Category: pyrimidines

Ta-Shma, Rachel; Torres, Avital; Chevion, Mordechai; Breuer, Eli; Quntar, Abed Al Aziz; Enk, Claes D.; Srebnik, Morris published the artcile< An autoxidation study of C2 substituted pyrimidine amino reductones>, Safety of 5-Hydroxypyrimidin-4(3H)-one, the main research area is autoxidation pyrimidine amino reductone.

Three pyrimidine derivatives I (R = Me, H, SMe) , differing from isouramil(I; R = OH) and divicine (I; R = NH2) at C2, were synthesized and their autoxidation rates measured spectrophotometrically. The autoxidation rates of all five pyrimidines were correlated with σ p + values (rho = -1.28, r2 = 0.949).

Tetrahedron published new progress about Autoxidation. 15837-41-9 belongs to class pyrimidines, and the molecular formula is C4H4N2O2, Safety of 5-Hydroxypyrimidin-4(3H)-one.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ishikawa, Fumiyoshi; Kosasayama, Akira; Yamaguchi, Hitoshi; Watanabe, Yoshifumi; Saegusa, Junji; Shibamura, Seiichi; Sakuma, Kyoko; Ashida, Shinichiro; Abiko, Yasushi published the artcile< Cyclic guanidines. 14. Imidazo[1,2-a]thienopyrimidin-2-one derivatives as blood platelet aggregation inhibitors>, Recommanded Product: 2,4-Dichlorothieno[2,3-d]pyrimidine, the main research area is cyclic guanidine; imidazothienopyrimidinone preparation blood platelet; thienopyrimidinone imidazo; pyrimidinone imidazothieno; structure blood platelet imidazothienopyrimidinone; reduction ethoxycarbonylmethylation amination dichlorothienopyrimidine.

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.

Journal of Medicinal Chemistry published new progress about Blood platelet. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Recommanded Product: 2,4-Dichlorothieno[2,3-d]pyrimidine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ouyang, Yao; Xu, Xiu-Hua; Qing, Feng-Ling published the artcile< Trifluoromethanesulfonic Anhydride as a Low-Cost and Versatile Trifluoromethylation Reagent>, Recommanded Product: 2,4-Dichlorothieno[2,3-d]pyrimidine, the main research area is fluoromethanesulfonic anhydride fluoromethylation reagent photoredox catalysis pyridine activation; photoredox catalysis; pyridine; radical; trifluoromethanesulfonic anhydride; trifluoromethylation.

A large number of reagents have been developed for the synthesis of trifluoromethylated compounds However, an ongoing challenge in trifluoromethylation reaction is the use of less expensive and practical trifluoromethyl sources. We report herein the unprecedented direct trifluoromethylation of (hetero)arenes using trifluoromethanesulfonic anhydride as a radical trifluoromethylation reagent by merging photoredox catalysis and pyridine activation. Furthermore, introduction of both the CF3 and OTf groups of the trifluoromethanesulfonic anhydride into internal alkynes to access tetrasubstituted trifluoromethylated alkenes was achieved. Since trifluoromethanesulfonic anhydride is a low-cost and abundant chem., this method provides a cost-efficient and practical route to trifluoromethylated compounds

Angewandte Chemie, International Edition published new progress about Alkynes, internal Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Recommanded Product: 2,4-Dichlorothieno[2,3-d]pyrimidine.

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

Gershon, Herman; Parmegiani, Raulo published the artcile< Antifungal activity of ring poly-chlorinated pyrimidines: structure activity relations>, Formula: C4H2Cl2N2, the main research area is DRUG RESISTANCE, MICROBIAL; FUNGICIDES; PYRIMIDINES.

A total of 48 ring chlorinated pyrimidines were screened against strains of 5 fungi by the disk-plate method, liquid culture, and for activity of the vapors of the compounds Correlations of the results obtained by the 3 methods were made, and structure:activity relations were discussed. The outstanding members of this series were found to be 2,4,5-trichloropyrimidine, 4,5,6-trichloropyrimidine, and 2-chloro-methyl-4,5,6-trichloropyrimidine.

Applied Microbiology published new progress about 6554-61-6. 6554-61-6 belongs to class pyrimidines, and the molecular formula is C4H2Cl2N2, Formula: C4H2Cl2N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Mitran, Raul-Augustin; Boscornea, Aurelian Cristian; Stancu, Izabela-Cristina; Tomas, Stefan published the artcile< Some unusual spectral properties of 6-azauracil derivatives>, Formula: C3H2BrN3O2, the main research area is fluorescence spectrometry azauracil derivative.

The optical properties of several new 6-azauracil derivatives have been obtained by means of fluorescence spectroscopy. This method allowed a rapid and accurate characterization, having high specificity and sensitivity.

Scientific Bulletin – University “Politehnica” of Bucharest, Series B: Chemistry and Materials Science published new progress about 4956-05-2. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Formula: C3H2BrN3O2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Mylari, Banavara L.; Miller, Max W.; Howes, Harold L. Jr.; Figdor, Sanford K.; Lynch, John E.; Koch, Richard C. published the artcile< Anticoccidial derivatives of 6-azauracil. 1. Enhancement of activity by benzylation of nitrogen-1. Observations on the design of nucleotide analogs in chemotherapy>, Related Products of 4956-05-2, the main research area is coccidiostat benzylazauracil derivative; azauracil derivative anticoccidial.

Of >100 6-azauracil derivatives prepared and tested against Eimeria tenella infections in Leghorn cockerels, the 1-benzyl derivatives were most active, with maximum activity shown by 1-benzyl derivatives with compact, electron-withdrawing substituents such as 3′- or 4′-fluorine, -chlorine, or -nitrile substituents. The most active compound was 1-(3-cyanobenzyl)-6-azauracil (I) [27414-41-1], with a potency ∼16 times that of 6-azauracil [461-89-2]. I was also effective against E. maxima, E. acervulina, E. brunetti, and E. necatrix. Metabolism experiments using C-14-labeled 1-benzyl-6-azauracil [5991-46-8] showed no cleavage of the side chain. Structure-activity relations are discussed.

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

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wu, Tianxiao; Qin, Qiaohua; Liu, Nian; Zhang, Chu; Lv, Ruicheng; Yin, Wenbo; Sun, Yin; Sun, Yixiang; Wang, Ruifeng; Zhao, Dongmei; Cheng, Maosheng published the artcile< Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold>, SDS of cas: 18740-39-1, the main research area is diaminopyrimidine preparation tropomyosin receptor kinase inhibitor SAR mol docking; Anticancer; NTRK gene fusion; Pharmacophore model; TRK inhibitors.

Tropomyosin receptor kinase (TRK) is an ideal target for treating cancers caused by the NTRK gene fusion. In this study, more than 60 2,4-diaminopyrimidine derivatives were prepared to understand the structure-activity relationship and confirm the rationality of the pharmacophore model reported previously. Among them, compound I was found to be a potent pan-TRK inhibitor that inhibits the proliferation of Km-12 cell lines. Addnl., compound I induced the apoptosis of Km-12 cells in a concentration-dependent manner. Western blot anal. revealed that compound I inhibited the phosphorylation of TRK to block downstream pathways. Compound I also possessed outstanding plasma stability and liver microsomal stability in vitro, with half-lives greater than 289.1 min and 145 min, resp. Pharmacokinetic studies indicated that the oral bioavailability of compound I is 17.4%. These results demonstrate that compound I could serve as a novel lead compound for overcoming NTRK-fusion cancers.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, SDS of cas: 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wang, Zhao; Kang, Dongwei; Feng, Da; Cherukupalli, Srinivasulu; Jiang, Xiangyi; Fu, Zhipeng; De Clercq, Erik; Pannecouque, Christophe; Liu, Xinyong; Zhan, Peng published the artcile< Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility>, Formula: C6H2Cl2N2S, the main research area is morpholine diarylpyrimidine synthesis antiHIV NNRTI HIV1 CYP450; HIV-1; Morpholine; NNRTIs; SARs; Tolerant region I; Tolerant region II.

To address the intractable issues of drug resistance and poor solubility, a novel series of morpholine-substituted diarylpyrimidines targeting the tolerant region I and tolerant region II of NNIBP were rationally designed by utilizing the available crystallog. studies. The biol. evaluation results showed that four most promising compounds (14e1, 14g1, 14g2 and 14j2) displayed excellent potency against WT HIV-1 strain with EC50 values ranging from 58 to 87 nM, being far more potent than NVP and comparable to ETV. Besides, some derivatives exhibited moderate activity in inhibiting the mutant HIV-1 strains. More encouragingly, 14d2 (RF = 0.4) possessed higher antiresistance profile than ETV (RF = 6.3) and K-5a2 (RF = 3.0) toward the double mutant strain F227L + V106A. The HIV-1 RT inhibition assay confirmed their binding target. The mol. docking studies were conducted and discussed in detail to rationalize the preliminary SARs. Further test indicated that morpholine could indeed promote the improvement of water solubility Addnl., the in silico prediction of physicochem. properties and CYP enzymic inhibitory ability were investigated to evaluate their drug-like features.

European Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Formula: C6H2Cl2N2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Rabal, Obdulia; San Jose-Eneriz, Edurne; Agirre, Xabier; Sanchez-Arias, Juan Antonio; de Miguel, Irene; Ordonez, Raquel; Garate, Leire; Miranda, Estibaliz; Saez, Elena; Vilas-Zornoza, Amaia; Pineda-Lucena, Antonio; Estella, Ander; Zhang, Feifei; Wu, Wei; Xu, Musheng; Prosper, Felipe; Oyarzabal, Julen published the artcile< Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with In Vivo Efficacy in Multiple Myeloma>, Category: pyrimidines, the main research area is histone deacetylases DNA methyltransferase G9a inhibitors multiple myeloma antitumor.

Concomitant inhibition of key epigenetic pathways involved in silencing tumor suppressor genes has been recognized as a promising strategy for cancer therapy. Herein, we report a first-in-class series of quinoline-based analogs that simultaneously inhibit histone deacetylases (from a low nanomolar range) and DNA methyltransferase-1 (from a mid-nanomolar range, IC50 < 200 nM). Addnl., lysine methyltransferase G9a inhibitory activity is achieved (from a low nanomolar range) by introduction of a key lysine mimic group at the 7-position of the quinoline ring. The corresponding epigenetic functional cellular responses are observed: histone-3 acetylation, DNA hypomethylation, and decreased histone-3 methylation at lysine-9. These chem. probes, multi-target epigenetic inhibitors, were validated against the multiple myeloma cell line MM1.S, demonstrating promising in vitro activity of 12a (CM-444) with GI50 of 32 nM, an adequate therapeutic window (>1 log unit), and a suitable pharmacokinetic profile. In vivo, 12a achieved significant antitumor efficacy in a xenograft mouse model of human multiple myeloma.

Journal of Medicinal Chemistry published new progress about Acetylation (histone H3). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia