Category: 62968-37-0

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

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

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

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

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

Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer was written by Wu, Chun-Feng;Wang, Qing-Chen;Chen, Rui;Zhou, Hai-Ling;Wu, Ting-Ting;Du, Yao;Zhang, Na-Na;Zhang, Hui-Min;Fan, Zu-Yan;Wang, Li-Li;Hu, Chu-Jiao;Sang, Zhi-Pei;Li, Hong-Liang;Wang, Ling;Tang, Lei;Zhang, Ji-Quan. And the article was included in European Journal of Medicinal Chemistry in 2022.Category: pyrimidines This article mentions the following:

The development of inhibitors targeting the PI3K-Akt-mTOR signaling pathway has been greatly hindered by the on-target AEs, such as hyperglycemia and hepatotoxicities. In this study, a series of diaryl urea derivatives has been designed and synthesized based on clin. candidate gedatolisib, and most of the newly synthesized derivatives showed kinase inhibitory and antiproliferative activities within nanomolar and submicromolar level, resp. The terminal L-proline amide substituted derivative I showed 8.6-fold more potent PI3K浼?inhibitory activity (0.7 nM) and 4.6-fold more potent antiproliferative effect against HCT116 cell lines (0.11娓璏) compared with control gedatolisib. The potential antitumor mechanism and efficacy of I in HCT116 xenograft models have also been evaluated, and found I showed comparable in vivo antitumor activity with gedatolisib. The safety investigations revealed that compound I exhibited more safer profiles in the selectivity of liver cells (selectivity index: >6.6 vs 1.85) and blood glucose regulation than gedatolisib. In addition, the in vitro stability assays also indicated that developed compound I possessed good metabolic stabilities. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Category: pyrimidines).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Efficient and convenient preparation of 3-aryl-2,2-dimethylpropanoates via Negishi coupling was written by Kwak, Young-Shin;Kanter, Aaron D.;Wang, Bing;Liu, Yugang. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2009.HPLC of Formula: 62968-37-0 This article mentions the following:

An efficient and convenient Negishi coupling protocol was developed for the preparation of 3-aryl-2,2-dimethylpropanoates providing easy access to key pharmaceutical intermediates that often require multi-step synthesis using conventional enolate chem. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0HPLC of Formula: 62968-37-0).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) 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.HPLC of Formula: 62968-37-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Suzuki-Miyaura cross-coupling reaction of aryl and heteroaryl pinacol boronates for the synthesis of 2-substituted pyrimidines was written by Asano, Shigehiro;Kamioka, Seiji;Isobe, Yoshiaki. And the article was included in Tetrahedron in 2012.Computed Properties of C8H10ClN3O This article mentions the following:

Suzuki-Miyaura cross-coupling reaction with 2-heteroarylboronic acids is generally challenging due to easy decomposition of these acids. To overcome this problem, we developed a coupling method that uses 2-heteroaryl pinacol boronates in the presence of 1.0 mol % Pd(OAc)₂ and 2.0 mol % S-Phos with 4 equiv amount of LiOH in dioxane and H₂O at 80 鎺矯 for 30 min. This developed method allowed for the synthesis of a wide variety of 2-heteroaryl pyrimidines from 2-chloropyrimidyl derivatives in high yields, and is also useful in the preparation of various biaryl derivatives from heteroaryl chlorides. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Computed Properties of C8H10ClN3O).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) 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.Computed Properties of C8H10ClN3O

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

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 μM) than the standard drug pyrimethamine (>19 μM) 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