Day: October 14, 2022

Farkas, Jiri published the artcile< Synthesis of 1,2,4-triazine-3,5(2H,4H)-diones containing electronegative substituents in position 6>, Application of C3H2BrN3O2, the main research area is triazinedione electroneg substituent.

Reaction of F2 with 1,2,4-triazine-3,5(2H,4H)-dione (I, R = H) afforded the fluoro derivative I (R = F) in 0.3% yield. The nitro compound I (R = NO2) was prepared by oxidation of the amino derivative of I (R = NH2) with H2O2, in 23% yield. Synthesis of the cyano compound I (R = cyano) was accomplished by treatment with CuCN. The effect of substituents on the CO frequencies of 6-substituted derivatives of I was studied.

Collection of Czechoslovak Chemical Communications published new progress about 4956-05-2. 4956-05-2 belongs to class pyrimidines, and the molecular formula is C3H2BrN3O2, Application of C3H2BrN3O2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Regan, Collin F.; Pierre, Fabrice; Schwaebe, Michael K.; Haddach, Mustapha; Jung, Michael E.; Ryckman, David M. published the artcile< A facile synthesis of 5-halopyrimidine-4-carboxylic acid esters via a Minisci reaction>, Synthetic Route of 6554-61-6, the main research area is Minisci homolytic alkoxycarbonylation halopyrimidine; bromopyrimidinecarboxylate; pyrimidine halo Minisci homolytic alkoxycarbonylation.

This paper reports the synthesis of various 5-halopyrimidine-4-carboxylic acid esters via the Minisci homolytic alkoxycarbonylation of 5-halopyrimidines. The reaction was found to be highly regioselective, allowing the one-step synthesis of useful amounts (>10 g) of Et 5-bromopyrimidine-4-carboxylate where other methods proved difficult. Et 5-bromopyrimidine-4-carboxylate was used for the preparation of potent CK2 inhibitors including CX-5011. This work represents an interesting application of radical chem. for the preparation of pharmacol. active mols.

Synlett published new progress about Alkoxycarbonylation (Minisci homolytic). 6554-61-6 belongs to class pyrimidines, and the molecular formula is C4H2Cl2N2, Synthetic Route of 6554-61-6.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Xu, Ana; He, Feng; Zhang, Xiangna; Li, Xiaoyang; Ran, Yingying; Wei, Chao; James Chou, C.; Zhang, Rui; Wu, Jingde published the artcile< Tacrine-hydroxamate derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease: Design, synthesis, and biological evaluation>, Recommanded Product: Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is tacrine hydroxamate derivative preparation anti Alzheimer; structure activity tacrine hydroxamate cholinesterase inhibitor; Alzheimer’s disease; Antioxidant; Cholinesterase inhibitor; Metal chelator; Multitarget-directed ligands.

In order to develop multitarget-directed ligands as potential treatments for Alzheimer’s disease, twenty-eight new tacrine-hydroxamate derivatives were designed, synthesized, and biol. evaluated. As expected, most of the compounds exhibited inhibitory activities against cholinesterases (ChEs) and histone deacetylase (HDACs). Among the tested compounds, I showed not only potent and selective inhibition on AChE at sub-nanomolar potency (AChEIC50 = 0.12 nM, BChEIC50 = 361.52 nM) but also potent inhibition on HDAC (IC50 = 0.23 nM). Moreover, I exhibited inhibitory activity on Aβ1-42 self-aggregation as well as disaggregation activity on pre-formed Aβ fibrils. Furthermore, I exhibited antioxidant activity and metal chelating properties. Further mechanistic studies demonstrated that I is a pan-inhibitor of HDACs and a mixed-type inhibitor for AChE. It was shown that I is a BBB penetrant by online prediction. Taken together, the results indicate that I can serve as a lead compound to develop promising candidate analogs as AD therapeutics.

Bioorganic Chemistry published new progress about Alzheimer disease. 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

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