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More than two decades ago, the quinoxalinedione scaffold was shown to act as an alpha-amino acid bioisoster. Following extensive structure-activity relationship (SAR) studies, the antagonists DNQX, CNQX, and NBQX in the ionotropic glutamate receptor field were identified. In this work, we revisit the quinoxalinedione scaffold and explore the incorporation of an acid functionality in the 6-position. The SAR studies disclose that by this strategy it was possible to tune in iGluR selectivity among the AMPA, NMDA, and KA receptors, and to some extent also obtain full receptor subtype selectivity. Highlights of the study of 44 new analogues are compound 2m being a high affinity ligand for native AMPA receptors (IC50= 0.48 muM), analogues 2e,f,h,k,v all displayed selectivity for native NMDA receptors, and compounds 2s,t,u are selective ligand for the GluK1 receptor. Most interestingly, compound 2w was shown to be a GluK3-preferring ligand with full selectivity over native AMPA, KA and NMDA receptors.

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This disclosure describes substituted 2,3,3a,4-tetrahydro-1H-pyrrolo[1′,2′:4,5][1,4]oxazino[2,3-b]quinoxalines and 1,2,3,4,4a,5-hexahydropyrido[1′,2′:4,5][1,4]oxazino[2,3-b]quinoxalines which possess anxioyltic activity.

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Though the past few decades, the development of new luminescent materials has received a lot of attention due to their applications as fluorescent sensors, in biological microscopy and in optoelectronic devices. Most of these applications are relied on intramolecular charge transfer (ICT). Presence of electron withdrawing N-heterocycles such as pyrazine and quinoxaline rings appeared therefore particularly interesting to be used as electron-attracting part in pi-conjugated structures. Moreover, presence of nitrogen atoms with lone electron pairs allows to the pyrazine and the quinoxaline ring to act as effective and stable complexing agent or as base that can be protonated. This review reports luminescent small molecules and oligomers including a pyrazine or quinoxaline ring in their scaffold highlighting their applications related to photoluminescence and electroluminescence.

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The present invention includes CSNK1A1 inhibitors that are useful in treating or preventing a cancer in a subject. In certain embodiments, the cancer comprises a hematological cancer, such as but not limited to acute myeloid leukemia (AML) and/or MDS (myelodysplastic syndrome, including 5q-MDS). In other embodiments, the cancer comprises colon cancer.

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The present invention relates to novel heterocyclic compounds useful in preparing drugs for the treatment of diseases associated with various functions of the histamine 4 receptor. Specifically, these drugs are useful in the prevention or treatment of inflammatory disorder, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itch skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, age-related macular degeneration, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (colitis, Crohn’s disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.

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METHOD OF TREATING GLYCOGEN STORAGE DISEASE

The present disclosure provides methods and compositions for the treatment of hepatic symptoms of glycogen storage diseases through the administration of thyroid hormone receptor agonists. The methods and compositions provided herein are useful in the treatment of hyperlipidemia, hypercholesterolemia, hepatic steatosis, cardiomegaly, hepatomegaly, hepatic fibrosis, and cirrhosis associated with glycogen storage diseases (GSD) and defects of glycogen metabolism. Said compounds may also be useful in the prevention of GSD-related hepatocellular adenoma and hepatocellular carcinoma.

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Synthesis, characterization and biological evaluation of some quinoxaline derivatives: A promising and potent new class of antitumor and antimicrobial agents

In continuation of our endeavor towards the development of potent and effective anticancer and antimicrobial agents; the present work deals with the synthesis of some novel tetrazolo[1,5-a]quinoxalines, N-pyrazoloquinoxalines, the corresponding Schiff bases, 1,2,4-triazinoquinoxalines and 1,2,4-triazoloquinoxalines. These compounds were synthesized via the reaction of the key intermediate hydrazinoquinoxalines with various reagents and evaluated for anticancer and antimicrobial activity. The results indicated that tetrazolo[1,5-a]quinoxaline derivatives showed the best result, with the highest inhibitory effects towards the three tested tumor cell lines, which were higher than that of the reference doxorubicin and these compounds were non-cytotoxic to normal cells (IC50 values > 100 mug/mL). Also, most of synthesized compounds exhibited the highest degrees of inhibition against the tested strains of Gram positive and negative bacteria, so tetrazolo[1,5-a]quinoxaline derivatives show dual activity as anticancer and antimicrobial agents.

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The synthesis of novel, visible-wavelength, oxidizable polymerization sensitizers based on the 8-halogeno-5,12-dihydroquinoxalino[2,3-b]quinoxaline skeleton

Novel dyes, based on the 8-halogeno-5,12-dihydroquinoxalino[2,3-b]quinoxaline skeleton, were synthesized and characterized using 1H NMR spectroscopy and chemical ionization mass spectroscopy. Their electrochemical and spectral properties, such as absorption and emission spectra, quantum yield of fluorescence and quantum yield of singlet oxygen generation, were also measured. These dyes were used as oxidizable sensitizers for diphenyliodonium and N-alkoxypyridinium salts. Photoredox pairs, consisting of dyes and pyridinium or iodonium salts, were found to be effective visible-wavelength initiators of free radical or cationic polymerization, respectively. The ability of each dye to act as a photoinitiator strongly depended upon its chemical structure. The heavy atoms present in the chemical structure could lead to excited triplet states within the dye, thereby facilitating electron transfer from these states.

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Application of 108229-82-9, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.108229-82-9, Name is 6-Bromo-2,3-dichloroquinoxaline, molecular formula is C8H3BrCl2N2. In a article£¬once mentioned of 108229-82-9

COMPOUNDS AND METHODS USEFUL FOR TREATING OR PREVENTING CANCERS

The present invention includes CSNK1A1 inhibitors that are useful in treating or preventing a cancer in a subject. In certain embodiments, the cancer comprises a hematological cancer, such as but not limited to acute myeloid leukemia (AML) and/or MDS (myelodysplastic syndrome, including 5q-MDS). In other embodiments, the cancer comprises colon cancer.

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Quinoxaline | C8H6N1997 | ChemSpider

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Synthesis of some new tetrazolo- [1,5-a]quinazolino[2,3-c]imidazo- [4,5-b]quinoxaline derivatives as antimicrobial agents

Treatment of 6,7-dimethoxy-2-chloroquinazolin-4-amine 1 and 7,8-dimethoxy tetrazolo-[1, 5-a]-quinazolin-5-amine 4 with 2, 3- dichloroquinoxaline 2a-e in glacial acetic acid /DMF afford corresponding substituted 6,7-dimethoxy-2- chloroquinazolo[3,4- c]-imidazo-[4,5-b]-quinoxalines 3a-e and 7,8-dimethoxytetrazolo- [1,5-a]-quinazolo-[2,3-c]-imidazo-[4,5-b]-quninoxalines 5a-e. The chemical structures of the newly synthesized compounds have been characterized by IR, NMR, mass spectral and CHN analysis. All the title compounds are subjected to in vitro antibacterial testing against two pathogenic strains and antifungal screening against two fungi. Among the tested compounds, 5b and 5c show significant antibacterial and antifungal activities. Also the compound 3b show significant antifungal activity against Candia albicans.

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