina V.; Lushchekina, Sofya V.; Lenina, Oksana A.; Gubaidullina, Lilya M.; Saifina, Lilya F.; Shulaeva, Marina M.; Kayumova, Ramilya M.; Saifina, Alina F.; Gubaidullin, Aidar T.; Kondrashova, Svetlana A.; Latypov, Shamil K.; Masson, Patrick; Petrov, Konstantin A. published an article.Safety of 6-Methylpyrimidine-2,4(1H,3H)-dione The title of the article was 6-Methyluracil derivatives as peripheral site ligand-hydroxamic acid conjugates: Reactivation for paraoxon-inhibited acetylcholinesterase. And the article contained the following:

New uncharged conjugates of 6-methyluracil derivatives with imidazole-2-aldoxime I (n = 1, 2, 3, 4) and 1,2,4-triazole-3-hydroxamic acid units II (n = 2, 3, 4) were synthesized and studied as reactivators of organophosphate-inhibited cholinesterase. Using paraoxon (POX) as a model organophosphate, it was shown that 6-methyluracil derivatives linked with hydroxamic acid are able to reactivate POX-inhibited human acetylcholinesterase (AChE) in vitro. The reactivating efficacy of one compound II (n = 3) is lower than that of pyridinium-2-aldoxime (2-PAM). Meanwhile, unlike 2-PAM, in vivo study showed that the lead compound II (n = 3) is able: (1) to reactivate POX-inhibited AChE in the brain; (2) to decrease death of neurons and, (3) to prevent memory impairment in rat model of POX-induced neurodegeneration. The experimental process involved the reaction of 6-Methylpyrimidine-2,4(1H,3H)-dione(cas: 626-48-2).Safety of 6-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to methyluracil imidazole aldoxime triazole hydroxamic acid preparation mol docking, reactivator paraoxon acetylcholinesterase butyrylcholinesterase inhibitor, 3,6-dimethyluracil, acetylcholinesterase, hydroxamic acids, molecular modeling, paraoxon, reactivator and other aspects.Safety of 6-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia