Pyrimidines

Deng, Jifeng; Peng, Li; Zhang, Guicheng; Lan, Xiaobing; Li, Chufang; Chen, Fuxin; Zhou, Yayao; Lin, Zuoxian; Chen, Ling; Dai, Renke; Xu, Hongjiang; Yang, Ling; Zhang, Xiquan; Hu, Wenhui published the artcile< The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes>, Category: pyrimidines, the main research area is thienopyrimidine preparation DDP IV inhibitor treatment diabetes; aminothiophenecarboxylate cyclization chlorination oxygenation alkylation substitution.

Some dipeptidyl peptidase IV inhibitors, e.g., I, were designed based on alogliptin using a scaffold-hopping strategy. All of the compounds constructed on a thienopyrimidine scaffold demonstrated good inhibition and selectivity for DPP-IV. Compound I exhibited subnanomolar (IC50 = 0.33 nM) DPP-IV inhibitory activity, good in vivo efficacy and an acceptable pharmacokinetic profile. A pharmacokinetic-driven optimization of I may lead to a class of clin. candidate DPP-IV inhibitors.

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

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Khmel’nitskii, R. A.; Klyuev, N. A.; Kunina, E. A.; Kropacheva, A. A. published the artcile< Mass spectra of methoxy derivatives of 4-aminopyrimidines>, Recommanded Product: 6-Chloro-2-methoxypyrimidin-4-amine, the main research area is mass spectra pyrimidinamine.

Mass spectra of the 2-methoxy-6-methyl, 6-methoxy-2-methyl, 2-methoxy-5-methyl, 2,6-dimethoxy, and 6-chloro-2-methoxy derivatives of 4-pyrimidinamine were determined and correlated with structure.

Khimiya Geterotsiklicheskikh Soedinenii published new progress about Mass spectra. 3286-55-3 belongs to class pyrimidines, and the molecular formula is C5H6ClN3O, Recommanded Product: 6-Chloro-2-methoxypyrimidin-4-amine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Okui, Kiyoshi published the artcile< Chemistry of sulfanilamidopyrimidine. Abnormal condensation products of 4-amino-6-chloro-2-methoxypyrimidine with p-nitro-benzenesulfonyl chloride>, Reference of 3286-55-3, the main research area is pyrimidine nitrobenzenesulfonyl chloride reaction; nitrobenzenesulfonamidopyrimidine; pyrimidinium betaine nitrobenzenesulfonamidopyrimidine.

Reaction of 4-amino-6-chloro-2-methoxypyrimidine with 4-ClSO2C6H4NO2 in the presence of pyridine gave the pyridinium betaines I and II in addition to the sulfonamide III. The yield of I increased with reaction time, accompanied by a corresponding decrease in III yield. I was also prepared by heating III with pyridine. The structure of II was also confirmed.

Heterocycles published new progress about 3286-55-3. 3286-55-3 belongs to class pyrimidines, and the molecular formula is C5H6ClN3O, Reference of 3286-55-3.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Jung, Seung-Youn; Nam, Ky-Youb; Park, Jeong-In; Song, Kyung-Hee; Ahn, Jiyeon; Park, Jong Kuk; Um, Hong-Duck; Hwang, Sang-Gu; Choi, Sang Un; Song, Jie-Young published the artcile< Radiosensitizing effect of novel phenylpyrimidine derivatives on human lung cancer cells via cell cycle perturbation>, Product Details of C4H2Br2N2, the main research area is lung cancer cell phenylpyrimidine derivative radiosensitizing.

Radiotherapy is one of the most common treatments for cancer, but radioresistance and injury to normal tissue are considered major obstacles to successful radiotherapy. Thus, there is an urgent need to develop radiosensitizers to improve the therapeutic outcomes of radiotherapy in cancer patients. Our previous efforts to identify novel radiosensitizers, using high-throughput screening targeting p53 and Nrf2 revealed a promising N-phenylpyrimidin-2-amine (PPA) lead compound; 17 derivatives of this lead compound were examined in the present study. PPA5, 13, 14, 15, and 17 inhibited cell viability by more than 50% with a marked increase in the proportion of cells arrested at the G2/M phase of cell cycle. Among these compounds, PPA15 markedly increased the sub-G1 cell population and increased the levels of cyclin B1 and phosphorylation levels of cyclin-dependent kinases 1 (CDK1). Combined treatment with radiation and PPA14 or PPA15 significantly decreased clonogenic survival. An in vitro kinase assay revealed that PPA15 inhibited multiple CDKs involved in cell cycle regulation. Compared with drug or radiation treatment alone, combined treatment with PPA15 and radiation resulted in the suppression of A549 tumor growth in mice by 59.5% and 52.7%, resp. Treatment with PPA15 alone directly inhibited tumor growth by 25.7%. These findings suggest that the novel pan CDK inhibitor, PPA15, may be a promising treatment to improve the effectiveness of radiotherapy for the treatment of cancer.

Journal of Pharmacology and Experimental Therapeutics published new progress about Apoptosis. 3921-01-5 belongs to class pyrimidines, and the molecular formula is C4H2Br2N2, Product Details of C4H2Br2N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Fang, Yuanying; Zhang, Shaokun; Li, Min; Xiong, Lijuan; Tu, Liangxing; Xie, Saisai; Jin, Yi; Liu, Yanhua; Yang, Zunhua; Liu, Ronghua published the artcile< Optimisation of novel 4, 8-disubstituted dihydropyrimido[5,4-b][1,4]oxazine derivatives as potent GPR 119 agonists>, Application of C5H4Cl2N2O, the main research area is dihydropyrimido oxazine derivative preparation GPR 119 agonist diabetes; GPR 119 agonists; Optimisation; pyrimidodihydrooxazine; type 2 diabetes mellitus.

GPR119 is a promising target for discovery of anti-type 2 diabetes mellitus agents. We described the optimization of a novel series of pyrimido[5,4-b][1,4]oxazine derivatives as GPR119 agonists. Most designed compounds exhibited good agonistic activities. Among them, compound and demonstrated the potent EC50 values (13 and 12 nM, resp.) and strong inherent activities. Moreover, significant hypoglycemic effect of compound was observed by reducing the blood glucose AUC0-2h at the dose of 30 mg/kg, which is stronger than Vildagliptin (23.4% reduction vs. 17.9% reduction).

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antidiabetic agents. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, Application of C5H4Cl2N2O.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Choi, Chulho; Nuhant, Philippe; Mousseau, James J.; Yang, Xiaojing; Gerstenberger, Brian S.; Williams, Jessica M.; Wright, Stephen W. published the artcile< Synthesis of Chiral Azabicycles from Pyroglutaminols>, Formula: C7H7ClN2O2, the main research area is chiral azabicycle morpholine piperazine derivative preparation; stereocontrolled intramol SN2 cyclization pyroglutaminol.

The stereocontrolled synthesis of a range of substituted bicyclic morpholine and piperazine derivatives is reported from substituted pyroglutaminols via an intramol. SN2 cyclization as the key step. This enantiospecific approach toward chiral bicyclic morpholines and piperazines offers new opportunities to access these challenging ring systems, which are becoming increasingly common motifs in drug discovery.

Organic Letters published new progress about Cyclization, stereoselective. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Formula: C7H7ClN2O2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Zhang, Xuqing; Zhu, Bin; Sun, Weimei; Wang, Mina; Albarazanji, Kamal; Ghosh, Brahma; Cummings, Maxwell; Lenhard, James; Leonard, James; Macielag, Mark; Lanter, James published the artcile< Discovery of a novel series of guanidinebenzoates as gut-restricted enteropeptidase and trypsin dual inhibitors for the treatment of metabolic syndrome>, Recommanded Product: Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is guanidinebenzoates gutrestricted enteropeptidase trypsin dual inhibitor treatment metabolic syndrome; Enteropeptidase inhibitor; Guanidinebenzoate; Gut-restriction; Trypsin inhibitor.

Novel series of guanidinebenzoate enteropeptidase and trypsin dual inhibitors has been discovered and SAR studies were conducted. Optimization was focused on improving properties for gut restriction, including increased aqueous solubility, lower cellular permeability, and reduced oral bioavailability. Lead compounds were identified with efficacy in a mouse fecal protein excretion study.

Bioorganic & Medicinal Chemistry Letters published new progress about Biological permeation. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Recommanded Product: Ethyl 2-chloropyrimidine-5-carboxylate.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

McGee, Danny P. C.; Martin, John C.; Verheyden, Julien P. H. published the artcile< Synthesis of the 7-deaza and 5-aza-7-deaza purine analogs of the antiherpes agent 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine (DHPG)>, Recommanded Product: 4-Methoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amine, the main research area is pyrrolopyrimidinone acyclic nucleoside analog; imidazotriazinone acyclic nucleoside analog; acyclic nucleoside pyrrolopyrimidinone imidazotriazinone; virucide acyclic nucleoside; DHPG analog; hydroxypyropoxymethylpyrrolopyrimidinone amino; hydroxypropoxymethylimidazotriazinone amino.

DHPG analogs I and II were prepared Reaction of 2-amino-4-methoxypyrrolo[2,3-d]pyrimidine with 1,3-dibenzyloxy-2-(chloromethyl)glycerol under phase-transfer conditions gave a product which on sequential treatment with p-MeC6H4SK (to cleave the Me ether) and BBr3 (for debenzylation) gave I. Reaction of 2-acetamidoimidazo[1,2-a]-s-triazin-4-one with 1,3-dibenzyloxy-2-(acetoxymetyl)glycerol gave a product, which on debenzylation (by catalytic transfer hydrogenation) and then deacetylation gave II. I and II were inactive against herpes simplex virus types I and II in cell culture.

Journal of Heterocyclic Chemistry published new progress about Antiviral agents. 84955-32-8 belongs to class pyrimidines, and the molecular formula is C7H8N4O, Recommanded Product: 4-Methoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sagong, Hye Yeon; Bauman, Joseph D.; Patel, Disha; Das, Kalyan; Arnold, Eddy; LaVoie, Edmond J. published the artcile< Phenyl Substituted 4-Hydroxypyridazin-3(2H)-ones and 5-Hydroxypyrimidin-4(3H)-ones: Inhibitors of Influenza A Endonuclease>, Application of C5H4Cl2N2O, the main research area is aryl hydroxypyridazinone preparation influenza A endonuclease inhibitor antiviral; hydroxypyrimidinone aryl preparation influenza A endonuclease inhibitor antiviral.

Seasonal and pandemic influenza outbreaks remain a major human health problem. Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is attractive for the development of new agents for the treatment of influenza infection. Authors’ earlier studies identified a series of 5- and 6-Ph substituted 3-hydroxypyridin-2(1H)-ones that were effective inhibitors of influenza endonuclease. These agents identified as bimetal chelating ligands binding to the active site of the enzyme. In the present study, several aza analogs of these Ph substituted 3-hydroxypyridin-2(1H)-one compounds were synthesized and evaluated for their ability to inhibit the endonuclease activity. In contrast to the 4-aza analog of 6-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one, the 5-aza analog (5-hydroxy-2-(4-fluorophenyl)pyrimidin-4(3H)-one) did exhibit significant activity as an endonuclease inhibitor. The 6-aza analog of 5-(4-fluorophenyl)-3-hydroxypyridin-2(1H)-one (6-(4-fluorophenyl)-4-hydroxypyridazin-3(2H)-one) also retained modest activity as an inhibitor. Several varied 6-phenyl-4-hydroxypyridazin-3(2H)-ones and 2-phenyl-5-hydroxypyrimidin-4(3H)-ones, e.g., I (X-rays crystal structure in complex with endonuclease shown), were synthesized and evaluated as endonuclease inhibitors. The SAR observed for these aza analogs are consistent with those previously observed with various Ph substituted 3-hydroxypyridin-2(1H)-ones.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 5018-38-2 belongs to class pyrimidines, and the molecular formula is C5H4Cl2N2O, Application of C5H4Cl2N2O.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

John, Joyamma published the artcile< Evaluate the hypoglycemic effect of vinca rosea leaf extracts in alloxan induced diabetic rats>, HPLC of Formula: 2244-11-3, the main research area is allaxon induced diabetic Vinca rosea leaf extract hypoglycemic effect.

The present study was carried out to evaluate the antidiabetic activity of aqueous leaf extract of Vinca rosea. The aqueous extract at high dose (300mg/100g) body weight showed a significant hypoglycemic activity. Improvement in the body weight and water and food consumption is also observed after the treatment with herbal extract

International Journal of Science and Nature published new progress about Antidiabetic agents. 2244-11-3 belongs to class pyrimidines, and the molecular formula is C4H4N2O5, HPLC of Formula: 2244-11-3.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia