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[Problems to be Solved by the Invention] To provide a drug having excellent antibacterial activity against Gram-positive bacteria and Gram-negative bacteria and also being excellent in terms of safety. [Means for Solving the Problems] A compound represented by the following formula (I) or a salt thereof: wherein R represents a hydrogen atom, a hydroxy group, or a halogen atom m represents an integer 0, 1, or 2, n represents an integer 0 or 1 Ar1 represents a bicyclic heterocyclic group represented by the following formula: wherein Aa represents a nitrogen atom or C-Ra, Ab represents a nitrogen atom or C-Rb, and Ac represents a nitrogen atom or C-Rc, Ra, Rb, and Rc independently represent a hydrogen atom or an alkyl group containing 1 to 6 carbon atoms, R1 and R2 independently represent a hydrogen atom, an alkoxy group containing 1 to 6 carbon atoms, a halogenoalkoxy group containing 1 to 6 carbon atoms, a halogen atom, or a cyano group, Ar2 represents a bicyclic heterocyclic group represented by the following formulae:

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Quinoxalinones and dihydroquinoxalinones having inhibitory activity on RSV replication and having the formula (I) including addition salts, and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

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The title reactions give 1-hydroxy-4-methylquinoxaline-2,3-diones (4) together with a variety of mono- and bi-cyclic byproducts. All of these may result from a common intermediate, viz. a 1-hydroxy-4-methyl-3,4-dihydro-1H-2,1,4-benzoxadiazine-3-carboxylate ester (18).

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Hepatitis C Virus Inhibitors

Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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Hepatitis C virus inhibitors

Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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Improving Hg-triggered gelation via structural modifications

The relationship between chemical structure and gelation ability was examined for a series of nine Hg-containing compounds. Both solid-state properties (dissolution enthalpies/entropies and packing structure) and gel properties (strength, morphology, cation selectivity, and anion tolerance) were examined. Overall, the results reveal a complex relationship between chemical structure and properties. The remediation potential of these Hg-triggered gelations was also investigated, revealing that >98% of the Hg2+ in water can be removed through gel formation.

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Electrochemically C-H/S-H Oxidative Cross-Coupling between Quinoxalin-2(1 H)-ones and Thiols for the Synthesis of 3-Thioquinoxalinones

An electrochemical method for the C(sp2)-H thioetherification of quinoxalin-2(1H)-ones with primary, secondary, and tertiary thiols has been reported. Various quinoxalin-2(1H)-ones underwent this thioetherification smoothly under metal- A nd chemical oxidant-free conditions, affording 3-alkylthiol-substituted quinoxalin-2(1H)-ones in moderate to good yields.

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Electrochemical Dehydrogenative Cross-Coupling of Quinoxalin-2(1H)-ones with Amines for the Synthesis of 3-Aminoquinoxalinones

An efficient protocol for the synthesis of 3-aminoquinoxalinones via the electrochemical dehydrogenative C-3 amination of quinoxalin-2(1H)-ones was developed. With aliphatic amines and azoles as the nitrogen sources, a series of 3-aminoquinoxalinones was obtained in up to 99% yield. This direct electrolytic method avoids the use of transition metals and external oxidants, and represents an appealing alternative for the synthesis of 3-aminoquinoxalinones. (Figure presented.).

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Iodine-Catalyzed C-N Bond Formation: Synthesis of 3-Aminoquinoxalinones under Ambient Conditions

A metal-free cross-dehydrogenative coupling between quinoxalinones (sp2 C-H) and amines (N-H) in the presence of catalytic iodine is reported. The reaction yields 3-aminoquinoxalinones in moderate to high yields under ambient conditions in dioxane as solvent and aqueous tert-butyl hydroperoxide (TBHP) as the terminal oxidant. The reaction is highly versatile and exhibits good functional group tolerance with a range of primary and secondary amines. It provides a practical access to pharmaceutically active 3-aminoquinoxalinone derivatives. Preliminary mechanistic studies reveal in situ iodination of the amine as the putative mode of activation.

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Convenient synthetic method for 3-(3-substituted indol-2-yl)quinoxalin-2- ones as VEGF inhibitor

It has already been reported that 3-(indol-2-yl)quinoxalin-2-ones 1)? have a potent inhibitory effect on the growth of tumor cells based on anti-angiogenesis activity. We have also carried out a structure-activity relationship (SAR) study of 3-(indol-2-yl)quinoxalin-2-ones, which showed a potent inhibitory activity toward the vascular endothelial growth factor (VEGF)-induced proliferation of human mesangial cells and the VEGF-induced auto-phosphorylation of human umbilical vein endothelial cells.2) Moreover, one of these compounds has a potent medicinal effect based on anti-angiogenic action, by oral administration2) (Chart 1, 9). However, since the existing synthetic methods1) for the preparation of 3-(indol-2-yl)quinoxalin-2-ones consist of multiple steps some of which require strict anhydrous conditions, a convenient and simple synthetic method in place of the existing method is desirable. As a result of the investigations into the synthetic procedures, 3-(3-substituted indol-2-yl)quinoxalin-2-ones can be easily prepared by the condensation of 3-substituted indoles with quinoxalin-2-ones in the presence of trifluoroacetic acid (TFA). Herein, we report the examination of these reaction conditions and the application of this new synthetic method to the synthesis of the derivatives as VEGF inhibitors.

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