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The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y 1 receptor activity.

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Reference£º
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N149 | ChemSpider

 

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New synthesis of diazepino[3,2,1-ij]quinoline and pyrido[1,2,3-de] quinoxalines via addition-elimination followed by cycloacylation

This paper describes a convenient and efficient synthesis of new fused tricyclic diazepino[3,2,1-ij]quinolines and substituted pyrido[1,2,3-de] quinoxalines. o-Phenylenediamines are transformed in the tricycle nucleus in only a few-step synthetic sequence to produce ethyl 2,8-dioxo-1,2,3,4- tetrahydro-8H [1,4]diazepino[3,2,1-ij]quinoline-7-carboxylate, ethyl 8-oxo-1,2,3,4-tetrahydro-8H-[1,4]diazepino[3,2,1-ij]quinoline-7-carboxylate and ethyl 2,7-dioxo-2,3-dihydro-1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxylate. The method is economical and simple to perform.

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Iodine-Catalyzed Oxidative Aromatization: A Metal-Free Concise Approach to meta-Substituted Phenols from Cyclohex-2-enones

A metal-free approach to meta-substituted phenols from cyclohex-2-enone via catalytic oxidative aromatization has been developed. The transformations are initiated with a catalytic amount of molecular iodine as the direct oxidant, while dimethyl sulfoxide is employed as the terminal oxidant. This practical approach is capable of avoiding the use of metal promoters and costly reagents, the lengthy synthesis, and overoxidation of products, and thus facilitates the efficient construction of meta-substituted phenol derivatives from inexpensive commercial chemicals under mild conditions. The synthetic utility of this approach is evident in the de novo syntheses of two bioactive molecules with good total yields, in which easily available chemicals were employed, protective groups were not utilized, and no unwanted carbon atoms were removed in each step. (Figure presented.).

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Quinoxaline – Wikipedia,
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Design, molecular docking and synthesis of some novel 4-acetyl-1-substituted-3,4-dihydroquinoxalin-2(1H)-one derivatives for anticonvulsant evaluation as AMPA-receptor antagonists

A new series of 4-acetyl-1-substituted-3,4-dihydroquinoxalin-2(1H)-ones (2?13) were designed and synthesized in order to evaluate their AMPA-receptor antagonism as a potential mode of anticonvulsant activity. The structure of the synthesized compounds was confirmed by elemental analysis and spectral data (IR, 1HNMR, 13CNMR and Mass). The molecular design was performed for all the synthesized compounds to predict their binding affinity to AMPA-receptor in order to rationalize their anticonvulsant activity in a qualitative way. The data obtained from the molecular modeling was strongly correlated with that obtained from the biological screening which revealed that; compounds 12b, 13, 12a and 7a showed the highest binding affinities toward AMPA-receptor and also showed the highest anticonvulsant activities against pentylenetetrazole -induced seizures in experimental mice. The relative potencies of these compounds were 1.66, 1.66, 1.61 and 0.82 respectively, in comparing to diazepam.

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Substituted pyrroloquinoxalinones and diones

Substituted pyrroloquinoxalinones and diones, useful as anti-inflammatory and anti-thrombotic agents.

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Quinoxaline – Wikipedia,
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Heterocyclic derivatives

The invention concerns a heterocyclic derivative of the formula I wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;, X¹ is oxy, thio, sulphinyl, sulphonyl or imino;, Ar is phenylene which may optionally bear one or two substituents or, Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;, R¹ is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; and, R² and R³ together form a group of the formula -A²-X²-A³- which, together with the carbon atom to which A² and A³ are attached, defines a ring having 4 to 7 ring atoms, wherein A² and A³, which may be the same or different, each is (1-4C)alkylene and X² is oxy, thio, sulphinyl, sulphonyl or imino;, or a pharmaceutically-acceptable salt thereof. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

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Quinoxaline – Wikipedia,
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Studies on antiamoebic compounds: Part II – Antiamoebic activity of dichloroacetamides of 1,5-benzodiazepinones and tetrahydroquinoxalinones

Several dichloroacetamides of 1,5-benzodiazepinones and of tetrahydroquinoxalinones have been synthesised and screened for luminal antiamoebic activity.Only compound 1 exhibit notable activity in this series against luminal amoebiasis.

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A novel application of heterocyclic compounds for biosensors based on NAD, FAD, and PQQ dependent oxidoreductases

Various five-, six-, and seven-membered heterocyclic compounds containing two nitrogen atoms as well as quinoid substances were synthesized and investigated. Electrochemical oxidation-polymerization of these heterocycles on carbon and platinum electrodes was performed in aqueous medium. Electrochemically pre-treated carbon electrodes modified with these heterocyclic compounds and were used for the electro-catalytic oxidation of NADH and for the design of mediated glucose biosensors.

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Heteroaryl amide derivatives and their use as TGR5 agonist application (by machine translation)

The invention belongs to the field of medical technology, in particular of formula (I) indicated by the heteroaryl amide TGR5 agonist compound, its pharmaceutically acceptable salt, ester, its stereoisomers or prodrugs, wherein R1 , R2 , R3 , R4 , R5 , R6 , R7 , R8 , R9 , R10 , R11 , X1 , X2 , X3 And Y as defined in the specification; the invention also relates to methods of preparing such compounds, pharmaceutical formulations, pharmaceutical composition and use of these compounds in treating and/or preventing and TGR5 active regulation in the use of the related diseases. (by machine translation)

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Quinoxaline – Wikipedia,
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A Combination of Visible-Light Organophotoredox Catalysis and Asymmetric Organocatalysis for the Enantioselective Mannich Reaction of Dihydroquinoxalinones with Ketones

An enantioselective photooxidative Mannich reaction of dihydroquinoxalinones with ketones by the merger of organophotoredox and asymmetric organocatalysis is described. This protocol features very mild reaction conditions using simple and cheap catalysts (Eosin Y and (S)-Proline) for the synthesis of chiral quinoxaline derivatives with good to high yields (up to 94%) and excellent enantioselectivities (up to 99% ee).

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N184 | ChemSpider