Tag: 100-200

Triazine-pyrimidine based molecular hybrids: synthesis, docking studies and evaluation of antimalarial activity was written by Kumar, Deepak;Khan, Shabana I.;Ponnan, Prija;Rawat, Diwan S.. And the article was included in New Journal of Chemistry in 2014.Related Products of 62968-37-0 This article mentions the following:

A series of novel triazine-pyrimidine hybrids have been synthesized and evaluated for their in vitro antimalarial activity. Some of the compounds showed promising antimalarial activity against both CQ-sensitive and CQ-resistant strains at micromolar level with a high selectivity index. All the compounds displayed better activity (IC₅₀ = 1.32-10.70 婵炴挾鎷? than the standard drug pyrimethamine (>19 婵炴挾鎷? against the chloroquine-resistant strain W2. All the tested compounds were nontoxic against mammalian cell lines. Docking studies of the most active compounds were performed on both wild type and quadruple mutant (N51I, C59R, S108N, I164L) PfDHFR-TS using Glide to analyze the interaction of the compounds with the binding site of the protein. The binding poses of compounds I and II, having a high Glide XP score and the lowest Glide energies, show an efficient binding pattern similar to that of the DHFR substrate (dihydrofolate) in the wild type and mutant DHFR active site. The anal. of the pharmacokinetic properties of the most active compounds using ADMET prediction attests to the possibility of developing compound I as a potent antimalarial lead. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Related Products of 62968-37-0).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Related Products of 62968-37-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Investigation of the reaction of 6-amino-3-methyl-4-oxo-3,4-dihydro-2-pyrimidinylhydrazine was written by Moustafa, M. A.;Gineinah, M. M.;Bayomi, S. M.;Ismaiel, A. M.. And the article was included in Archives of Pharmacal Research in 1990.Safety of 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one This article mentions the following:

The hydrazine derivative I was utilized for the synthesis of three different fused 1,2,4-triazolo [4,3-a]pyrimidine derivatives II (R = H, R¹ = C₆H₄Cl-p, SH; R = CHO, R¹ = H) and a tetrazolo[1,5-a]pyrimidine derivative III. Reaction of I with the chalcone analog 2-thenylidene-2′-acetothienone, gave the pyrazoline derivative IV. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Safety of 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. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Safety of 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

N-Metallacycles from [Cp^*MX₂]₂ and Alkynylpyridines: Synthesis, Reaction Pathway, and Aromaticity was written by Teo, Jing Wei;Sridevi, Venugopal Shanmugham;Leong, Weng Kee. And the article was included in Organometallics in 2014.Electric Literature of C6H4N2 This article mentions the following:

The reaction of [Cp^*MX₂]₂ (M = Rh or Ir, X = Cl, Br, or I) with alkynylpyridines afforded halogen-substituted N-metallacyclic complexes. The reaction pathway has been examined through deuterium labeling and other experiments and computational studies and is proposed to proceed via halide dissociation followed by attack at the alkyne. These N-metallacycles exhibit aromaticity and undergo Sonogashira coupling reactions. In the experiment, the researchers used many compounds, for example, 2-Ethynylpyrimidine (cas: 37972-24-0Electric Literature of 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. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Electric Literature of C6H4N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Palladium(0)/NHC-Catalyzed Reductive Heck Reaction of Enones: A Detailed Mechanistic Study was written by Raoufmoghaddam, Saeed;Mannathan, Subramaniyan;Minnaard, Adriaan J.;de Vries, Johannes G.;Reek, Joost N. H.. And the article was included in Chemistry – A European Journal in 2015.Application of 16879-39-3 This article mentions the following:

We have studied the mechanism of the palladium-catalyzed reductive Heck reaction of para-substituted enones with 4-iodoanisole by using N,N-diisopropylethylamine (DIPEA) as the reductant. Kinetic studies and in situ spectroscopic anal. have provided a detailed insight into the reaction. Progress kinetic anal. demonstrated that neither catalyst decomposition nor product inhibition occurred during the catalysis. The reaction is first order in the palladium and aryl iodide, and zero order in the activated alkene, N-heterocyclic carbene (NHC) ligand, and DIPEA. The experiments with deuterated solvent ([D₇]DMF) and deuterated base ([D₁₅]Et₃N) supported the role of the amine as a reductant in the reaction. The palladium complex [Pd⁰(NHC)(1)] has been identified as the resting state. The kinetic experiments by stopped-flow UV/Vis also revealed that the presence of the second substrate, benzylideneacetone 1, slows down the oxidative addition of 4-iodoanisole through its competing coordination to the palladium center. The kinetic and mechanistic studies indicated that the oxidative addition of the aryl iodide is the rate-determining step. Various scenarios for the oxidative addition step have been analyzed by using DFT calculations (bp86/def2-TZVP) that supported the inhibiting effect of substrate 1 by formation of resting state [Pd⁰(NHC)(1)] species at the cost of further increase in the energy barrier of the oxidative addition step. 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 ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. 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.Application of 16879-39-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis of cyano-substituted heterocycles by tetraethylammonium cyanide was written by Hermann, Klaus;Simchen, Gerhard. And the article was included in Liebigs Annalen der Chemie in 1981.Product Details of 75833-38-4 This article mentions the following:

RCN (R = optionally substituted 2-pyridinyl, 4-pyrimidinyl, 4-quinazolinyl, 2-quinazolinyl, 2-quinoxalinyl) were prepared by treating RCl with NMe₃ and treating RN⁺Me₃ Cl^– with Et₄N⁺ CN^– to give RCN. In the experiment, the researchers used many compounds, for example, 2-Chloropyrimidine-4-carbonitrile (cas: 75833-38-4Product Details of 75833-38-4).

2-Chloropyrimidine-4-carbonitrile (cas: 75833-38-4) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. 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 75833-38-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Aminopyrimidines as electron-rich azadienes: extension of the synthetic potential of hetero Diels-Alder reactions under acidic conditions was written by Garcia, Celeste;Melguizo, Manuel;Cobo, Justo;Sanchez, Adolfo;Nogueras, Manuel;Lopez, Ma Dolores;Low, John N.. And the article was included in Synlett in 2001.SDS of cas: 54030-56-7 This article mentions the following:

By addition of a catalytic amount of a strong acid and selection of the appropriate solvent, the cycloaddition reactions of MeO₂CC濡炪倖鑹鹃幐绀怬₂Me (DMAD) to 6-pyrimidinamines drastically changed their course leading to pyrrolo[3,4-c]pyridines, while, in the absence of acid, 6-amino-3,4-pyridinedicarboxylates were obtained. This change was interpreted on the basis of acid interception of the non-isolable adducts formed by initial hetero Diels-Alder cycloaddition between the reactants. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7SDS of cas: 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. 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.SDS of cas: 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Thermodynamic Understanding of an Aza-Michael Reaction Enables Five-Step Synthesis of the Potent Integrin Inhibitor MK-0429 was written by Gupta, Anya;Condakes, Matthew L.. And the article was included in Journal of Organic Chemistry in 2021.SDS of cas: 90905-32-1 This article mentions the following:

A general strategy for the aza-Michael addition of nucleophilic heterocycles into 閻?substituted acrylates using potassium tert-butoxide as catalyst was describe . Demonstrating that the reaction is under thermodn. control underpins optimization efforts and enables rapid exploration of the substrate scope, with yields ranging from 55% to 94%. It was further leverage these lessons in a significantly shortened synthesis of MK-0429, a potent pan-integrin inhibitor previously taken into human clin. trials for the treatment of prostate cancer and osteoporosis. In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1SDS of cas: 90905-32-1).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.SDS of cas: 90905-32-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pd/PTABS: Catalyst for Room Temperature Amination of Heteroarenes was written by Murthy Bandaru, Siva Sankar;Bhilare, Shatrughn;Chrysochos, Nicolas;Gayakhe, Vijay;Trentin, Ivan;Schulzke, Carola;Kapdi, Anant R.. And the article was included in Organic Letters in 2018.Electric Literature of C8H10ClN3O This article mentions the following:

A mild and highly efficient catalytic amination procedure for chloroheteroarenes at ambient temperature using the Pd/PTABS catalytic system is reported. The protocol is selective for the amination of chloroheteroarenes using secondary amines such as piperidine, pyrrolidine, and several others. The exceptional mildness of the developed protocol is beneficial for the synthesis of a crucial Buparlisib intermediate as well as the formal synthesis of Alogliptin in competitive yields. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Electric Literature of C8H10ClN3O).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) 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. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Electric Literature of C8H10ClN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis of 4-amino substituted quinolines and their 閻?hematin inhibitory activity was written by Singh, Jaybir;Dhakarey, R. K. S.;Singh, Shiv Vardan;Suthar, Manish K.;Saxena, J. K.;Dwivedi, Anil Kumar. And the article was included in Chemistry & Biology Interface in 2012.Related Products of 62968-37-0 This article mentions the following:

In present study, new side chain modified 4-aminoquinoline derivatives and quinoline pyrimidine hybrids were synthesized and evaluated in vitro against 閻?hematin formation. Compounds 20, 21, 22, 23 have shown significant inhibitory activity against 閻?hematin formation. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Related Products of 62968-37-0).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Related Products of 62968-37-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery of 3-Oxabicyclo[4.1.0]heptane, a Non-nitrogen Containing Morpholine Isostere, and Its Application in Novel Inhibitors of the PI3K-AKT-mTOR Pathway was written by Hobbs, Heather;Bravi, Gianpaolo;Campbell, Ian;Convery, Maire;Davies, Hannah;Inglis, Graham;Pal, Sandeep;Peace, Simon;Redmond, Joanna;Summers, Declan. And the article was included in Journal of Medicinal Chemistry in 2019.Reference of 62968-37-0 This article mentions the following:

4-(Pyrimidin-4-yl)morpholines are privileged pharmacophores for PI3K and PIKKs inhibition by virtue of the morpholine oxygen, both forming the key hydrogen bonding interaction and conveying selectivity over the broader kinome. Key to the morpholine utility as a kinase hinge binder is its ability to adopt a coplanar conformation with an adjacent aromatic core favored by the morpholine nitrogen nonbonding pair of electrons interacting with the electron deficient pyrimidine 闁?system. Few selective morpholine replacements have been identified to date. Herein we describe the discovery of a potent non-nitrogen containing morpholine isostere with the ability to mimic this conformation and its application in a potent selective dual inhibitor of mTORC1 and mTORC2 (29b). In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Reference of 62968-37-0).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Reference of 62968-37-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia