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A new series of 3-[2-(5-mercapto-4-phenyl-4H-1,2,4-traiazol-3-yl)ethyl] quinoxalin-2(1H)-one (5a-v) derivatives was synthesized and subjected to in vitro evaluation for anti-inflammatory activity (BSA anti-denaturation assay) and p38alpha MAPK inhibition. Few selected compounds (5a, 5e, 5f, 5g, 5h, 5l, 5q and 5u) were studied for their in vivo anti-inflammatory activity, ulcerogenicity and lipid peroxidation potential. Compounds 5e and 5f were found to be the most active in the series showing 83.45% and 84.15% anti-inflammatory activity respectively when compared to diclofenac sodium (83.22%). They were also found to have low ulcerogenic potential and lipid peroxidation. The p38alpha MAP kinase inhibition of the compounds 5e and 5f was also found to be slightly better than the standard SB 203580. The compounds were also docked against p38alpha MAP kinase enzyme in order to predict their binding mode. Compounds 5e and 5f showed stronger binding with an additional hydrogen bond interaction with ASP-168 which was not observed in SB 203580.

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Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. Application In Synthesis of 3-(3-Hydroxyquinoxalin-2-yl)propanoic acid, In a article, mentioned the application of 7712-28-9, Name is 3-(3-Hydroxyquinoxalin-2-yl)propanoic acid, molecular formula is C11H10N2O3

Quinoxalines belong to a class of excellent heterocyclic scaffolds owing to their wide biological properties and diverse therapeutic applications in medicinal research. They are complementary in shapes and charges to numerous biomolecules they interact with, thereby resulting in increased binding affinity. The pharmacokinetic properties of drugs bearing quinoxaline cores have shown them to be relatively easy to administer either as intramuscular solutions, oral capsules or rectal suppositories. This work deals with recent advances in the synthesis and pharmacological diversities of quinoxaline motifs which might pave ways for novel drugs development.

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New Advances in Chemical Research, May 2021. In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of 3-(3-Hydroxyquinoxalin-2-yl)propanoic acid, We’ll be discussing some of the latest developments in chemical about CAS: 7712-28-9, name is 3-(3-Hydroxyquinoxalin-2-yl)propanoic acid. In an article,Which mentioned a new discovery about 7712-28-9

Infection by human immunodeficiency virus still represents a continuous serious concern and a global threat to human health. Due to appearance of multi-resistant virus strains and the serious adverse side effects of the antiretroviral therapy administered, there is an urgent need for the development of new treatment agents, more active, less toxic and with increased tolerability to mutations. Quinoxaline derivatives are an emergent class of heterocyclic compounds with a wide spectrum of biological activities and therapeutic applications. These types of compounds have also shown high potency in the inhibition of HIV reverse transcriptase and HIV replication in cell culture. For these reasons we propose, in this work, the design, synthesis and biological evaluation of quinoxaline derivatives targeting HIV reverse transcriptase enzyme. For this, we first carried out a structure-based development of target-specific compound virtual chemical library of quinoxaline derivatives. The rational construction of the virtual chemical library was based on previously assigned pharmacophore features. This library was processed by a virtual screening protocol employing molecular docking and 3D-QSAR. Twenty-five quinoxaline compounds were selected for synthesis in the basis of their docking and 3D-QSAR scores and chemical synthetic simplicity. They were evaluated as inhibitors of the recombinant wild-type reverse transcriptase enzyme. Finally, the anti-HIV activity and cytotoxicity of the synthesized quinoxaline compounds with highest reverse transcriptase inhibitory capabilities was evaluated. This simple screening strategy led to the discovery of two selective and potent quinoxaline reverse transcriptase inhibitors with high selectivity index.

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The binding of ten quinoxaline compounds (1?10) to a site adjacent to S2 (AS2) of cruzain (CRZ) was evaluated by a protocol that include a first analysis through docking experiments followed by a second analysis using the Molecular Mechanics-Poisson-Boltzmann Surface Area method (MM-PBSA). Through them we demonstrated that quinoxaline compounds bearing substituents of different sizes at positions 3 or 4 of the heterocyclic ring might interact with the AS2, particularly interesting site for drug design. These compounds showed docking scores (DeltaGdock) which were similar to those estimated for inhibitors that bind to the enzyme through non-covalent interactions. Nevertheless, the free binding energies (DeltaG) values estimated by MM-PBSA indicated that the derivatives 8?10, which bear bulky substituents at position 3 of the heterocycle ring, became detached from the binding site under a dynamic study. Surprisingly, the evaluation of the inhibitory activity of cruzipain (CZ) of some derivatives showed that they increase the enzymatic activity. These results lead us to conclude about the relevance of AS2 as a pocket for compounds binding site, but not necessarily for the design of anti-chagasic compounds.

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In recent years, great efforts have been dedicated to the design of compounds acting as selective inhibitors of the HIV-1 reverse transcriptase (RT). Due to the promissory results previously attained with some quinoxaline derivatives, we aimed to improve the specific standard Hinsberg synthetic pathway by means of biocatalysis or microwave (MW) irradiation. Both techniques rendered the products in very good yields. However, employing the microwave-assisted organic synthesis (MAOS), in the absence of solvent, the same reactions may be completed in minutes. Some of these quinoxalinone derivatives exhibited good inhibitor activity against some human tumoral cells and the lymphoma related to HIV-1.

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The invention discloses a matrix metalloprotease inhibiting activity of the quinoxaline derivative and its preparation method and application, the invention synthesizes a series of specific matrix metalloproteinase – 9 and/or matrix metalloprotease – 13 inhibiting activity of the quinoxaline derivatives, such compounds can be used as MMP – 9 and/or matrix metalloprotease – 13 specific inhibitor, and then can become a therapeutic index higher can be used for clinical drug, solved in the prior art in the treatment of osteoarthritis, osteoporosis, periodontal disease drug type less, curative effect is not sufficiently precise and the like. (by machine translation)

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Compounds of the formula below are useful for expanding the lumina or air passages in a mammal in need of said treatment. The compounds are also useful for treating atopic eczema and urticaria. STR1 wherein X and Y are the same or different and are hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, alkyl of one to four carbon atoms, inclusive, alkoxy of one to four carbon atoms, inclusive, and cyano; R1 is hydrogen, methyl or ethyl; R2 is hydrogen, alkyl of one to six carbon atoms, inclusive, phenyl, benzyl, CH2 Z wherein Z is fluoro, chloro, or bromo, CO2 M, CH2 CO2 M, CH2 CH2 CO2 M and CHR3 CO2 M wherein M is hydrogen, alkyl of one to four carbon atoms, inclusive, or a physiologically acceptable metal or amine cation and R3 is alkyl of one to three carbon atoms, inclusive, with the proviso that M is not hydrogen when R2 is CH2 CO2 M or a CHR3 CO2 M.

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New Advances in Chemical Research, May 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing theoretical assessments of solvent structures and their interactions with reaction intermediates. name: 3-(3-Hydroxyquinoxalin-2-yl)propanoic acid, We’ll be discussing some of the latest developments in chemical about CAS: 7712-28-9, name is 3-(3-Hydroxyquinoxalin-2-yl)propanoic acid. In an article,Which mentioned a new discovery about 7712-28-9

Quinoxalines belong to a class of excellent heterocyclic scaffolds owing to their wide biological properties and diverse therapeutic applications in medicinal research. They are complementary in shapes and charges to numerous biomolecules they interact with, thereby resulting in increased binding affinity. The pharmacokinetic properties of drugs bearing quinoxaline cores have shown them to be relatively easy to administer either as intramuscular solutions, oral capsules or rectal suppositories. This work deals with recent advances in the synthesis and pharmacological diversities of quinoxaline motifs which might pave ways for novel drugs development.

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A series of quinoxalinone derivatives was synthesized by the condensation of 1,2-diaminobenzene with alpha-ketoglutaric acid to yield 3-(3-oxo-3,4-dihydroquinoxalin-2-yl) propionic acid (2) and then treated with hydrazine hydrate to yield its hydrazones (3). This was further reacted with substituted aromatic aldehydes to produce final compounds (4a-r). These hydrazones derivatives were characterized by FT-IR and 1H-NMR data. All the synthesized compounds were evaluated for their antimicrobial and antiinflammatory activity.

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This chapter embodies catalyst-free synthetic protocols based on the application of ball-milling, for expedient and green synthesis of organic molecules of potential interests.

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