Tag: M.W=300-400

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 302964-08-5, Name is 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide, molecular formula is C16H13Cl2N5OS, belongs to pyrimidines compound, is a common compound. In a patnet, author is Kim, Sang-Hoon, once mentioned the new application about 302964-08-5, Name: 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide.

Structural basis for the substrate specificity and catalytic features of pseudouridine kinase from Arabidopsis thaliana

RNA modifications can regulate the stability of RNAs, mRNA-protein interactions, and translation efficiency. Pseudouridine is a prevalent RNA modification, and its metabolic fate after RNA turnover was recently characterized in eukaryotes, in the plant Arabidopsis thaliana. Here, we present structural and biochemical analyses of PSEUDOURIDINE KINASE from Arabidopsis (AtPUKI), the enzyme catalyzing the first step in pseudouridine degradation. AtPUKI, a member of the PfkB family of carbohydrate kinases, is a homodimeric alpha/beta protein with a protruding small beta-strand domain, which serves simultaneously as dimerization interface and dynamic substrate specificity determinant. AtPUKI has a unique nucleoside binding site specifying the binding of pseudourine, in particular at the nucleobase, by multiple hydrophilic interactions, of which one is mediated by a loop from the small beta-strand domain of the adjacent monomer. Conformational transition of the dimerized small beta-strand domains containing active site residues is required for substrate specificity. These dynamic features explain the higher catalytic efficiency for pseudouridine over uridine. Both substrates bind well (similar K-m), but only pseudouridine is turned over efficiently. Our studies provide an example for structural and functional divergence in the PfkB family and highlight how AtPUKI avoids futile uridine phosphorylation which in vivo would disturb pyrimidine homeostasis.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 302964-08-5. The above is the message from the blog manager. Name: 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide.

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

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 1981-58-4, Name is Sulfamethazine sodium, molecular formula is C12H13N4NaO2S. In an article, author is Zhou, Jiadi,once mentioned of 1981-58-4, Category: pyrimidines.

delta-Regioselective heteroarylation of free alcohols through 1,5-hydrogen-atom transfer

An efficient silver-catalyzed d-regioselective C(sp(3))-H heteroarylation of free alcohols has been developed. Various alcohols reacted with quinolines, isoquinoline, pyridines, pyrimidine, phthalazine, 4-hydroxyquinazoline, acridine, quinoxaline and pyrazine to give the corresponding C(sp(2))-H alkylation products in 31-89% yields. Notably, all types (1 degrees, 2 degrees, and 3 degrees) of d-C(sp(3))-H bonds in the alcohols could be regioselectively activated. This protocol provides a platform to access divergent functionalizations of alcohols and heteroaryls by forming the challenging d-selective C(sp(3))-C(sp(2)) bond.

Interested yet? Keep reading other articles of 1981-58-4, you can contact me at any time and look forward to more communication. Category: pyrimidines.

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

Synthetic Route of 764659-72-5, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 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, SMILES is O=C([C@@H]1O[C@H](N2C=C(F)C(N)=NC2=O)CS1)O[C@H]3[C@H](C(C)C)CC[C@@H](C)C3, belongs to pyrimidines compound. In a article, author is Hosokawa, Mika, introduce new discover of the category.

Optimization of Analytical Conditions for Hydrophilic Nucleic Acids Using Mixed-Mode and Reversed-Phase Pentabromobenzyl Columns

The aim of this study was to investigate appropriate analytical conditions for hydrophilic nucleosides and nucleotides (monophosphates and triphosphates) by HPLC methods using a mixed-mode AX- C18 column with anion-exchange and hydrophobic interactions by quaternary ammonium and C18, respectively, and a reversed-phase pentabromobenzyl (PBr) column with dispersion force and hydrophobic interactions by PBr group. The higher compound polarity led to stronger retention on AX-C18 (triphosphates > monophosphates > nucleosides). AX- C18 demonstrated feasible retention of nucleotides via anion-exchange interaction by increasing the salt and methanol concentrations. In contrast, on PBr, the lower compound polarity led to stronger retention. On PBr, feasible retention of both nucleosides and nucleotides was obtained via dispersion interactions with purine and pyrimidine rings by increasing the methanol concentration. Regarding the pH of phosphate buffer used as the mobile phase, pH 7.0 should be used in measuring nucleoside triphosphates on AX- C18, whereas pH 2.5 is better suited for measuring nucleotides on PBr. In terms of selectivity to highly hydrophilic nucleotides, the mixed-mode AX-C18 column had an advantage over the reverse-phase PBr column. In contrast, PBr column was more versatile than the AX-C18 column. Taken together, HPLC analyses of nucleosides and nucleotides should be carried out by optimizing the interactions between the stationary phase and nucleic acids.

Synthetic Route of 764659-72-5, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 764659-72-5 is helpful to your research.

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

Electric Literature of 139756-21-1, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 139756-21-1, Name is 5-(2-Ethoxyphenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one, SMILES is O=C1C(N(C)N=C2CCC)=C2N=C(C3=CC=CC=C3OCC)N1, belongs to pyrimidines compound. In a article, author is Ladds, Marcus J. G. W., introduce new discover of the category.

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.

Electric Literature of 139756-21-1, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 139756-21-1 is helpful to your research.

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

In an article, author is Kreppel, Andrea, once mentioned the application of 302964-08-5, Category: pyrimidines, Name is 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide, molecular formula is C16H13Cl2N5OS, molecular weight is 394.2783, MDL number is MFCD11045075, category is pyrimidines. Now introduce a scientific discovery about this category.

The Enzymatic Decarboxylation Mechanism of 5-Carboxy Uracil: A Comprehensive Quantum Chemical Study

Dynamic regulation of DNA methylation is an important process for the control of gene expression in mammals. It is believed that in the demethylation pathway of 5-methyl cytosine, the intermediate 5-carboxy cytosine (5caC) can be actively decarboxylated alongside the substitution in the base excision repair. For the active decarboxylation of 5caC, a decarboxylase has not been identified so far. Due to the similar chemistry of the decarboxylation of 5-carboxy uracil (5caU) to uracil (U) in the pyrimidine salvage pathway catalyzed by the iso-orotate decarboxylase (IDCase), the study of this reaction might give valuable insights into the active 5caC decarboxylation process. In this work, we employ quantum chemical and molecular mechanic calculations and find that the catalytic mechanism of IDCase proceeds via a direct decarboxylation mechanism. Detailed investigations on the reaction coordinate reveal that it is a one-step mechanism with concerted proton transfer and C-C bond opening.

If you are interested in 302964-08-5, you can contact me at any time and look forward to more communication. Category: pyrimidines.

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

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 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 document, author is Hill, Brian, introduce the new discover, Application In Synthesis of 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine.

A pilot clinical trial of oral tetrahydrouridine/decitabine for noncytotoxic epigenetic therapy of chemoresistant lymphoid malignancies

One mechanism by which lymphoid malignancies resist standard apoptosis-intending (cytotoxic) treatments is genetic attenuation of the p53/p16-CDKN2A apoptosis axis. Depletion of the epigenetic protein DNA methyltransferase 1 (DNMT1) using the deoxycytidine analog decitabine is a validated approach to cytoreduce malignancy independent of p53/p16. In vivo decitabine activity, however, is restricted by rapid catabolism by cytidine deaminase (CDA). We, therefore, combined decitabine with the CDA-inhibitor tetrahydrouridine and conducted a pilot clinical trial in patients with relapsed lymphoid malignancies: the doses of tetrahydrouridine/decitabine used (similar to 10/0.2 mg/kg orally (PO) 2x/week) were selected for the molecular pharmacodynamic objective of non-cytotoxic, S-phase dependent, DNMT1-depletion, guided by previous Phase 1 studies. Patients with relapsed/refractory B- or T-cell malignancies (n = 7) were treated for up to 18 weeks. Neutropenia without concurrent thrombocytopenia is an expected toxicity of DNMT1-depletion and occurred in all patients (Grade 3/4). Subjective and objective clinical improvements occurred in 4 of 7 patients, but these responses were lost upon treatment interruptions and reductions to manage neutropenia. We thus performed parallel experiments in a preclinical in vivo model of lymphoma to identify regimen refinements that might sustain DNMT1-targeting in malignant cells but limit neutropenia. We found that timed-alternation of decitabine with the related molecule 5-azacytidine, and combination with inhibitors of CDA and de novo pyrimidine synthesis could leverage feedback responses of pyrimidine metabolism to substantially increase lymphoma cytoreduction but with less neutropenia. In sum, regimen innovations beyond incorporation of a CDA-inhibitor are needed to sustain decitabine DNMT1-targeting and efficacy against chemo-resistant lymphoid malignancy. Such potential solutions were explored in preclinical in vivo studies. (C) 2020 Elsevier Inc. 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 150728-13-5 is helpful to your research. Application In Synthesis of 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine.

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

Reference of 1981-58-4, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 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 article, author is Suprun, Elena, V, introduce new discover of the category.

Deoxyuridine triphosphates modified with tyrosine or tryptophan aromatic groups for direct electrochemical detection of double-stranded DNA

Deoxyuridine triphosphates (dUTP) modified with tyrosine or tryptophan aromatic groups attached through CH=CH-CH2-NH-C(O)-(CH2)(n)- linker at the C5 position of the pyrimidine ring and the corresponding products of polymerase chain reaction (PCR) were studied by cyclic and square wave voltammetry on carbon screen printed electrodes. A strong effect of the additional functional groups on the electrochemical activity of nucleotides was revealed. In particular, 5-aminoallyl-2′-deoxyuridine-5′-triphosphates modified with indole acetic, indole-3-propionic, indole-4-butyric, or 4-hydroxyphenylacetic acids demonstrated novel well-defined oxidation peaks at 0.5-0.7 V, similar to tryptophan or tyrosine amino acids, respectively. The oxidation potential maxima for dUTP derivatives under study were about 0.2-0.3 V less positive than the oxidation potential of dGTP (the most easily oxidizable nucleotide). Moreover, dUTP derivatives modified with tyrosine or tryptophan aromatic groups were incorporated by PCR into dsDNA fragments (amplicons) instead of dITP. The PCR-generated dsDNA fragments with modified nucleotides were detected through the oxidation of their electroactive ‘labels’ at micromolar concentrations, while no oxidation peaks were observed for unmodified amplicons under the same conditions. The tyrosine and tryptophan aromatic groups well complement the existing palette of electroactive tags for direct detection of nucleic acids. Compared to other electroactive ‘labels’, the main advantage of the developed oxidizable moieties is a good compatibility with polymerase enzymes including those used in PCR. In addition, the demonstrated signal recording procedure for modified amplicons on disposable carbon electrodes renders itself suitable for in situ analysis of biological samples for biochemical and medical applications. (C) 2020 Elsevier Ltd. All rights reserved.

Reference of 1981-58-4, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 1981-58-4.

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

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, molecular formula is , belongs to pyrimidines compound. In a document, author is Basu, Kallol, Recommanded Product: 150728-13-5.

Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 3: Development of a One-Pot Formylation-Cyclization Sequence to the Diaminopyrimidine Core

The development of a safe, robust, and efficient manufacturing route for the synthesis of diaminopyrimidine 1, a key intermediate to gefapixant citrate (MK-7264), is described. A full mechanistic understanding of the cyclization step in the presence of guanidine was established by performing isotopic labeling experiments and identification of impurities. Guided by the mechanistic understanding, further attempts to modify the cyclization reaction by employing additives to reduce the triazine (9) formation and guanidine loading will also be presented. This newly developed method delivered compound 1 in 88-94% yield on a commercial scale and addressed the shortcomings of the early synthetic route including high PMI, low atom economy, long cycle-time, and multiple purifications to achieve the desired quality.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 150728-13-5, in my other articles. Recommanded Product: 150728-13-5.

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

Application of 764659-72-5, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 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, SMILES is O=C([C@@H]1O[C@H](N2C=C(F)C(N)=NC2=O)CS1)O[C@H]3[C@H](C(C)C)CC[C@@H](C)C3, belongs to pyrimidines compound. In a article, author is Zhang, Tian-Yi, introduce new discover of the category.

Synthesis and evaluation of ursolic acid-based 1,2,4-triazolo[1,5-a]pyrimidines derivatives as anti-inflammatory agents

Here, two series of novel ursolic acid-based 1,2,4-triazolo[1,5-a]pyrimidines derivatives were synthesized and screened for their anti-inflammatory activity by evaluating their inhibition effect of using LPS-induced inflammatory response in RAW 264.7 macrophages in vitro; the effects of different concentrations of the compounds on the secretion of nitric oxide (NO) and inflammatory cytokines including TNF-alpha and IL-6 were evaluated. Their toxicity was also assessed in vitro. Results showed that the most prominent compound 3 could significantly decrease production of the above inflammatory factors. Docking study was performed for the representative compounds 3, UA, and Celecoxib to explain their interaction with cyclooxygenase-2 (COX-2) receptor active site. In vitro enzyme study implied that compound 3 exerted its anti-inflammatory activity through COX-2 inhibition.

Application of 764659-72-5, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 764659-72-5.

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

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 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. In a document, author is Verma, Vaijinath A., introduce the new discover, Recommanded Product: 5-(2-Ethoxyphenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one.

Synthesis of novel indolo[3,2-c]isoquinoline derivatives bearing pyrimidine, piperazine rings and their biological evaluation and docking studies against COVID-19 virus main protease

A series of hybrid indolo[3,2-c]isoquinoline (delta-carboline) analogs incorporating two pyrimidine and piperizine ring frameworks were synthesized. Intending biological activities and SAR we propose replacements of fluorine, methyl and methoxy of synthetic compounds for noteworthy antimicrobial, antioxidant, anticancer and anti-tuberculosis activities. Among these compounds 3a, 4a and 5e were progressively strong against E. coli and K. pneumonia. Whereas, compounds 4a, 5a and 6a with addition of various functional groups (OCH3, CH3) were excellent against S. aureus and B. subtilis. Compound 5c exhibited strong RSA and dynamic ferrous ion (Fe2+) metal chelating impact with IC50 of 7.88 +/- 0.93 and 4.06 +/- 0.31 mu g/mL, respectively. Compound 5e was considerably cytotoxic against all cancer cells displaying activity better than the standard drug. Compounds 6b and 6e inhibited M. tuberculosis (MIC 1.0 mg/L) considerably. Molecular docking studies indicate that compounds 4d, 5a, 5b, 6b and 6f exhibited good interactions with 6LZE (COVID-19) and 6XFN (SARS-CoV-2) at active sites. The structure of the synthesized compounds were elementally analyzed using IR, H-1, C-13 NMR and mass spectral information. (C) 2020 Elsevier B.V. All rights reserved.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 139756-21-1. Recommanded Product: 5-(2-Ethoxyphenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one.

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