Tag: 100-200

Nonpeptide 濞?sub>v閻?sub>3 Antagonists. Part 11: Discovery and Preclinical Evaluation of Potent 濞?sub>v閻?sub>3 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 濞?sub>v閻?sub>3 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

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閻犺櫣鏋巘₂O. 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

Behavior of some 2-(闁?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闁?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

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

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

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

Three-component synthesis of hexahydropyridopyrimidine-spirocyclohexanetriones induced by microwave was written by Quiroga, Jairo;Cruz, Silvia;Insuasty, Braulio;Abonia, Rodrigo;Nogueras, Manuel;Cobo, Justo. And the article was included in Tetrahedron Letters in 2006.Electric Literature of C6H9N3OS This article mentions the following:

Spiro pyridopyrimidinone cyclohexanediones and pyrimido[4,5-b]quinolinones were obtained in a three-component microwave-assisted reaction of 6-aminopyrimidin-4-ones with dimedone and formaldehyde solution or paraformaldehyde, resp. A mechanism is proposed based on the presence of a basic catalyst (Et₃N in this case) and the fact that single condensation intermediates are isolated prior to the cyclization leading to the final products. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Electric Literature of C6H9N3OS).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Electric Literature of C6H9N3OS

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Construction of 1-Heteroaryl-3-azabicyclo[3.1.0]hexanes by sp³-sp² Suzuki-Miyaura and Chan-Evans-Lam Coupling Reactions of Tertiary Trifluoroborates was written by Harris, Michael R.;Li, Qifang;Lian, Yajing;Xiao, Jun;Londregan, Allyn T.. And the article was included in Organic Letters in 2017.Product Details of 51421-99-9 This article mentions the following:

Compounds that contain the 1-heteroaryl-3-azabicyclo[3.1.0]hexane architecture are of particular interest to the pharmaceutical industry yet remain a challenge to synthesize. We report herein an expedient and modular approach to the synthesis of 1-heteroaryl-3-azabicyclo[3.1.0]hexanes by Suzuki-Miyaura and Chan-Evans-Lam coupling reactions of tertiary trifluoroborate salts. Our Suzuki-Miyaura cross-coupling protocol is compatible with a broad range of aryl and heteroaryl bromides and chlorides. The unprecedented Chan-Evans-Lam coupling of tertiary trifluoroborates allows the facile construction of 1-heteroaryl-3-azabicyclo[3.1.0]hexanes containing C-tertiary arylamines at the ring juncture. In the experiment, the researchers used many compounds, for example, 4-Chloro-2-methoxypyrimidine (cas: 51421-99-9Product Details of 51421-99-9).

4-Chloro-2-methoxypyrimidine (cas: 51421-99-9) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. 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.Product Details of 51421-99-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Nucleophilic substitutions in the 2-methane sulfonylpyrimidine series was written by Budesinsky, Zdenek;Vavrina, Josef. And the article was included in Collection of Czechoslovak Chemical Communications in 1972.Application of 38275-61-5 This article mentions the following:

Oxidation of 5-substituted 2-methylthiopyrimidines gave the 2-methylsulfonyl derivatives, the nucleophilic substitution of which with NaOMe, N2H4, PhCH2NH2, NaCN, NaSH, and NaCH(CN)CO2Me gave the appropriate 5-substituted 2-methoxy-, 2-mercapto-, 2-hydrazino, 2-benzylamino-, 2-cyano-, and 2-(methoxycarbonylcyano-methyl)pyrimidine. 2-Methylsulfonyl-5-fluoropyrimidine (I) treated at 0闁?with NaOMe gave 2-methoxy-5-fluoropyrimidine but at a higher temperature and with excess NaOMe, 2,5-dimethoxypyrimidine was formed. I and N2H4 gave 5-hydrazino-2-meth-ylsulfonylpyrimidine. 5-Benzylamino-2-methylsulfonylpyri-midine was prepared analogously. At 10-20闁? the reaction of 2 methylsulfonyl-5-halo(fluoro, chloro, bromo)pyrimidines with-NaCN gave the 2-cyano derivatives but at a higher temperature, 2-cyano-5-methylsulfonylpyrimidine was formed. 2-Cyano-5-methylpyrimidine, 2-cyano-5-methoxypyrimidine, 2-cyano-5-fluoropyrimidine, 2-cyano-5-chloropyrimidine, and 2-cyano-5-bromopyrimidine exhibited an intensive sweet taste. In the experiment, the researchers used many compounds, for example, 5-Chloropyrimidine-2-carboxylic acid (cas: 38275-61-5Application of 38275-61-5).

5-Chloropyrimidine-2-carboxylic acid (cas: 38275-61-5) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. 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.Application of 38275-61-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hemilabile MICN^{铏?/sup> ligands allow oxidant-free Au(I)/Au(III) arylation-lactonization of 绾?alkenoic acids was written by Font, Pau;Valdes, Hugo;Guisado-Barrios, Gregorio;Ribas, Xavi. And the article was included in Chemical Science in 2022.Name: 2-Ethynylpyrimidine This article mentions the following:}

Here authors describe the synthesis of two Au(I) complexes bearing bidentate hemilabile MICN^{铏?/sup> ligands ligands, [AuI(MICN铏?/sup>)Cl], and their ability to stabilize square-planar Au(III) species (MIC = mesoionic carbene). The presence of the hemilabile N-ligand contributed to stabilize the ensuing Au(III) species acting as a five-membered ring chelate upon its coordination to the metal center. The Au(III) complexes can be obtained either by using external oxidants or, alternatively, by means of feasible oxidative addition with strained biphenylene C_sp2-C_sp2 bonds as well as with aryl iodides. Based on the fundamental knowledge gained on the redox properties on these Au(I)/Au(III) systems, authors successfully develop a novel Au(I)-catalytic procedure for the synthesis of 绾?substituted 绾?butyrolactones through the arylation-lactonization reaction of the corresponding 绾?alkenoic acid. The oxidative addition of the aryl iodide, which in turn is allowed by the hemilabile nature of the MICN铏?/sup> ligand, is an essential step for this transformation. In the experiment, the researchers used many compounds, for example, 2-Ethynylpyrimidine (cas: 37972-24-0Name: 2-Ethynylpyrimidine).}

2-Ethynylpyrimidine (cas: 37972-24-0) 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. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Name: 2-Ethynylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia