Day: November 11, 2022

Xu, Yingying published the artcileIridium-Catalyzed Carbenoid Insertion of Sulfoxonium Ylides for Synthesis of Quinoxalines and β-Keto Thioethers in Water, Formula: C12H8N2S, the main research area is keto thioether green preparation carbenoid insertion annulation water; quinoxaline green preparation carbenoid insertion annulation water.

Sulfoxonium ylides as safe carbene precursors are described for iridium-catalyzed carbene insertions and annulation, providing a facile and green approach to access a variety of quinoxaline derivatives in water. This water-mediated method also allows the preparation of β-keto thioethers under mild condition.

European Journal of Organic Chemistry published new progress about Aromatic diamines Role: RCT (Reactant), RACT (Reactant or Reagent) (ortho). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Formula: C12H8N2S.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Emmadi, Narender Reddy published the artcileSodium dodecylsulfate induced synthesis of quinoxalines, Related Products of quinoxaline, the main research area is quinoxaline preparation; phenylenediamine bromo ketone sodium dodecyl sulfate heterocyclization green chem.

A simple and efficient sodium dodecylsulfate (SDS) induced method for the synthesis of quinoxalines in excellent yields in water at room temperature by the reaction of phenacyl bromides and o-phenylene diamines was developed. Simple reaction conditions, wide compatibility and high yields were the advantages of this protocol.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent) (bromo). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Related Products of quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Liu, Yun-Kui published the artcileRegiospecific Synthesis of Nitroarenes by Palladium-Catalyzed Nitrogen-Donor-Directed Aromatic C-H Nitration, Category: quinoxaline, the main research area is nitro arene regioselective preparation palladium catalyst; regioselective nitration arene nitrogen functional group guided.

Regioselective approach to nitroarenes involving palladium-catalyzed direct ortho-nitration of aromatic C-H bonds guided by a nitrogen functional group is described. E.g., Pd-catalyzed ortho-nitration of aromatic C-H bonds directed by a quinoxaline ligand (e.g., I) in presence of Pd(OAc)2, AgNO2, and K2S2O8 as oxidant gave 86% nitroarene II. The nitrating protocol was applied to other N-donor tethered aromatics [e.g., 2-arylpyridines, benzo[h]quinoline, 2-arylpyrazoles].

Chemistry – A European Journal published new progress about Aromatic nitro compounds Role: SPN (Synthetic Preparation), PREP (Preparation). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Category: quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Ko, Kwangseok published the artcileDiscovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis, Formula: C9H6Cl2N2, the main research area is atopic dermatitis H4 receptor antagonist preparation; pyrido tetrazolo pyrazine analog preparation atopic dermatitis.

The histamine H4 receptor (H4R), a member of the G-protein coupled receptor family, has been considered as a potential therapeutic target for treating atopic dermatitis (AD). A large number of H4R antagonists have been disclosed, but no efficient agents controlling both pruritus and inflammation in AD have been developed yet. Here, we have discovered a novel class of orally available H4R antagonists showing strong anti-itching and anti-inflammation activity as well as excellent selectivity against off-targets. A pharmacophore-based virtual screening system constructed in house successfully identified initial hit compound 9, and the subsequent homol. model-guided optimization efficiently led us to discover pyrido[2,3-e]tetrazolo[1,5-a]pyrazine analog 48 as a novel chemotype of a potent and highly selective H4R antagonist. Importantly, orally administered compound 48 exhibits remarkable efficacy on antipruritus and anti-inflammation with a favorable pharmacokinetic (PK) profile in several mouse models of AD. Thus, these data strongly suggest that our compound 48 is a promising clin. candidate for treatment of AD.

Journal of Medicinal Chemistry published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Formula: C9H6Cl2N2.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Knudsen, Lotte Bjerre published the artcileSmall-molecule agonists for the glucagon-like peptide 1 receptor, SDS of cas: 25983-14-6, the main research area is glucagon like peptide receptor agonist thiadiazolyl quinoxaline preparation SAR.

The peptide hormone glucagon-like peptide (GLP)-1 has important actions resulting in glucose lowering along with weight loss in patients with type 2 diabetes. As a peptide hormone, GLP-1 has to be administered by injection. Only a few small-mol. agonists to peptide hormone receptors have been described and none in the B family of the G protein coupled receptors to which the GLP-1 receptor belongs. We have discovered a series of small mols. known as ago-allosteric modulators selective for the human GLP-1 receptor. These compounds act as both allosteric activators of the receptor and independent agonists. Potency of GLP-1 was not changed by the allosteric agonists, but affinity of GLP-1 for the receptor was increased. The most potent compound identified (I) stimulates glucose-dependent insulin release from normal mouse islets but, importantly, not from GLP-1 receptor knockout mice. Also, the compound stimulates insulin release from perfused rat pancreas in a manner additive with GLP-1 itself. These compounds may lead to the identification or design of orally active GLP-1 agonists.

Proceedings of the National Academy of Sciences of the United States of America published new progress about Glucagon receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 25983-14-6 belongs to class quinoxaline, name is 2,3,6,7-Tetrachloroquinoxaline, and the molecular formula is C8H2Cl4N2, SDS of cas: 25983-14-6.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Gan, Linling published the artcileTetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities, HPLC of Formula: 39267-05-5, the main research area is tetrazanbigen derivative peroxisome proliferator activated receptor gamma partial agonist; anticancer tetrazanbigen derivative.

Tetrazanbigen (TNBG) is a novel sterol isoquinoline derivative with poor water solubility and moderate inhibitory effects on human cancer cell lines via lipoapoptosis induction. Herein, we developed a series of novel TNBG analogs with improved water solubility and antiproliferative activities. The CCK-8 assay enabled us to identify a novel compound, 14g, which strongly inhibited HepG2 and A549 cell growth with IC50 values of 0.54 and 0.47μM, resp. The anticancer effects might be explained by the partial activation and upregulation of PPARγ expression, as indicated by the transactivation assay and western blotting evaluation. Furthermore, the in vitro antiproliferative activity was verified in an in vivo xenograft model in which 14g strongly reduced tumor growth at a dose of 10 mg/kg. In line with these pos. observations, 14g exhibited an excellent water solubility of 31.4 mg/mL, which was more than 1000-fold higher than that of TNBG (4μg/mL). Together, these results suggest that 14g is a promising anticancer therapeutic that deserves further investigation.

Journal of Medicinal Chemistry published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (PTEN). 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, HPLC of Formula: 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Liu, Chun-He published the artcileDesign, synthesis, and biological evaluation of novel 4-alkylamino-1-hydroxymethylimidazo[1,2-a]quinoxalines as adenosine A1 receptor antagonists, HPLC of Formula: 25983-14-6, the main research area is oxoalkylamino chloroquinoxaline heterocyclization; imidazoquinoxaline preparation amine amination; aminoimidazoquinoxaline preparation adenosine receptor ligand.

A series of 4-alkylamino-1-hydroxymethylimidazo[1,2-a]quinoxalines, e.g., I, have been synthesized and evaluated for their adenosine A1 receptor inhibitory activity in the radioligand binding assays. These compounds were tested for the inhibition percent (IP) and the affinity toward A1AR (Ki) that IP were more than 90% in the nanomolar range. 4-Cyclopentylamino-7,8-dichloro-1-hydroxymethylimidazo[1,2-a]quinoxaline (I) was the most potent compound in this series, having Ki = 7 nM, which is remarkably higher than that of IRFI-165 (Ki = 48). 1-Hydroxymethyl groups of the tricyclic heteroaromatic compounds displayed the potent affinities toward A1AR.

Bioorganic & Medicinal Chemistry published new progress about Structure-activity relationship, purinergic receptor-binding. 25983-14-6 belongs to class quinoxaline, name is 2,3,6,7-Tetrachloroquinoxaline, and the molecular formula is C8H2Cl4N2, HPLC of Formula: 25983-14-6.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Crundwell, Guy published the artcileBis[2-(thiophen-2-yl)quinoxaline-κN 4]silver(I) tetrafluoridoborate, Recommanded Product: 2-(Thiophen-2-yl)quinoxaline, the main research area is crystal structure coordination compound silver bisthienylquinoxaline complex tetrafluoridoborate; mol structure silver bisthienylquinoxaline complex tetrafluoridoborate.

In the title compound, [Ag(C12H8N2S)2]BF4, the two-coordinate AgI ion lies on a crystallog. inversion center and is linearly bonded to the N-donor atoms of two sep. quinoxaline ligands. The thienyl ring of the ligand is nearly coplanar with the quinoxaline ring system [dihedral angle = 9.15 (13)°]. In the crystal, the complex mols. pack in layers parallel to (-102) and form weak π-π ring stacking interactions [min. ring centroid separation = 3.7054 (17) Å]. The tetrafluoridoroborate anion is equally disordered about an inversion center. Crystallog. data are given.

Acta Crystallographica, Section E: Structure Reports Online published new progress about Crystal structure. 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Recommanded Product: 2-(Thiophen-2-yl)quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Dubovtsev, Alexey Yu. published the artcileNature of the Nucleophilic Oxygenation Reagent Is Key to Acid-Free Gold-Catalyzed Conversion of Terminal and Internal Alkynes to 1,2-Dicarbonyls, SDS of cas: 40353-41-1, the main research area is alkyne gold catalyst dichloropyridine nitrogen oxide nucleophilic oxygenation; diketone preparation; azaheterocycle one pot preparation.

2,3-Dichloropyridine N-oxide, a novel oxygen transfer reagent, allows the conductance of the gold(I)-catalyzed oxidation of alkynes to 1,2-dicarbonyls in the absence of any acid additives and under mild conditions to furnish the target species, including those derivatized by highly acid-sensitive groups. The developed strategy is effective for a wide range of alkyne substrates such as terminal- and internal alkynes, ynamides, alkynyl ethers/thioethers, and even unsubstituted acetylene (40 examples; yields up to 99%). The oxidation was successfully integrated into the trapping of reactive dicarbonyls by one-pot heterocyclization and into the synthesis of six-membered azaheterocycles. This synthetic acid-free route was also successfully applied for the total synthesis of a natural 1,2-diketone.

Journal of Organic Chemistry published new progress about Catalyst supports, oxidation catalyst supports. 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, SDS of cas: 40353-41-1.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Gazit, Aviv published the artcileTyrphostins. 5. Potent Inhibitors of Platelet-Derived Growth Factor Receptor Tyrosine Kinase: Structure-Activity Relationships in Quinoxalines, Quinolines, and Indole Tyrphostins, Related Products of quinoxaline, the main research area is quinoxaline tyrosine kinase inhibitor preparation structure; platelet growth factor receptor kinase preparation; quinoline tyrosine kinase inhibitor preparation structure; indole tyrphostin tyrosine kinase inhibitor preparation; MSBAR tyrosine kinase inhibitor tyrphostin.

A series of 3-indoleacrylonitrile tyrphostins, 2-chloro-3-phenylquinolines, and 3-arylquinoxalines were prepared and tested for inhibition of platelet-derived growth factor receptor tyrosine kinase (PDGF-RTK) activity. The potency of the inhibitors was quinoxalines >quinolines >indoles. Lipophilic groups (Me, methoxy) in the 6 and 7 positions and Ph at the 3 position of quinoxalines and quinolines were essential for potency, in contrast to the hydrophilic catechol group in tyrphostins active against EGFR kinase inhibition at different sites. The inhibitors showed selectivity for PDGF and were not active against EGF receptor and HER-2/c-ErbB-2 receptor.

Journal of Medicinal Chemistry published new progress about. 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Related Products of quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider