Category: pyrimidines

On January 31, 2012, Zeng, Yan-Bo; Zhu, Shun-Hai; Dong, Hui; Han, Hong-Yu; Jiang, Lian-Lian; Wang, Quan; Cheng, Jun; Zhao, Qi-Ping; Ma, Wei-Jiao; Huang, Bing published an article.COA of Formula: C17H24N4O6 The title of the article was Great efficacy of sulfachloropyrazine-sodium against acute murine toxoplasmosis. And the article contained the following:

Objective: To identify more effective and less toxic drugs to treat animal toxoplasmosis. Methods: Efficacy of seven kinds of sulfonamides against Toxoplasma gondii (T. gondii) in an acute murine model was evaluated. The mice used throughout the study were randomly assigned to many groups (10 mice each), which either remained uninfected or were infected i.p. with tachyzoites of T. gondii (strains RH and CN). All groups were then treated with different sulfonamides and the optimal treatment protocol was determined candidates. Sulfadiazine-sodium (SD) was used for comparison. Results: The optimal therapy involved gavaging mice twice per day with 250 mg/kg bw of sulfachloropyrazine-sodium (SPZ) for five days. Using this protocol, the average survival time and the time-point of 50% fatalities were prolonged significantly compared with SD treatment. Treatment with SPZ protected 40% of mice from death, and the heart and kidney tissue of these animals was parasite-free, as determined by nested-PCR, SPZ showed excellent therapeutic effects in the treatment of T. gondii in an acute murine model and is therefore a promising drug candidate for the treatment and prevention of T. gondii in animals. Conclusions: II can be concluded that the effective drug sulfachloropyrazine may be the new therapeutic options against animal toxoplasmosis. The experimental process involved the reaction of 5-(3,4,5-Trimethoxybenzyl)pyrimidine-2,4-diamine 2-hydroxypropanoate(cas: 23256-42-0).COA of Formula: C17H24N4O6

The Article related to protozoacide sulfachloropyrazine sodium toxoplasma toxoplasmosis heart liver lung kidney, efficacy, murine, sulfachloropyrazine-sodium, sulfonamides, therapeutic effect, therapy, toxoplasma gondii, toxoplasmosis and other aspects.COA of Formula: C17H24N4O6

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kropinski, Andrew M.; Turner, Dann; Nash, John H. E.; Ackermann, Hans-Wolfgang; Lingohr, Erika J.; Warren, Richard A.; Ehrlich, Kenneth C.; Ehrlich, Melanie published an article in 2018, the title of the article was The sequence of two bacteriophages with hypermodified bases reveals novel phage-host interactions.HPLC of Formula: 4433-40-3 And the article contains the following content:

Bacteriophages SP-15 and ΦW-14 are members of the Myoviridae infecting Bacillus subtilis and Delftia (formerly Pseudomonas) acidovorans, resp. What links them is that in both cases, approx. 50% of the thymine residues are replaced by hypermodified bases. The consequence of this is that the physico-chem. properties of the DNA are radically altered (melting temperature (Tm), buoyant d. and susceptibility to restriction endonucleases). Using 454 pyrosequencing technol., we sequenced the genomes of both viruses. Phage ΦW-14 possesses a 157-kb genome (56.3% GC) specifying 236 proteins, while SP-15 is larger at 222 kb (38.6 mol % G + C) and encodes 318 proteins. In both cases, the phages can be considered genomic singletons since they do not possess BLASTn homologs. While no obvious genes were identified as being responsible for the modified base in ΦW-14, SP-15 contains a cluster of genes obviously involved in carbohydrate metabolism The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).HPLC of Formula: 4433-40-3

The Article related to carbohydrate metabolism myoviridae bacillus delftia, 5-hydroxymethyluracil, 5-hydroxypentyluracil, bacillus, dna sequencing, delftia, sp-15, alpha-putrescinylthymine, bacteriophage, hypermodified bases, φw-14 and other aspects.HPLC of Formula: 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 30, 2021, Ishizaki, Tetsuo; Mazaki, Junichi; Enomoto, Masanobu; Shigoka, Masatoshi; Kasahara, Kenta; Matsudo, Takaaki; Kawakita, Hideaki; Nagakawa, Yuichi; Katsumata, Kenji; Tsuchida, Akihiko published an article.Application In Synthesis of 5-Methylpyrimidine-2,4(1H,3H)-dione The title of the article was Prospective multicenter phase II study of biweekly TAS-102 and bevacizumab for metastatic colorectal cancer. And the article contained the following:

This study assessed the efficacy and safety of biweekly trifluridine and tipiracil hydrochloride (TAS-102) with bevacizumab combination therapy for patients with metastatic colorectal cancer (mCRC). We included 19 patients with mCRC who received TAS-102 and bevacizumab combination therapy biweekly as third-line chemotherapy. The primary endpoint was progression-free survival. Patients had a median age of 73 years and most (73.4%) were men. The median progression-free and overall survival were 5.6 and 11.5 mo, resp. Five (26.3%) patients achieved a response and the disease control rate was 12/19 (63.1%). One patient (5.2%) experienced neutropenia grade 3 or more. The median time from baseline performance status 0/1 to worsening to 2 or more was 10.3 mo. Biweekly TAS-102 plus bevacizumab facilitates tumor shrinkage by reducing the incidence of grade 3 or more neutropenia, improving survival, and maintaining performance status. This combination may represent a treatment option for patients with late-stage rnCRC receiving third- or later-line therapy. The experimental process involved the reaction of 5-Methylpyrimidine-2,4(1H,3H)-dione(cas: 65-71-4).Application In Synthesis of 5-Methylpyrimidine-2,4(1H,3H)-dione

The Article related to metastatic colorectal cancer trifluridine tipiracil hydrochloride bevacizumab chemotherapy, clin trial phase 2 adverse svent biweekly, biweekly, tas-102, bevacizumab, metastatic colorectal cancer, neutropenia and other aspects.Application In Synthesis of 5-Methylpyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Dahabiyeh, Lina A.; Mujammami, Muhammad; Arafat, Tawfiq; Benabdelkamel, Hicham; Alfadda, Assim A.; Abdel Rahman, Anas M. published an article in 2021, the title of the article was A metabolic pattern in healthy subjects given a single dose of metformin: a metabolomics approach.Electric Literature of 4433-40-3 And the article contains the following content:

Metformin is a widely prescribed medication for the treatment of type 2 diabetes mellitus (T2DM). It possesses effective roles in various disorders, including cancer, dyslipidemia, and obesity. However, the underlying mechanisms of metformin′s multiple benefits are not fully understood. Herein, a mass spectrometry-based untargeted metabolomics approach was used to investigate the metabolic changes associated with the administration of a single dose of metformin in the plasma of 26 healthy subjects at five-time points; pre-dose, before the maximum concentration of metformin (Cmax), Cmax, after Cmax, and 36 h postdose. A total of 111 metabolites involved in various biochem. processes were perturbed, with branched-chain amino acid (BCAA) being the most significantly altered pathway. Addnl., the Pearson similarity test revealed that 63 metabolites showed a change in their levels dependent on metformin level. Out of these 63, the level of 36 metabolites was significantly altered by metformin. Significantly altered metformin-dependent metabolites, including hydroxymethyl uracil, propionic acid, glycerophospholipids, and eicosanoids, pointed to fundamental biochem. processes such as lipid network signaling, energy homeostasis, DNA lesion repair mechanisms, and gut microbiota functions that could be linked to the multiple beneficial roles of metformin. Thus, the distinctive metabolic pattern linked to metformin administration can be used as a metabolic signature to predict the potential effect and mechanism of actions of new chem. entities during drug development. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Electric Literature of 4433-40-3

The Article related to metabolic pattern healthy human single dose metformin metabolomics, branched-chain amino acids, cancer, eicosanoids, glycerophospholipid, mass spectrometry, metabolomics, metformin, type 2 diabetes mellitus and other aspects.Electric Literature of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 1, 2017, Kang, Soyeong; Jang, Seok Hyeon; Lee, Juyeol; Kim, Dong-gil; Kim, Mijin; Jeong, Wook; Rhee, Young Ho published an article.Application of 4433-40-3 The title of the article was Pd-Catalyzed Regioselective Asymmetric Addition Reaction of Unprotected Pyrimidines to Alkoxyallene. And the article contained the following:

Catalytic asym. synthesis of N-heterocyclic glycosides free of protecting and directing groups is reported. The key reaction is highlighted by the atom-efficient and regioselective addition of unprotected pyrimidines to highly functionalized alkoxyallene. Numerous acyclic and cyclic N-heterocyclic glycosides are accessed with minimal formation of organic byproducts. The synthetic utility of the reaction is demonstrated by the first catalytic asym. synthesis of anticancer pharmaceutical (-)-Tegafur and stereoselective synthesis of an oxepane nucleoside derivative The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Application of 4433-40-3

The Article related to protecting group free heterocyclic glycoside enantioselective synthesis, regioselective addition unprotected pyrimidine alkoxyallene chiral catalysis, tegafur stereoselective synthesis oxepane nucleoside and other aspects.Application of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kawasaki, Fumiko; Beraldi, Dario; Hardisty, Robyn E.; McInroy, Gordon R.; van Delft, Pieter; Balasubramanian, Shankar published an article in 2017, the title of the article was Genome-wide mapping of 5-hydroxymethyluracil in the eukaryote parasite Leishmania.Application of 4433-40-3 And the article contains the following content:

Background: 5-Hydroxymethyluracil (5hmU) is a thymine base modification found in the genomes of a diverse range of organisms. To explore the functional importance of 5hmU, we develop a method for the genome-wide mapping of 5hmU-modified loci based on a chem. tagging strategy for the hydroxymethyl group. Results: We apply the method to generate genome-wide maps of 5hmU in the parasitic protozoan Leishmania sp. In this genus, another thymine modification, 5-(β-glucopyranosyl) hydroxymethyluracil (base J), plays a key role during transcription. To elucidate the relationship between 5hmU and base J, we also map base J loci by introducing a chem. tagging strategy for the glucopyranoside residue. : bserved 5hmU peaks are highly consistent among tech. replicates, confirming the robustness of the method. 5hmU is enriched in strand switch regions, telomeric regions, and intergenic regions. Over 90% of 5hmU-enriched loci overlapped with base J-enriched loci, which occurs mostly within strand switch regions. We also identify loci comprising 5hmU but not base J, which are enriched with motifs consisting of a stretch of thymine bases. Conclusions: By chem. detecting 5hmU we present a method to provide a genome-wide map of this modification, which will help address the emerging interest in the role of 5hmU. This method will also be applicable to other organisms bearing 5hmU. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Application of 4433-40-3

The Article related to genome wide mapping 5hydroxymethyluracil transcription dna sequencing leishmania, 5-formyluracil (5fu), 5-hydroxymethyluracil (5hmu), base j, genome-wide mapping, leishmania donovani, leishmania major and other aspects.Application of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Aleidi, Shereen M.; Dahabiyeh, Lina A.; Gu, Xinyun; Al Dubayee, Mohammed; Alshahrani, Awad; Benabdelkamel, Hicham; Mujammami, Muhammad; Li, Liang; Aljada, Ahmad; Abdel Rahman, Anas M. published an article in 2020, the title of the article was Obesity connected metabolic changes in type 2 diabetic patients treated with metformin.Related Products of 4433-40-3 And the article contains the following content:

Metformin is widely used in the treatment of Type 2 Diabetes Mellitus (T2DM). However, it is known to have beneficial effects in many other conditions, including obesity and cancer. In this study, we aimed to investigate the metabolic effect of metformin in T2DM and its impact on obesity. A mass spectrometry (MS)-based metabolomics approach was used to analyze samples from two cohorts, including healthy lean and obese control, and lean as well as obese T2DM patients on metformin regimen in the last 6 mo. The results show a clear group separation and sample clustering between the study groups due to both T2DM and metformin administration. Seventy-one metabolites were dysregulated in diabetic obese patients (30 up-regulated and 41 down-regulated), and their levels were unchanged with metformin administration. However, 30 metabolites were dysregulated (21 were up-regulated and 9 were down-regulated) and then restored to obese control levels by metformin administration in obese diabetic patients. Furthermore, in obese diabetic patients, the level of 10 metabolites was dysregulated only after metformin administration. Most of these dysregulated metabolites were dipeptides, aliphatic amino acids, nucleic acid derivatives, and urea cycle components. The metabolic pattern of 62 metabolites was persistent, and their levels were affected by neither T2DM nor metformin in obesity. Interestingly, 9 metabolites were significantly dysregulated between lean and obese cohorts due to T2DM and metformin regardless of the obesity status. These include arginine, citrulline, guanidoacetic acid, proline, alanine, taurine, 5-hydroxyindoleacetic acid, and 5-hydroxymethyluracil. Understanding the metabolic alterations taking place upon metformin treatment would shed light on possible mol. targets of metformin, especially in conditions like T2DM and obesity. The experimental process involved the reaction of 5-(Hydroxymethyl)pyrimidine-2,4(1H,3H)-dione(cas: 4433-40-3).Related Products of 4433-40-3

The Article related to metformin diabetes mellitus obesity cancer metabolomics metabolic effect, amino acid, t2dm, body mass index-bmi, mass spectrometry-lc-ms/ms, metabolomics, metformin, obesity, type 2 diabete mellitus and other aspects.Related Products of 4433-40-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On November 4, 2021, Xu, Qing; Alt, Carsten; Li, Zhe; Nilar, Shahul; Rademacher, Peter Michael; Yee, Calvin Wesley published a patent.Category: pyrimidines The title of the patent was Prepartion of pyrimidines as ferroportin inhibitors. And the patent contained the following:

The invention is related to a method of inhibiting iron transport mediated by ferroportin in a subject, comprising administering to the subject an effective amount of a compound I [Z= N, CR5; R5 = H, halo, alkyl; R6 = independently at each occurrence halo, OH, (un)substituted alkoxy, alkyl, etc.; or two R6 groups, taken together with the atom to which each is attached, form an (un)substituted 5- or 6-membered monocyclic heterocyclyl fused with ring B, a C4-C7 cycloalkyl fused with ring B, a Ph fused with ring B, or a 5- to 6-membered monocyclic heteroaryl fused with ring B; n = 0-3; Y = (Y1)0-1; Y1-4 = independently CH, N, NH, O, S, SH, SR6, NR6, CR6; provided that 1 or 2 of Y1-4 can be N, NR6, NH, O, SH or SR6; R1, R2 = independently H, alkyl, haloalkyl, alkoxy, and OH; R1 and R2 taken together with the atom to which each is attached form ring A; wherein A = (un)substituted C5-C6 cycloalkyl, 5- or 6-membered heterocyclyl, Ph, and 5- or 6-membered heteroaryl; R3 = H , optionally deuterated C1-C3 alkyl, hydroxyalkyl, C1-C3 alkoxyalkyl, haloalkyl, cyclopropyl, phenyl; R4 = CH2CONH2 and derivatives, cycloalkyl, alkylsulfonylalkyl, etc.; or R3NR4 = (un)substituted4- to 12-membered heterocyclyl] and their pharmaceutical salts. The invention is laos relates to methods of administering them for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries and to pharmaceutical compositions containing compounds I. Preparation of compounds I and their pharmaceutical acceptable salts is also given. Thus, II was prepared in 6 steps from 2-chloro-4-methylpyridine and diethylcarbonate using N-tert-Butyl-2-[(2-chloro-5H,6H,7H-cyclopenta[d]pyrimidin-4-yl)amino]acetamide (preparation given). II was tested in an in vitro ferroportin internalization assay (pEC50 = 7.7). The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Category: pyrimidines

The Article related to pyrimdine cycloalkapyrimidine thienopyrimidine preparation ferroportin inhibitor, thienopyrimidine cyclopentapyrimidinyl amino acid amide preparation ferroportin inhibitor, hepcidin iron metabolism disorder cycloalkapyrimidine thienopyrimidine preparation, iron overload state thalassemia hemochromatosis treatment cycloalkapyridine thienopyrimidine preparation and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On June 28, 2012, Bohno, Ayako; Matsuda, Daisuke; Otake, Norikazu; Kakinuma, Hiroyuki; Kobashi, Yohei; Kawamura, Madoka; Shiozawa, Fumiyasu; Kawabe, Kenichi; Iwata, Yuki; Hamada, Makoto published a patent.Name: 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of 4-piperidinyl-condensed heterocyclic compounds as GPR119 agonists. And the patent contained the following:

The title compounds represented by general formula [I; group A = each (un)substituted Ph or 5 or 6-membered heteroaryl; W = a single bond, O, NH, OCH2, or CH2O; X = a nitrogen atom or CR21; Y1 = a nitrogen atom or CR22; Y2 = a nitrogen atom or CR23; Y3 = a nitrogen atom or CR24; R21, R22, R23, R24 = a hydrogen atom or C1-6 alkyl; group B = C2-6 alkyl, C3-8 cycloalkyl, (C3-8 cycloalkyl)C1-6 alkyl, (aryl)C1-6 alkyl, (saturated heterocyclyl)C1-6 alkyl, CO2R31 (R31 = C1-6 alkyl, C3-8 cycloalkyl, aryl or saturated heterocyclyl), or 5 or 6-membered heteroaryl] or pharmaceutically permitted salts thereof are prepared These compounds including indazolylpiperidine, benzotriazolylpiperidine, pyrazolopyridinylpiperidine, and triazolopyridinylpiperidine compounds have an outstanding glucose-dependent insulinotropic polypeptide receptors (GPR119) agonist action. They are useful as blood-sugar lowering agents for the prevention and/or treatment of diabetes. Thus, a solution of 150 mg tert-Bu 4-[5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indazol-1-yl]piperidine-1-carboxylate in 1.5 mL DMF was treated with 155 mg 4-(1H-Tetrazol-1-yl)phenyl trifluoromethanesulfonate, [1,1′-bis(diphenylphosphino)ferrocene]palladium(II) chloride and 525 μL 2 M aqueous Na2CO3 solution, stirred at 100° for 1.5 h, and concentrated under reduced pressure to give, after silica gel chromatog., 100 mg tert-Bu 4-(5-[4-(1H-tetrazol-1-yl)phenyl]-1H-indazol-1-yl)piperidine-1-carboxylate (II). II and 4-[3-[1-(5-Chloropyrimidin-2-yl)piperidin-4-yl]-3H-[1,2,3]triazolo[4,5-c]pyridin-6-yl]-N-ethyl-2,3-difluorobenzamide(III) in vitro promoted the cellular production of cAMP with ED50 of 13 and 2 nM, resp., in cells expressing human GPR119. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Name: 2-Chloro-5-isopropylpyrimidine

The Article related to diabetes prevention treatment piperidinyl condensed heterocyclic compound preparation, piperidinyl condensed heterocyclic compound preparation gpr119 agonist, indazolylpiperidine benzotriazolylpiperidine preparation gpr119 agonist, pyrazolopyridinylpiperidine triazolopyridinylpiperidine preparation gpr119 agonist and other aspects.Name: 2-Chloro-5-isopropylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On October 20, 2011, Barba, Oscar; Gattrell, William; Smyth, Donald; Swain, Simon published a patent.Recommanded Product: 596114-50-0 The title of the patent was Preparation of 3-substituted 5-(pyrrolidine-1-carbonyl)pyrrolidine and its derivatives for use in the treatment of metabolic disorders. And the patent contained the following:

The title compounds I [p, q = 1-2; Z = NC(O)OR4, NC(O)NR4R5, N-heteroaryl, etc.; Y = CH2, CF2, CHF, O, NR1, C(O) or B (wherein B = 5-membered heteroaryl containing one or more heteroatoms selected from N, O and S); when Y = CH2, CF2, CHF, O, NR1 or C(O), X = (un)branched alkylene; or when Y = O or NR1, X may also be -ACHR2- (wherein A = 5-membered heteroaryl containing one or more heteroatoms selected from N, O and S); and when Y = B, X = OCHR3; Ar = (un)substituted para-substituted 6-membered heteroaryl containing one or two N atoms; R1-R3 = H, alkyl; R4 = aryl, heteroaryl, alkyl,(un)substituted cycloalkyl; R5 = H or alkyl; V = II (T = CH2, or, when m = 1, T may also be S; when T = CH2, R6 = F or CN, and when T = S, R6 = CN; R7 = H, alkyl; m = 0-1; s = 0-2); n = 0-1] which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes, were prepared For example, Pd-catalyzed coupling 2-bromo-5-{3-[1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}pyridine with tert-Bu (2S,4S)-4-amino-2-(pyrrolidine-1-carbonyl)pyrrolidine-1-carboxylate (preparations given) followed by Boc-deprotection afforded (2S,4S)-III. Compounds I produced a concentration-dependent increase in intracellular cAMP level and generally had an EC50 of <10 μM when tested in GPR119 cAMP assay. All exemplified compounds I showed activity in DPP-IV assay having an IC50 of <20 μM. Pharmaceutical composition comprising compound I is disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Recommanded Product: 596114-50-0

The Article related to pyrrolidinecarbonylpyrrolidine preparation glucose dependent insulinotropic polypeptide receptor gpr119 agonist, metabolic disorder type ii diabetes treatment pyrrolidinecarbonylpyrrolidine preparation, antidiabetic pyrrolidinecarbonylpyrrolidine preparation gpr119 agonist dipeptidyl peptidase dppiv modulator and other aspects.Recommanded Product: 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia