Month: February 2023

Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation was written by Woodring, Jennifer L.;Bachovchin, Kelly A.;Brady, Kimberly G.;Gallerstein, Mitchell F.;Erath, Jessey;Tanghe, Scott;Leed, Susan E.;Rodriguez, Ana;Mensa-Wilmot, Kojo;Sciotti, Richard J.;Pollastri, Michael P.. And the article was included in European Journal of Medicinal Chemistry in 2017.Formula: C8H10ClN3O This article mentions the following:

Human African trypanosomiasis (HAT) is a deadly disease in need of new chemotherapeutics that can cross into the central nervous system. The authors previously reported the discovery of (NEU-617), a small mol. with activity against T. brucei bloodstream proliferation. Further optimization of NEU-617 to improve the physicochem. properties (LogP, LLE, [1], and MPO score) [2] have led us to twelve sub-micromolar compounds, most importantly the headgroup variants I and II, and the linker variant III. Although these 3 compounds had reduced potency compared to NEU-617, they all had improved LogP, LLE and MPO scores. Cross-screening these analogs against other protozoan parasites uncovered IV with potent activity towards T. brucei, T. cruzi and L. major, while four others compounds showed activity towards P. falciparum D6. This reinforces the effectiveness of lead repurposing for the discovery of new protozoan disease therapeutics. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Formula: C8H10ClN3O).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Formula: C8H10ClN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Novel procedure for selective C-nitrosation of aminopyrimidine derivatives under neutral conditions. Scope and synthetic applications was written by Marchal, Antonio;Melguizo, Manuel;Nogueras, Manuel;Sanchez, Adolfo;Low, John N.. And the article was included in Synlett in 2002.Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one This article mentions the following:

A novel simple method, based on treatment with isoamyl nitrite (IAN) in DMSO without any added acid, to produce selective C(5)-nitrosation of aminopyrimidine derivatives is described. It proved to be suitable for a multigram scale and applicable to a larger range of pyrimidine derivatives, including aminodialkoxypyrimidines, than the procedures previously known. Its scope is analyzed and some examples on the usefulness of the newly prepared substances as intermediates in the synthesis of fused heterobicyclic derivatives of potential biol. interest are presented. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Metronidazole-triazole conjugates: Activity against Clostridium difficile and parasites was written by Jarrad, Angie M.;Karoli, Tomislav;Debnath, Anjan;Tay, Chin Yen;Huang, Johnny X.;Kaeslin, Geraldine;Elliott, Alysha G.;Miyamoto, Yukiko;Ramu, Soumya;Kavanagh, Angela M.;Zuegg, Johannes;Eckmann, Lars;Blaskovich, Mark A. T.;Cooper, Matthew A.. And the article was included in European Journal of Medicinal Chemistry in 2015.COA of Formula: C6H4N2 This article mentions the following:

Metronidazole has been used clin. for over 50 years as an antiparasitic and broad-spectrum antibacterial agent effective against anaerobic bacteria. However resistance to metronidazole in parasites and bacteria has been reported, and improved second-generation metronidazole analogs are needed. The copper-catalyzed Huigsen azide-alkyne 1,3-dipolar cycloaddition offers a way to efficiently assemble new libraries of metronidazole analogs. Several new metronidazole-triazole conjugates (Mtz-triazoles) have been identified with excellent broad spectrum antimicrobial and antiparasitic activity targeting Clostridium difficile, Entamoeba histolytica, and Giardia lamblia. Cross resistance to metronidazole was observed against stable metronidazole resistant C. difficile and G. lamblia strains. However for the most potent Mtz-triazoles, the activity remained in a therapeutically relevant window. In the experiment, the researchers used many compounds, for example, 2-Ethynylpyrimidine (cas: 37972-24-0COA of Formula: C6H4N2).

2-Ethynylpyrimidine (cas: 37972-24-0) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.COA of Formula: C6H4N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hyperactive magnetically separable nano-sized MgFe₂O₄ catalyst for the synthesis of several five- and six-membered heterocycles was written by Bansal, Shobha;Kumar, Yogendra;Das, Dipak Kumar;Singh, Prabal Pratap. And the article was included in Chemistry & Chemical Technology in 2019.Recommanded Product: 40230-24-8 This article mentions the following:

MgFe₂O₄ nanoparticle ferrites were synthesized by combustion technique using pure ferric nitrate and magnesium nitratecarbonate. The magnetically separable MgFe₂O₄ MNP’s were found to be hyper active catalyst for the synthesis of a wide range of biol. active five and six-membered heterocyclic moieties at refluxing conditions. Reaction times were lowest in comparison to all reported in literature with excellent yields. Strong electron pull of Fe³⁺ was responsible for its hyper activity, which was substantiated by substitution of Fe³⁺ by other trivalent metal ions. Mg²⁺ contain a unique role because replacement of Mg²⁺ has poor catalytic activity. The developed protocol was efficiently utilized for the synthesis of a series of substituted mono/bis pyrimidines, pyrimidin-2-ol, pyrimidin-2-thiol, pyrazoles and isoxazoles by condensing monochalcones/1,4-bischalcones with various bis-nucleophiles in the presence of catalytic amount of heterogenous magnetic MgFe₂O₄ nanoparticles. The structure of these synthesized compounds was determined by FTIR, ¹H, ¹³C and mass spectra. The catalyst was removed easily from reaction mixture by using a simple external magnet. Nanoparticles of ferrite were recovered and reused with no appreciable change in the activity even after the five runs. Nanoparticles were characterized by XRD, TEM and IR spectroscopy. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Recommanded Product: 40230-24-8).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. A Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones enables an efficient and facile synthesis of structurally important pyrimidines via a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization.Recommanded Product: 40230-24-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sedimentary spectrum and potential ecological risks of residual pharmaceuticals in relation to sediment-water partitioning and land uses in a watershed was written by Hong, Bing;Yu, Shen;Zhou, Min;Li, Juan;Li, Qi;Ding, Jing;Lin, Qiaoying;Lin, Xiaodan;Liu, Xun;Chen, Peiji;Zhang, Linlin. And the article was included in Science of the Total Environment in 2022.Name: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide This article mentions the following:

Pharmaceutical residues in river surficial sediment are prone to anthropogenic impacts and environmental factors in watershed, but the mechanisms remain unclear. This study attempted to reveal surficial sediment-water pseudo-partitioning and anthropogenic (land use) patterns of pharmaceutical residues in surficial sediment among 23 subwatersheds of Jiulong River, southeast China with a gradient of urban land use percentile in dry and wet seasons. Thirty-eight out of target 86 compounds from six-category pharmaceuticals were quantified and ranged from below the quantification limits (0.001 mg kg^-1 dry mass) up to 8.19 mg kg^-1 dry mass (chlortetracycline) using a developed SPE-HPLC-MS/MS protocol. Antibiotics and non-steroidal anti-inflammatory drugs (NSAIDs) collectively dominated sedimentary pharmaceutical residues for 34.5-99.8% of the total quantified compounds (median at 92%). Land uses in subwatersheds showed high consistency with sedimentary pharmaceutical residues in the dry season rather than the wet season, especially for human use only and veterinary use only compounds Surficial sediment-water partitioning of pharmaceutical compounds influenced their sedimentary residues regardless of season, which were determined by properties of compound and surficial sediment interactively. All tetracycline compounds, trimethoprim (sulfonamides synergist), caffeine (central nervous system drug), and oxfendazole (antiparasitic drug) were quantified to pose high potential ecol. risks to aquatics. Findings of this study suggest that pseudo-persistent legacy of human and veterinary pharmaceuticals requires a wider coverage of pharmaceutical compounds for a comprehensive ecol. assessment in the environment and more involvement of anthropogenic impacts and socioeconomic factors in the future studies. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Name: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Name: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Macroscopic Zn-doped α-Fe₂O₃/graphene aerogel mediated persulfate activation for heterogeneous catalytic degradation of sulfamonomethoxine wastewater was written by Dong, Shuying;Yan, Xuanxuan;Li, Wenli;Liu, Yafei;Han, Xiaoxu;Liu, Xiaodan;Feng, Jinglan;Yu, Chongfei;Zhang, Chunyan;Sun, Jianhui. And the article was included in Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) in 2022.Recommanded Product: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide This article mentions the following:

In order to obtain a robust, durable and efficient heterogeneous catalyst, macroscopic monolithic Zn-doped α-Fe₂O₃/graphene aerogel (GA) hybrid architecture with integrated morphol. and hierarchically porous structure were controllably synthesized via a facile in-situ hydrothermal method and then used as persulfate (PS) activator for sulfamonomethoxine (SMM) wastewater purification Several key reaction parameters including the initial SMM concentration, reaction temperature, coexisting inorganic anions and SMM in real natural water samples had different influence on the SMM removal efficiency. The catalytic efficiency of Zn-doped α-Fe₂O₃/GA with the molar ratio of Fe/Zn = 2:1.5 was about 66%, 62%, 66% and 11%∼33% higher than that of GA, α-Fe₂O₃/GA, Zn/GA and other Fe/Zn molar ratio. The improved activity of Fe/Zn = 2:1.5 benefits from the synergistic effects of the sp² hybridized carbon and porous framework, as well as the surface oxygenic functional groups, which accelerate the pollutant/oxidant dispersion and electron transfer. ESR results indicate that ·OH, ¹O₂ and SO·^–₄ radicals account for the catalytic degradation of SMM and the activation of PS in present system is different from conventional homogeneous systems, and speculate mechanism was proposed based on the obtained data. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Recommanded Product: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Recommanded Product: 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Behavior of some 2-(ω-bromoalkylthio)-4,6-dimethylpyrimidines during heating was written by Mikhailov, A. S.;Pashkurov, N. G.;Reznik, V. S.. And the article was included in Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya in 1981.Application of 16879-39-3 This article mentions the following:

The thermal behavior of I (n = 4, 5, 6) on heating in vacuo to 150-240° depended on the value of n; cyclization played a significant role in the reaction patterns only when n = 4. Products found included, e.g., II and thiophane, as well as more complex compounds In the experiment, the researchers used many compounds, for example, 2-Bromo-4,6-dimethylpyrimidine (cas: 16879-39-3Application of 16879-39-3).

2-Bromo-4,6-dimethylpyrimidine (cas: 16879-39-3) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Application of 16879-39-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis of pyrimidine derivatives by the reaction of pyrylium salts with guanidine and compounds of its series was written by Zvezdina, E. A.;Zhdanova, M. P.;Dorofeenko, G. N.. And the article was included in Khimiya Geterotsiklicheskikh Soedinenii in 1980.Application In Synthesis of 4,6-Diphenylpyrimidin-2-amine This article mentions the following:

Treatment of pyrylium salts I (R = Ph, p-MeOC₆H₄, p-O₂NC₆H₄; R¹ = Ph) with H₂NC(:NH)NH₂.HBr gave 35-63% pyrimidinylpyridinium salts II. Pyrimidinum salts III (R = Ph, p-MeOC₆H₄) were obtained in 43 and 69% yield, resp. by reaction of I with methylguanidine nitrate. I and sulfanylguanidine gave pyridinium salts IV (R = R¹ = Ph, Me). 1,2,4,6-Tetraphenylpyridinium perchlorate was obtained in 25% yield by reaction of I with PhNHC(:NPh)NH₂. In the experiment, the researchers used many compounds, for example, 4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8Application In Synthesis of 4,6-Diphenylpyrimidin-2-amine).

4,6-Diphenylpyrimidin-2-amine (cas: 40230-24-8) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Application In Synthesis of 4,6-Diphenylpyrimidin-2-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

4-aminopyrimidine-5-carbaldehydes as intermediates in a Friedlander-type synthesis of 7-arylpyrido[2,3-d]pyrimidines was written by Quiroga, Jairo;Trilleras, Jorge;Abonia, Rodrigo;Insuasty, Braulio;Nogueras, Manuel;Cobo, Justo;de la Torre, Jose M.. And the article was included in ARKIVOC (Gainesville, FL, United States) in 2009.HPLC of Formula: 54030-56-7 This article mentions the following:

A study of formylation of 6-aminopyrimidines leads to the conclusion that the formylation at C5 occurs only when there is no contribution of heteroaromaticity in the pyrimidine ring and that the corresponding pyrimidoformamides are formed in heteroaromatic pyrimidines. Once 4-aminopyrimidin-4(3H)-one-5-carboxaldehydes were prepared, a series of 7-arylpyrido[2,3-d]pyrimidines derivatives were synthesized by a Friedlander type reaction with acetophenones under solvent-free conditions and in the presence of BF₃·Et₂O. The yields of 7-arylpyrido[2,3-d]pyrimidines range from moderate to good and the reaction times were quite short. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7HPLC of Formula: 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.HPLC of Formula: 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Nonpeptide α_vβ₃ Antagonists. Part 11: Discovery and Preclinical Evaluation of Potent α_vβ₃ Antagonists for the Prevention and Treatment of Osteoporosis was written by Coleman, Paul J.;Brashear, Karen M.;Askew, Ben C.;Hutchinson, John H.;McVean, Carol A.;Duong, Le T.;Feuston, Bradley P.;Fernandez-Metzler, Carmen;Gentile, Michael A.;Hartman, George D.;Kimmel, Donald B.;Leu, Chih-Tai;Lipfert, Lorraine;Merkle, Kara;Pennypacker, Brenda;Prueksaritanont, Thomayant;Rodan, Gideon A.;Wesolowski, Gregg A.;Rodan, Sevgi B.;Duggan, Mark E.. And the article was included in Journal of Medicinal Chemistry in 2004.Related Products of 90905-32-1 This article mentions the following:

3-(S)-Pyrimidin-5-yl-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5e) and 3-(S)-(methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5f) were identified as potent and selective antagonists of the α_vβ₃ receptor. These compounds have excellent in vitro profiles (IC₅₀ = 0.07 and 0.08 nM, resp.), significant unbound fractions in human plasma (6 and 4%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in an in vivo model of bone turnover following once-daily oral administration, these two compounds were selected for clin. development for the treatment of osteoporosis. In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1Related Products of 90905-32-1).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Related Products of 90905-32-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia