Tag: M.W=300-400

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 330786-24-8, Name is 3-(4-Phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, formurla is C17H13N5O. In a document, author is Ladds, Marcus J. G. W., introducing its new discovery. Application In Synthesis of 3-(4-Phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine.

Exploitation of dihydroorotate dehydrogenase (DHODH) and p53 activation as therapeutic targets: A case study in polypharmacology

The tenovins are a frequently studied class of compounds capable of inhibiting sirtuin activity, which is thought to result in increased acetylation and protection of the tumor suppressor p53 from degradation. However, as we and other laboratories have shown previously, certain tenovins are also capable of inhibiting autophagic flux, demonstrating the ability of these compounds to engage with more than one target. In this study, we present two additional mechanisms by which tenovins are able to activate p53 and kill tumor cells in culture. These mechanisms are the inhibition of a key enzyme of the de novo pyrimidine synthesis pathway, dihydroorotate dehydrogenase (DHODH), and the blockage of uridine transport into cells. These findings hold a 3-fold significance: first, we demonstrate that tenovins, and perhaps other compounds that activate p53, may activate p53 by more than one mechanism; second, that work previously conducted with certain tenovins as SirT1 inhibitors should additionally be viewed through the lens of DHODH inhibition as this is a major contributor to the mechanism of action of the most widely used tenovins; and finally, that small changes in the structure of a small molecule can lead to a dramatic change in the target profile of the molecule even when the phenotypic readout remains static.

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Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Safety of 3-(4-Phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 330786-24-8, Name is 3-(4-Phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, molecular formula is C17H13N5O. In an article, author is Motamedi, Milad,once mentioned of 330786-24-8.

Experimental/computational assessments of steel in HCl medium containing aminocarbonitrile-incorporated polyhydroxy-functionalized pyrido[2,3-d]pyrimidine as a green corrosion inhibitor

This research deals with insights into the inhibitory effects of a new synthetic bio/green corrosion inhibitor based on aminocarbonitrile-incorporated polyhydroxy-functionalized pyrido[2,3-d]pyrimidine derivative (PPAC) on steel substrate exposed to 1 M HCl cleaning electrolyte. The electrochemical examinations resulted in mixed corrosion inhibition activity having a paramount cathodic hindrance with ca. 91% reduction in corrosion current density (i(corr)) and also 92.5% inhibition efficiency (eta%) achievement after 6 h steel exposing to 0.5 mM PPAC/ HCl solution. A new-route, in-situ multi-step image processing method was successfully created to extract the adsorbed hydrogen bubbles on the electrolyte/steel interface by developing a mathematical exponentiated model. The model based on image-based shape descriptors precisely reproduced the electrochemical data with errors of less than 13%. A low corrosion rate upon PPAC adsorption led to a considerable diminution of bubbles number, T, while their surface area, SA, increased remarkably. The variations of experimental i(corr), data against (T)(-2.09) (SA)(0.65) and also vertical bar Z vertical bar(10mHz) values against (T)(-)(0.)(3) (SA)(-)(0.)(24) showed the best correlative results (R-2 similar to 0.99).Theoretical atomic/electronic simulations relying on DFT, classical MD, and MC proved PPAC planar orientation via the donor-acceptor adsorptive mechanism of its functional groups with the greatest protonation power of C N and C=O in the pyrimidine-fused aminocarbonitrile moiety for strong spontaneous physical/chemical bondings with Fe. (C) 2020 Elsevier B.V. All rights reserved.

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Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 1981-58-4, Name is Sulfamethazine sodium, formurla is C12H13N4NaO2S. In a document, author is Materon, Elsa M., introducing its new discovery. SDS of cas: 1981-58-4.

y Role of sphingomyelin on the interaction of the anticancer drug gemcitabine hydrochloride with cell membrane models

The fight against drug resistance in chemotherapy requires a molecular-level understanding of the drug interaction with cell membranes, which today is feasible with membrane models. In this study, we report on the interaction of gemcitabine (GEM), a pyrimidine nucleoside antimetabolite used to treat pancreatic cancer, with Langmuir films that mimic healthy and cancerous cell membranes. The cell membrane models were made with eight compositions of a quaternary mixture containing 1,2-dipalmitoyl-sn-glycerol-3-phosphocholine (DPPC), 1,2-dipalmitoyl-sn-glycero-3-phosphoserine (DPPS), sphingomyelin (SM), and cholesterol (CHOL). The relative concentration of SM was increased so that four of these compositions represented cancerous cells. GEM was found to increase the mean molecular area, also increasing their surface elasticity, with stronger interactions being observed for membranes corresponding to cancerous cells. More specifically, GEM penetrated deepest in the membrane with the highest SM concentration (40 mol%), as inferred from polarization-modulated infrared reflection absorption spectroscopy (PM-IRRAS). This finding was confirmed with molecular dynamics simulations that also indicated how GEM approaches the membrane, which could be useful for guiding the design of drug delivery systems. The experimental and simulation results are consistent with the preferential attachment of GEM onto cancerous cells and highlight the role of SM on drug-cell interactions.

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Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Application of 302964-08-5, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 302964-08-5, Name is 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide, SMILES is CC1=CC=CC(Cl)=C1NC(=O)C1=CN=C(NC2=CC(Cl)=NC(C)=N2)S1, belongs to pyrimidines compound. In a article, author is Klupczynska, Agnieszka, introduce new discover of the category.

Identification and quantification of honeybee venom constituents by multiplatform metabolomics

Honeybee (Apis mellifera) venom (HBV) has been a subject of extensive proteomics research; however, scarce information on its metabolite composition can be found in the literature. The aim of the study was to identify and quantify the metabolites present in HBV. To gain the highest metabolite coverage, three different mass spectrometry (MS)-based methodologies were applied. In the first step, untargeted metabolomics was used, which employed high-resolution, accurate-mass Orbitrap MS. It allowed obtaining a broad overview of HBV metabolic components. Then, two targeted metabolomics approaches, which employed triple quadrupole MS, were applied to quantify metabolites in HBV samples. The untargeted metabolomics not only confirmed the presence of amines, amino acids, carbohydrates, and organic acids in HBV, but also provided information on venom components from other metabolite classes (e.g., nucleosides, alcohols, purine and pyrimidine derivatives). The combination of three MS-based metabolomics platforms facilitated the identification of 214 metabolites in HBV samples, among which 138 were quantified. The obtaining of the wide free amino acid profiles of HBV is one of the project’s achievements. Our study contributed significantly to broadening the knowledge about HBV composition and should be continued to obtain the most comprehensive metabolite profile of HBV.

Application of 302964-08-5, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 302964-08-5.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, 1981-58-4, Name is Sulfamethazine sodium, SMILES is CC1=CC(C)=NC([N-]S(=O)(C2=CC=C(N)C=C2)=O)=N1.[Na+], belongs to pyrimidines compound. In a document, author is Pawluczyk, Joseph M., introduce the new discover, SDS of cas: 1981-58-4.

Route evaluation and development of a practical synthesis of methyl (S)-2-chloro-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-7-carboxylate

A rapid and reliable route to methyl (S)-2-chloro-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-7-carboxylate moiety that is useful as a synthetic scaffold is described. Previously, this Boc-protected entity was prepared in 10 chemical steps starting with L-hydroxyproline with an overall yield of 0.67%. The newly developed synthetic route provided the desired target in seven chemical steps with an overall yield up to 38%. Three main issues that needed to be addressed with the previous route were; first, the ring expansion of the L-hydroxyproline that generated an inseparable regioisomeric mixture (1.5:1) by flash chromatography; secondly, the low yielding condensation step between the keto ester and urea; thirdly, the low yielding chlorination of the desired isomer. Starting with commercially available (2-chloropyrimidin-5-yl)methanol, the new route incorporates a Knochel iodination, a Negishi cross-coupling, and a ring closure as the key steps. This new route afforded us the opportunity to deliver enantiomerically pure intermediate in support of drug discovery efforts. (C) 2020 Elsevier Ltd. All rights reserved.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 1981-58-4 is helpful to your research. SDS of cas: 1981-58-4.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 764659-72-5, Name is (2R,5S)-(1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl 5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate, formurla is C18H26FN3O4S. In a document, author is Mossanen-Parsi, Amir, introducing its new discovery. Computed Properties of C18H26FN3O4S.

Histone mRNA is subject to 3 ‘ uridylation and re-adenylation in Aspergillus nidulans

The role of post-transcriptional RNA modification is of growing interest. One example is the addition of non-templated uridine residues to the 3 ‘ end of transcripts. In mammalian systems, uridylation is integral to cell cycle control of histone mRNA levels. This regulatory mechanism is dependent on the nonsense-mediated decay (NMD) component, Upf1, which promotes histone mRNA uridylation and degradation in response to the arrest of DNA synthesis. We have identified a similar system in Aspergillus nidulans, where Upf1 is required for the regulation of histone mRNA levels. However, other NMD components are also implicated, distinguishing it from the mammalian system. As in human cells, 3 ‘ uridylation of histone mRNA is induced upon replication arrest. Disruption of this 3 ‘ tagging has a significant but limited effect on histone transcript regulation, consistent with multiple mechanisms acting to regulate mRNA levels. Interestingly, 3 ‘ end degraded transcripts are also subject to re-adenylation. Both mRNA pyrimidine tagging and re-adenylation are dependent on the same terminal-nucleotidyltransferases, CutA, and CutB, and we show this is consistent with the in vitro activities of both enzymes. Based on these data we argue that mRNA 3 ‘ tagging has diverse and distinct roles associated with transcript degradation, functionality and regulation.

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Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, SMILES is ClC1=NC(=NC(=C1OC2=C(C=CC=C2)OC)Cl)C3=NC=CC=N3, in an article , author is Naikoo, Rayees Ahmad, once mentioned of 150728-13-5, Name: 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine.

7-Endo-trig Pictet-Spengler type cyclization of 5-alkylidene/arylidene-amino-3H-pyrimidin-4-ones: An efficient and diastereoselective synthesis of pyrimido[4,5-b] [1,4]benzodiazepines

The manuscript describes an efficient, atom economical synthesis of pyrimido[4,5-b][1,4]benzodiazepin-4-ones by relatively unexplored 7-endo-trig Pictet-Spengler type cyclisations. The synthetic methdodlogy involves the synthesis of different variants of 5-arylidene-amino-3H-pyrimidines and their p-toluene sulfonic acid mediated 7-endo-trig Pictet-Spengler type cyclisations to afford biologically relavent functionalized benzodiazepine condensed pyrimidinones such as pyrimido[4,5-b][1,4]benzodiazepines in good to excellent yields (82-94%).

Interested yet? Read on for other articles about 150728-13-5, you can contact me at any time and look forward to more communication. Name: 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

In an article, author is Halim, Karema N. M., once mentioned the application of 330786-24-8, HPLC of Formula: C17H13N5O, Name is 3-(4-Phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, molecular formula is C17H13N5O, molecular weight is 303.318, MDL number is MFCD20270360, category is pyrimidines. Now introduce a scientific discovery about this category.

Straightforward synthesis, antiproliferative screening, and density functional theory study of some pyrazolylpyrimidine derivatives

Tetrahydropyrimidinone derivative was synthesized through one-pot three components condensation of 1,3-diphenylpyrazole-4-carbaldehyde with pentan-2,4-dione and urea under Biginelli reaction conditions. The corresponding chloro- and hydrazino derivatives were synthesized and utilized for the construction of some valuable N-heterocycles encompassing both pyrazole and pyrimidine cores, such as triazolopyrimidine, tetrazolopyrimidine, pyrazole, and pyrazolone derivatives through condensation with nitrogen nucleophiles and carbon electrophiles. The antiproliferative activity evaluation of the synthesized compounds against four human carcinoma cell lines namely, liver carcinoma (HepG2), breast adenocarcinoma (MCF7), prostate cancer (PC3), and colon cancer (HCT-116) cell lines revealed that some of them provided significant potency, as well as the density-functional theory (DFT) was studied. The permeability of various hydrophilic and hydrophobic synthesized compounds across both normal and cancer cells is confirmed via DFT simulation in which the much higher permeability through aquaporin channels revealed the selective cytotoxicity toward cancer cells.

If you are interested in 330786-24-8, you can contact me at any time and look forward to more communication. HPLC of Formula: C17H13N5O.

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Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 139756-21-1, Name is 5-(2-Ethoxyphenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one, molecular formula is C17H20N4O2, belongs to pyrimidines compound, is a common compound. In a patnet, author is Luban, Jeremy, once mentioned the new application about 139756-21-1, Product Details of 139756-21-1.

The DHODH inhibitor PTC299 arrests SARS-CoV-2 replication and suppresses induction of inflammatory cytokines

The coronavirus disease 2019 (COVID-19) pandemic has created an urgent need for therapeutics that inhibit the SARS-COV-2 virus and suppress the fulminant inflammation characteristic of advanced illness. Here, we describe the anti-COVID-19 potential of PTC299, an orally bioavailable compound that is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), the rate-limiting enzyme of the de novo pyrimidine nucleotide biosynthesis pathway. In tissue culture, PTC299 manifests robust, dose-dependent, and DHODH-dependent inhibition of SARS-COV-2 replication (EC50 range, 2.0-31.6 nM) with a selectivity index >3,800. PTC299 also blocked replication of other RNA viruses, including Ebola virus. Consistent with known DHODH requirements for immunomodulatory cytokine production, PTC299 inhibited the production of interleukin (IL)-6, IL-17A (also called IL-17), IL-17 F, and vascular endothelial growth factor (VEGF) in tissue culture models. The combination of anti-SARS-CoV-2 activity, cytokine inhibitory activity, and previously established favorable pharmacokinetic and human safety profiles render PTC299 a promising therapeutic for COVID-19.

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Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Reference of 150728-13-5, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, SMILES is ClC1=NC(=NC(=C1OC2=C(C=CC=C2)OC)Cl)C3=NC=CC=N3, belongs to pyrimidines compound. In a article, author is Huang, Kuan-Hsiang, introduce new discover of the category.

Bridging Functional Groups Governing the Charge Transfer Dynamic in an Amorphous Carbon Nitride Allotropic Heterojunction toward Efficient Solar Hydrogen Evolution

Modulation of the charge transfer dynamic in amorphous carbon nitride allotropic heterojunctions by an alternation in bridging functional groups for the heptazine- and triazine-based fragments is demonstrated to boost the photocatalytic activity for hydrogen evolution. Pyrimidine-bridged and NH-bridged amorphous carbon nitride allotropic heterojunctions are synthesized by thermal polycondensation of a supramolecular complex. Due to the improved charge separation efficiency and visible-light harvesting ability, both allotropic heterojunctions present more than tenfold enhanced photocatalytic activities for hydrogen evolution compared to the conventional heptazine-based carbon nitride under visible-light illumination. Moreover, the photocatalytic activity of the NH-bridged carbon nitride allotropic heterojunction with type-II charge transfer dynamic is superior to the pyrimidine-bridged one with a Z-scheme characteristic. The findings in this study emphasize that the electronic structure at the heterojunction interface governed by the bridging group greatly influences the charge transfer dynamic and therefore is a crucial factor driving the photocatalytic activity of carbon nitride allotropic heterojunctions.

Reference of 150728-13-5, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 150728-13-5 is helpful to your research.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia