Category: 4956-05-2

Lee, Kuan Han; Han, Chein Hwa; Hwang, Long Chih; Wang, Eng Chi; Tzeng, Cherng Chyi published the artcile< Acyclic nucleosides. Part 3: Synthesis of certain 1-[(1,3-dihydroxy-2-propoxy)methyl]-6-azauracils as potential antiviral agents>, Category: pyrimidines, the main research area is acyclic nucleoside azauracil preparation virucide; hydroxypropoxymethylazauracil acyclic nucleoside.

A number of 6-azauracils were trimethylsilylated and then coupled with 1,3-dibenzyloxy-2-chloromethoxypropane to give 1-[(1,3-dibenzyloxy-2-propoxy)methyl]-6-azauracils which were debenzylated with either BCl3 or Pd2O to yield the title compounds I (R = H, Me, Cl, Br).

Gaoxiong Yixue Kexue Zazhi published new progress about Acyclonucleosides Role: SPN (Synthetic Preparation), PREP (Preparation). 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Riederer, Heinz; Huettermann, Juergen; Symons, Martyn C. R. published the artcile< Matrix-isolation of free radicals from 5-halouracils. 2. Electron spin resonance of hydrogen atom reactions in acidic glasses>, Electric Literature of 4956-05-2, the main research area is hydrogen atom nucleic acid constituent; nucleoside hydrogen atom; nucleotide hydrogen atom; uracil hydrogen atom; ESR nucleic acid constituent; radical nucleic acid constituent.

The reaction of H· atoms produced in acidic glasses (H2SO4 and H3PO4) by radiolysis and photolysis with the nucleic acid constituents by uracil, thymine, and the row of 5-halo-substituted uracils as well as their nucleoside (nucleotide) derivatives and deoxyribose were studied by ESR spectroscopy. With the pyrimidines, addition at either site of the 5,6 double bond was the only reaction, the relative yield of 5-yl or 6-yl radicals depending largely on the nature of the nonhydrogen 5 or 6 substituent. The spectral parameters of both radical types were determined by spectra simulation. In deoxyribose, abstraction of a carbon-bound hydrogen takes place from probably only 2 initial sites, the corresponding radicals undergoing a fast and a slow secondary reaction. In nucleosides (nucleotides), the base and deoxyribose (deoxyribose phosphate) moiety react independently. The relative yield of both subgroup radicals was determined and explained in terms of a “”miss or react”” mechanism. The findings are discussed in terms of solid-state vs. liquid solution type reaction mechanisms.

Journal of Physical Chemistry published new progress about ESR (electron spin resonance). 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Electric Literature of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Purkayastha, Subhasish; Lazrek, Bihi H.; Panzica, Raymond P.; Naguib, Fardos N. M.; El Kouni, Mahmoud H. published the artcile< as-Triazine acyclonucleosides: potential inhibitors of pyrimidine enzymes>, Synthetic Route of 4956-05-2, the main research area is triazine acyclonucleoside; nucleoside acyclo triazine; pyrimidine enzyme inhibitor acyclonucleoside.

Seven as-triazine-3,5-dione acyclonucleosides I (R = Ac, H, R1 = SCH2Ph, Br, H; R = H, R1 = NH2) were prepared starting with the alkylation of the corresponding O-trimethylsilylated as-triazine-3,5-diones with AcOCH2CH2OCH2Br. I were evaluated as inhibitors of orotate phosphoribosyltransferase (OPRTase, EC 2.4.2.10), orotidine 5′-monophosphate decarboxylase (ODCase, EC 4.1.2.23), uridine phosphorylase (UrdPase, EC 2.4.2.3), and thymidine phosphorylase (dThdPase, EC 2.4.2.4). I did not inhibit any of these enzymes.

Nucleosides & Nucleotides published new progress about 4956-05-2. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Synthetic Route of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sanemitsu, Yuzuru; Nakayama, Yoshinori; Tanabe, Yoo; Matsumoto, Hiroshi; Hashimoto, Shunichi published the artcile< 5-Substituted amino-3,6-dichloro-1,2,4-triazines as new potential herbicides>, Safety of 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione, the main research area is herbicide triazine structure activity.

5-Substituted 3,6-dichloro-1,2,4-triazines were tested for their preemergent herbicidal activity against 3 weeds, Echinochloa crus-galli, Scirpus juncoides, and Eleocharia acicularis. The activity was related to the structure, e.g., 5-tert-butylamino- and 5-anilino-3,6-dichloro-1,2,4-triazine derivatives exhibited strong herbicidal activity, whereas, Me, OMe, PhO at the 5-position decreased the activity. Also, derivatives with substitution at the 3- and/or 6-position failed to product activity. 5-Diisopropylamino- and 2,6-dimethylpiperidino-1,2,4-triazines were selected as promising new herbicides.

Agricultural and Biological Chemistry published new progress about Echinochloa crus-galli. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Safety of 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hin, Niyada; Duvall, Bridget; Ferraris, Dana; Alt, Jesse; Thomas, Ajit G.; Rais, Rana; Rojas, Camilo; Wu, Ying; Wozniak, Krystyna M.; Slusher, Barbara S.; Tsukamoto, Takashi published the artcile< 6-Hydroxy-1,2,4-triazine-3,5(2H,4H)-dione Derivatives as Novel D-Amino Acid Oxidase Inhibitors>, Quality Control of 4956-05-2, the main research area is hydroxytriazinedione preparation amino acid oxidase inhibitor.

A series of 2-substituted 6-hydroxy-1,2,4-triazine-3,5(2H,4H)-dione derivatives were synthesized as inhibitors of D-amino acid oxidase (DAAO). Many compounds in this series were found to be potent DAAO inhibitors, with IC50 values in the double-digit nanomolar range. The 6-hydroxy-1,2,4-triazine-3,5(2H,4H)-dione pharmacophore appears metabolically resistant to O-glucuronidation unlike other structurally related DAAO inhibitors. Among them, compound I was found to be selective over a number of targets and orally available in mice. Furthermore, oral coadministration of D-serine with I enhanced the plasma levels of D-serine in mice compared to the oral administration of D-serine alone, demonstrating its ability to serve as a pharmacoenhancer of D-serine.

Journal of Medicinal Chemistry published new progress about Alkylation. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Quality Control of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Mohammadi, Ali; Eshghi, Hossein; Bakavoli, Mehdi; Hadizadeh, Farzin; Moradi, Hassanali published the artcile< Synthesis of novel 3-substituted-5H-benzo[5,6][1, 4]thiazino[3,2-e][1,2,4]triazines and their 15-lipoxygenase inhibitory activity>, Synthetic Route of 4956-05-2, the main research area is benzothiazinotriazine preparation mol docking lipoxygenase inhibitor.

A new group of 3-substituted-5H-benzo[5,6][1,4]thiazino[3,2-e][1,2,4]triazines I (R = morpholin-4-yl, pyrrolidin-1-yl, 4-methylpiperidin-1-yl, etc.) was designed, synthesized and evaluated as inhibitors of 15-lipoxygenase (15-LO), and the results were compared with those of standard ligand 4-methyl-2-(4-methylpiperazin-1-yl)pyrimido[4,5-b][1,4]benzothiazine (4-MMPB). Among the newly designed ligands I, compound I (R = 4-phenylpiperazin-1-yl) showed the best IC50 of 15-LO inhibition (IC50 = 38 μM). The docking calculations were performed in MOE software based on the function of force-field scoring, in order to study the interaction of these new compounds I and standard ligand with 15-LO. The docking study implied that these ligands I have hydrogen bond interaction with the residue of active site of 15-LO.

Journal of the Iranian Chemical Society published new progress about Cyclic amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Synthetic Route of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Matyugina, Elena; Novikov, Mikhail; Babkov, Denis; Ozerov, Alexander; Chernousova, Larisa; Andreevskaya, Sofia; Smirnova, Tatiana; Karpenko, Inna; Chizhov, Alexander; Muthu, Pravin; Lutz, Stefan; Kochetkov, Sergei; Seley-Radtke, Katherine L.; Khandazhinskaya, Anastasia L. published the artcile< 5-Arylaminouracil Derivatives: New Inhibitors of Mycobacterium tuberculosis>, HPLC of Formula: 4956-05-2, the main research area is arylaminouracil preparation Mycobacterium tuberculosis tuberculostatic; Mycobacterium tuberculosis; carbocyclic nucleosides; uracil derivatives.

Three series of 5-arylaminouracil derivatives, including 5-(phenylamino)uracils, 1-(4′-hydroxy-2′-cyclopenten-1′-yl)-5-(phenylamino)uracils, and 1,3-di-(4′-hydroxy-2′-cyclopenten-1′-yl)-5-(phenylamino)uracils, were synthesized and screened for potential antimicrobial activity. Most of compounds had a neg. effect on the growth of the Mycobacterium tuberculosis H37Rv strain, with 100% inhibition observed at concentrations between 5 and 40 μg/mL. Of those 1-(4′-hydroxy-2′-cyclopenten-1′-yl)-3-(4”’-hydroxy-2”’-cyclopenten-1”’-yl)-5-(4”-butyloxyphenylamino)uracil proved to be the most active among tested compounds against the M. tuberculosis multidrug-resistant strain MS-115 (MIC90 5 μg/mL). In addition, the thymidylate kinase of M. tuberculosis was evaluated as a possible enzymic target.

Chemical Biology & Drug Design published new progress about Mycobacterium tuberculosis. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, HPLC of Formula: 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Dao, Pascal; Lietha, Daniel; Etheve-Quelquejeu, Melanie; Garbay, Christiane; Chen, Huixiong published the artcile< Synthesis of novel 1,2,4-triazine scaffold as FAK inhibitors with antitumor activity>, Reference of 4956-05-2, the main research area is arylamino chlorotriazine preparation antitumor agent FAK inhibitor; structure arylamino chlorotriazine inhibition FAK antitumor activity; mol docking calculation methoxymorpholinylphenylamino methylcarbamoylphenyl chlorotriazine; 1,2,4-Triazines; Anti-cancer activity; FAK inhibitors; Molecular docking; Synthesis.

Bis(arylamino)chloro-1,2,4-triazines I [R = 3,4,5-(MeO)3C6H2, 4-H2NCH2C6H4, 4-Cl-2-MeO-5-MeC6H2, 4-(4-morpholinyl)phenyl, 2-MeO-4-(4-morpholinyl)phenyl; R1 = 3-MeSO2NHC6H4, 2-MeNHCOC6H4] were prepared as inhibitors of focal adhesion kinase (FAK) for potential use as antitumor agents; their inhibition of FAK, of human cancer cells, and of tumorigenesis in cancer cells was determined I [R = 2-MeO-4-(4-morpholinyl)phenyl; R1 = 2-MeNHCOC6H4] inhibited FAK with an IC50 value of 230 nM and was toxic to cancer cells with IC50 values of 13 μM and 0.19 μM; colony formation in cancer cells was inhibited by I [R = 2-MeO-4-(4-morpholinyl)phenyl; R1 = 2-MeNHCOC6H4] with IC50 values of 1.5 μM and 1.0 μM. The structure of I [R = 2-MeO-4-(4-morpholinyl)phenyl; R1 = 2-MeNHCOC6H4] bound to FAK was determined by mol. docking calculations

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Reference of 4956-05-2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Mitran, Raul-Augustin; Draghici, Constantin; Tomas, Stefan published the artcile< New 6-azauracil derivatives>, Recommanded Product: 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione, the main research area is aromatic amine bromoazauracil nucleophilic substitution; phenol bromoazauracil nucleophilic substitution; aryl azauracil preparation.

Six new 6-azauracil derivatives were obtained through the nucleophilic substitution of 5-bromo-6-azauracil with various aromatic amines and phenols. These compounds were characterized by means of UV-VIS, IR and 1H-NMR spectroscopy.

Revista de Chimie (Bucharest, Romania) published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Recommanded Product: 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Matyugina, Elena; Novikov, Mikhail; Babkov, Denis; Ozerov, Alexander; Chernousova, Larisa; Andreevskaya, Sofia; Smirnova, Tatiana; Karpenko, Inna; Chizhov, Alexander; Muthu, Pravin; Lutz, Stefan; Kochetkov, Sergei; Seley-Radtke, Katherine L.; Khandazhinskaya, Anastasia L. published the artcile< 5-Arylaminouracil Derivatives: New Inhibitors of Mycobacterium tuberculosis [Erratum to document cited in CA163:608335]>, Product Details of C3H2BrN3O2, the main research area is erratum arylaminouracil preparation Mycobacterium tuberculosis tuberculostatic.

On page 1387, the tenth author’s name was misspelled; the corrected name is Pravin Muthu.

Chemical Biology & Drug Design published new progress about Mycobacterium tuberculosis. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Product Details of C3H2BrN3O2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia