Day: October 20, 2022

Filip, Jiri; Skoda, Jan; Hradec, Hynek published the artcile< Preparation of 6-azauracil-5-t and 6-azauridine-5-t of high molar activity>, Name: 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione, the main research area is tritium label azauracil azauridine; stability tritium label.

Catalytic reductive dehalogenation of 5-bromo-6-azauracil with carrier-free T gave 6-azauracil-5-3H of a molar activity of 19.0Ci/mmole. The conditions for the catalytic reductive dehalo-genation were examined in tracer experiments Microbial transformation gave 6-azauridine-5-3H from 6-azauracil-5-3H having molar activity of 18.8 Ci/mmole. The stability of T was investigated in aqueous medium at 100°C.

Journal of Labelled Compounds published new progress about Exchange reaction. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Name: 6-Bromo-1,2,4-triazine-3,5(2H,4H)-dione.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Yang, Zhuang; Shen, Mingsheng; Tang, Minghai; Zhang, Wanhua; Cui, Xue; Zhang, Zihao; Pei, Heying; Li, Yong; Hu, Mengshi; Bai, Peng; Chen, Lijuan published the artcile< Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy>, Safety of Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is oxadiazole hydroxamic acid preparation histone deacetylase inhibitor human cancer; 1,2,4-Oxadiazole; Anticancer; Antiproliferative; HDAC.

In this study, a series of novel HDAC inhibitors containing 1,2,4-oxadiazole as the cap group, were synthesized and evaluated in vitro. Compound I, displayed the most potent histone deacetylase (HDAC) inhibition, especially against HDAC1, 2, and 3 with IC50 values of 1.8, 3.6 and 3.0 nM, resp. In vitro antiproliferative studies confirmed that I was more potent than SAHA, with IC50 values against 12 types of cancer cell lines ranging from 9.8 to 44.9 nM. The results of Western blot assays showed that compound I can significantly up-regulate the acetylation of the biomarker his-H3 and mol. docking analyses revealed the mode of action of compound I against HDAC1. The results of flow-cytometry anal. suggested that the above compound induces cell cycle arrest at the G1 phase and has apoptotic effects and further investigation of the activity on the primary cells of three patients, showed IC50 values of 21.3, 61.1, and 77.4 nM. More importantly, an oral bioavailability of up to 53.52% was observed for compound I. An in vivo pharmacodynamic evaluation demonstrated that compound I can significantly inhibit tumor growth in a Daudi Burkitt’s lymphoma xenograft model, with tumor inhibition rates of 53.8 and 46.1% observed at 20 and 10 mg/kg when administered p.o. and i.v., resp. These results indicate that compound I may be a suitable lead for further evaluation and development as an HDAC inhibitors and potent anticancer agents.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Safety of Ethyl 2-chloropyrimidine-5-carboxylate.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Zhang, Hongwang; Zhou, Longhu; Amichai, Sarah; Zandi, Keivan; Cox, Bryan; Schinazi, Raymond; Amblard, Franck published the artcile< Novel influenza polymerase PB2 inhibitors for the treatment of influenza A infection>, Application In Synthesis of 18740-39-1, the main research area is pimodivir derivative preparation influenza A infection polymerase PB2 inhibitor; Antiviral; Flu; Influenza A; Virus.

Exploration of the chem. space of known influenza polymerase PB2 inhibitor Pimodivir, was performed by our group. We synthesized and identified compounds I and II, two novel thienopyrimidine derivatives displaying anti-influenza A activity in the single digit nanomolar range in cell culture. Binding of these unique compounds in the influenza polymerase PB2 pocket was also determined using mol. modeling.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiviral agents (anti-influenza A). 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Application In Synthesis of 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adriaens, E. L.; Lozet, F. published the artcile< Fermented beverages of Ruanda natives>, Computed Properties of 3921-01-5, the main research area is .

The preparation of hydromel (I), and banana (II) and sorgho (III) beers is described. I contained before and after fermentation: dry extract 365.26-115.28, inorganic matter 10.78-6.20, total N 3.15-1.93, reducing sugars in glucose 250.0-66.11, sucrose 12.45-4.29, acidity as H2SO4 1.62-5.78 g./l.; in the wort: wax and sorgho yeast 86.9 g./l.; in the I EtOH 8.6°. Corresponding data for II were: 197.12-52.63, 11.14-9.87, trace-3.15, 93.74-19.16, 80.29-2.95, 3.28-4.21 g./l. and EtOH in the end product 9.46°. “”Inkanganza”” made from II with addition of honey and sorgho yeast gave, before and after fermentation: 149.2-52.88, 10.88-5.34, 5.08-3.75, 116.54-12.45, 11.91-4.33, 4.9-3.92 g./l., EtOH 11.5°. Wort of III and the end product contained: dry extract 172.9-256.8, inorganic 5.16-6.86, N 6.08-26.56, glucose 43.02-trace, sucrose 5.57-16.06, acids 2.11-5.98 g./l., EtOH 3.75°. Uryama, a III containing about 10% honey, gave: 244.83-136.24, 7.08-7.37, 10.68-3.15, 105.17-37.43, trace-0.0, 3.92-10.15 g./l., EtOH 6.4°.

Bull. Agr. Congo Belge published new progress about Beer. 3921-01-5 belongs to class pyrimidines, and the molecular formula is C4H2Br2N2, Computed Properties of 3921-01-5.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reddy, L. Srikanth; Naik, B. Eswara published the artcile< Design,synthesis and structural elucidation of some novel heterocyclic molecules derived from thieno [2, 3-d] pyrimidine nucleus>, Product Details of C6H2Cl2N2S, the main research area is phenyl thienotriazolopyrimidine preparation.

Several new thieno[2,3-d]pyrimidine derivtives, 3-substituted phenyl-5-(thiophen-2- yl)thieno[3,2-e][1,2,4]triazolo[4,3-c]pyrimidines were synthesized starting from thieno[2,3-d]pyrimidine-2,4-diol. The characterization of the newly synthesized compounds was established by IR, 1H NMR, 13C NMR and mass Spectral anal.

Heterocyclic Letters published new progress about Aromatic carboxylic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Product Details of C6H2Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Guan, Aiying; Wang, Mingan; Yang, Jinlong; Wang, Lizeng; Xie, Yong; Lan, Jie; Liu, Changling published the artcile< Discovery of a New Fungicide Candidate through Lead Optimization of Pyrimidinamine Derivatives and Its Activity against Cucumber Downy Mildew>, Formula: C5H4Cl2N2O, the main research area is fungicide pyrimidinamine derivative preparation lead optimization cucumber downy mildew; development of resistance; downy mildew; pyrimidinamine fungicide candidate; unique mode of action.

Downy mildew is one of the most highly destructive of the diseases that cause damage to fruits and vegetables. Because of the continual development of resistance, it is important to discover new fungicides with different modes of action from existing fungicides for the control of downy mildew. This study is a continuation of our previous work on the novel pyrimidinamine lead compound, (I), and includes field trials for the identification of the optimal candidate. A new compound, 5-Chloro-N-(2-(6-(4-chlorophenoxy)pyridin-3yl)ethyl)-6-(difluoromethyl)pyrimidin-4-amine, (II), was obtained from 4,5-Dichloro-6-(difluoromethyl)pyrimidine and 2-(6-(4-chlorophenoxy)pyridin-3-yl)ethanamine, which gave a lower EC50 value (0.10 mg/L) against downy mildew than lead compound I (0.19 mg/L) and the com. fungicides diflumetorim, dimethomorph, and cyazofamid (1.01-23.06 mg/L). Compound II displayed similar broad-spectrum fungicidal activity to compound I but better field efficacy than compound I, cyazofamid, and flumorph. The present work indicates that pyrimidinamine compound II is a candidate for further development as a com. fungicide for the control of downy mildew.

Journal of Agricultural and Food Chemistry published new progress about Agrochemical fungicides. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, Formula: C5H4Cl2N2O.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Rao, T. Sudhakar; Revankar, Ganapathi R. published the artcile< Synthesis of certain alkenyl purines and purine analogs>, Product Details of C7H8N4O, the main research area is alkenyl purine analog.

Synthesis of alkenyl derivatives of certain purines and purine analogs is described. Direct alkylation of the sodium salt of 6-chloropurine with 1-bromo-2-pentene or 4-bromo-2-methyl-2-butene in N,N-dimethylformamide furnished N-7, and N-9 alkenyl derivatives Similar alkylation of 2-amino-6-chloropurine provided the corresponding N-7, and N-9 alkenyl derivatives Acid hydrolysis of these chloro derivatives furnished the corresponding alkenyl hypoxanthines or alkenyl guanines. The direct alkylation of pyrrolo[2,3-d]pyrimidin-4(3H)-one gave N-3 alkenyl derivatives; the N-7 alkenyl derivatives were prepared starting from the 4-chloro derivatives Synthesis of 2-amino-7-(2-penten-1-yl)pyrrolo[2,3-d]pyrimidin-4(3H)-one was accomplished starting from 2-amino-4-methoxypyrrolo[2,3-d]pyrimidine. These alkenyl derivatives were found to be devoid of anti-HCMV activity in vitro.

Journal of Heterocyclic Chemistry published new progress about Alkenylation. 84955-32-8 belongs to class pyrimidines, and the molecular formula is C7H8N4O, Product Details of C7H8N4O.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Raubo, Piotr; Carbajo, Rodrigo J.; McCoull, William; Raubo, Joanna; Thomas, Morgan published the artcile< Diversity-orientated synthesis of macrocyclic heterocycles using a double SNAr approach>, Reference of 18740-39-1, the main research area is macrocyclic heterocycle preparation enantioselective diastereoselective regioselective antitumor activity microwave.

An efficient macrocyclization approach based on the double aromatic nucleophilic substitution (SNACK) was developed. This methodol. allows a facile incorporation of heterocyclic motifs into macrocyclic rings and rapid synthesis of a significant number of structurally diverse macrocycles e.g., I. SNACK macrocyclization enables preparation of stable diastereoisomers of conformationally restricted macrocycles (atropisomers) e.g., II and e.g., III. Practical application of SNACK macrocyclization in a drug discovery project was exemplified by the identification of high affinity macrocyclic binders of B-cell lymphoma 6 (BCL6).

Organic & Biomolecular Chemistry published new progress about Antitumor agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Reference of 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

O’Brien, Darrell E.; Weinstock, Louis T.; Springer, Robert H.; Cheng, Chia-Chung published the artcile< Pyrimidines. XIX. Pyrimidol[4,5 - e]dihydro - 1,3-oxazines and related compounds>, Category: pyrimidines, the main research area is PYRIMIDO DIHYDRO OXAZINES; OXAZINES PYRIMIDO DIHYDRO.

A number of 2-substituted 4,5-dihydroxy-6-(substituted aminomethyl)pyridimines (I) were prepared from the corresponding 2-substituted 4,5-dihydroxypyrimidines by a new pyrimidine Mannich reaction. The structure of I was proved by an independent synthesis. Further study of this reaction led to the synthesis of pyrimido[4,5-e]dihydro-1,3-oxazines (II). 24 references.

Journal of Heterocyclic Chemistry published new progress about Mannich reaction. 15837-41-9 belongs to class pyrimidines, and the molecular formula is C4H4N2O2, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia