Day: November 16, 2022

Henen, Morkos A. published the artcile[1,2,4]Triazolo[4,3-a]quinoxaline: synthesis, antiviral, and antimicrobial activities, Quality Control of 39267-05-5, the main research area is triazoloquinoxaline bioisostere pyrimidotriazoloquinoxaline preparation antibacterial antifungal antiviral agent.

Several novel [1,2,4]triazolo[4,3-a]quinoxaline derivatives and their isosteres, pyrimidine-quinoxaline derivatives [i.e., Pyrimido[1′,2′:1,5][1,2,4]triazolo[4,3-a]quinoxaline derivatives] were designed as potential antiviral and antimicrobial agents and the synthesis of the target compounds was achieved using 4-chloro-8-methyl[1,2,4]triazolo[4,3-a]quinoxalin-1-amine as a key intermediate in an an aromatic nucleophilic substitution with different amines or triazolethiol. Some of the title compounds were subjected to an in-vitro antiviral and cytotoxicity screening by a plaque-reduction assay method. Most of the tested compounds exhibited cytotoxicity at a concentration 160 μg/mL and one compound displayed promising antiviral activity. In-vitro antimicrobial screening against different pathogenic organisms using an agar diffusion method demonstrated that several compounds also exhibited antibacterial and/or antifungal activities.

Medicinal Chemistry Research published new progress about Anti-infective agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Quality Control of 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Smits, Rogier A. published the artcileFragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo, COA of Formula: C8H2Cl4N2, the main research area is methylpiperazin quinoxaline derivative preparation structure H4 receptor ligand antiinflammatory.

Using a previously reported flexible alignment model the authors have designed, synthesized, and evaluated a series of compounds at the human histamine H4 receptor (H4R) from which 2-(4-methyl-piperazin-1-yl)-quinoxaline (I) was identified as a new lead structure for H4R ligands. Exploration of the structure-activity relationship (SAR) of this scaffold led to the identification of 6,7-dichloro 3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one (VUF 10214, II) and 2-benzyl-3-(4-methyl-piperazin-1-yl)quinoxaline (VUF 10148, III) as potent H4R ligands with nanomolar affinities. In vivo studies in the rat reveal that compound II has significant anti-inflammatory properties in the carrageenan-induced paw-edema model.

Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 25983-14-6 belongs to class quinoxaline, name is 2,3,6,7-Tetrachloroquinoxaline, and the molecular formula is C8H2Cl4N2, COA of Formula: C8H2Cl4N2.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Noorulla, S. Md. published the artcileSynthesis of certain substituted quinoxaline as antiinflammatory agents, Safety of 2,3-Dichloro-6-methylquinoxaline, the main research area is quinoxaline preparation antiinflammatory agent.

Substituted quinoxaline have received considerable attention during last two decades as they are endowed with variety of biol. activities and have wide range of therapeutic properties. A literature survey indicates that quinoxaline derivatives possess different pharmacol. and biol. activities, of which the most potent is anti-inflammatory activity. In view of above literature survey, the authors thought to synthesize a novel substituted quinoxaline system. An example compound thus prepared and evaluated was an isoniazid hydrazide (I) [i.e., 4-pyridinecarboxylic acid 2-[7-methyl-3-[2-[(2,4-dichlorophenyl)methylene]hydrazinyl]-2-quinoxalinyl]hydrazide derivatives, isoniazid quinoxaline Schiff base derivative]. The synthesis of the target compounds was achieved by a condensation of 4-pyridinecarboxylic acid hydrazide (i.e., isoniazid) with 2-chloro-2-[(phenylmethylene)hydrazinyl]quinoxaline derivatives

International Journal of Research in Pharmacy and Chemistry published new progress about Anti-inflammatory agents. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Safety of 2,3-Dichloro-6-methylquinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Sun, Huikai published the artcileFirst-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson’s Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate, Recommanded Product: 2,3-Dichloro-6-methylquinoxaline, the main research area is Parkinson’s disease GPR6 inverse agonists GPCR D2R motor.

Parkinson’s disease (PD) is a chronic and progressive movement disorder with the urgent unmet need for efficient symptomatic therapies with fewer side effects. GPR6 is an orphan G-protein coupled receptor (GPCR) with highly restricted expression in dopamine receptor D2-type medium spiny neurons (MSNs) of the indirect pathway, a striatal brain circuit which shows aberrant hyperactivity in PD patients. Potent and selective GPR6 inverse agonists (IAG) were developed starting from a low-potency screening hit (EC50 = 43μM). Herein, we describe the multiple parameter optimization that led to the discovery of multiple nanomolar potent and selective GPR6 IAG, including our clin. compound CVN424 (I). GPR6 IAG reversed haloperidol-induced catalepsy in rats and restored mobility in the bilateral 6-OHDA-lesioned rat PD model demonstrating that inhibition of GPR6 activity in vivo normalizes activity in basal ganglia circuitry and motor behavior. CVN424 is currently in clin. development to treat motor symptoms in Parkinson’s disease.

Journal of Medicinal Chemistry published new progress about Basal ganglia (circuitry). 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Recommanded Product: 2,3-Dichloro-6-methylquinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

McKinney, Andrew M. published the artcileA rapid and efficient method for the reduction of quinoxalines, Application In Synthesis of 40353-41-1, the main research area is quinoxaline borane stereoselective reduction; hydroquinoxaline preparation.

Mono- and di-substituted alkyl- and arylquinoxalines are rapidly reduced in high yield to their resp. 1,2,3,4-tetrahydro derivatives by BH3 in THF solution In the case of the 2,3-di-substituted compounds, reduction is stereoselective yielding exclusively the cis-isomers. NaBH4 in AcOH also reduces alkyl- and arylquinoxalines, but proceeds with lower yields and often produces side products. NaBH4 in EtOH reduces quinoxaline and 2-methylquinoxaline in high yield. However, the reaction is very slow, whereas 2,3-dialkyl- and 2-arylquinoxalines are not efficiently reduced by NaBH4 in EtOH.

Journal of Heterocyclic Chemistry published new progress about Reduction, stereoselective. 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Application In Synthesis of 40353-41-1.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Clark, Terence published the artcileThe photolysis of quinomethionate in benzene solution, Formula: C9H6Cl2N2, the main research area is photolysis quinomethionate fungicide mechanism; quinoxaline.

Photolysis of the fungicide quinomethionate (I) (C6H6, for 8 h) resulted in cleavage of the dithiole ring with loss of both S atoms to give quinoxaline dione II and the methylquinoxalines III (R ≠ R1 = H, Me). A mechanism is proposed involving initial loss of CO followed by rapid loss of S, either as the element or after oxidation

Pesticide Science published new progress about Cyclocondensation reaction. 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

Shi, Ren-xin published the artcileSodium tetrachloroaurate(III) dihydrate-catalyzed efficient synthesis of 1,5-benzodiazepine and quinoxaline derivatives, Safety of 2-(Thiophen-2-yl)quinoxaline, the main research area is quinoxaline benzodiazepine preparation sodium tetrachloroaurate; furan thiophene phenyl quinoxaline preparation.

Both 1,5-benzodiazepine and quinoxaline derivatives are important heterocyclic components in pharmaceutical compounds The synthesis of the target compounds was achieved efficiently and cleanly using benzenediamine and ketones as reactants and sodium tetrachloroaurate(III) dihydrate as catalyst. This catalyst was shown to be effective for the synthesis of quinoxaline derivatives from phenylenediamine and α-bromo ketones under similar reaction conditions.

Journal of Zhejiang University, Science, B published new progress about Cyclocondensation reaction. 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Safety of 2-(Thiophen-2-yl)quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

El-Sharief, A. M. SH. published the artcileNovel synthesis and cyclization reactions of 3-amino-2-mercaptopyrrole derivatives, SDS of cas: 39267-05-5, the main research area is pyrrolopyrrolinedione preparation; pyrrolothiazole preparation; pyrrolothiazine preparation; pyrrole aminomercapto preparation cyclization; cyanothioformamide chalcone cyclization; aminomercaptopyrrole preparation cyclization chloroacetate chloroacetamide chloronaphthoquinone; isocyanate cyclization aminomercaptopyrrole; chlorobenzoyl chloride cyclization aminomercaptopyrrole.

Interaction of cyanothioformamides RNHC(:S)CN (R = Me, Et, Ph) with chalcones gave 3-amino-2-mercaptopyrroles I (R1, R2 = H, Cl, Br), which have the tautomeric structures of 3-aminopyrroline-2-thiones and 3-iminopyrrolidine-2-thiones. I reacted with chloroacetic acid, Et chloroacetate, chloroacetamide and 2,3-dichloro-1,4-naphthoquinone to give pyrrolothiazines. Reaction of I with PhN:C:O or p-ClC6H4COCl gave pyrrolothiazoles. Reaction of maleimides with RNHC(:S)CN gave pyrrolopyrrolinediones.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Cyclocondensation reaction. 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, SDS of cas: 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Peng, Yun published the artcileReactivity Umpolung of the C=N Bond in Quinoxaline Scaffold Enabling Direct Nucleophilic Attack of Alkyl Grignard Reagents at the N-Terminus, Recommanded Product: 2-(Thiophen-2-yl)quinoxaline, the main research area is quinoxaline Grignard reagent tandem regioselective alkylation carbon bond cleavage; quinoxalinone preparation.

The reactivity umpolung of the C=N bond in the quinoxaline scaffold was successfully realized for the first time by introduction of a formyl or an acyl group adjacent to the C-position of the C=N moiety. The reversed reactivity of the C=N bond thus enabled direct nucleophilic attack of alkyl Grignard reagents at the N-terminus rather than the C-terminus, thereby providing an unprecedented and efficient method for the synthesis of quinoxalin-2(1H)-one derivatives involving a tandem N-alkylation/C-C bond cleavage process.

Organic Letters published new progress about Alkylation, regioselective. 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