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The quinoxaline moiety in antitumor quinoxaline antibiotics cleaved double stranded DNA at the 5? side guanine of the 5?-GG-3? site upon irradiation with UV light with a long wavelength and without any additive. The quinoxaline-carbohydrate hybrid system was very effective for the DNA cleavage. Furthermore, the quinoxaline-carbohydrate hybrids exhibited strong and selective cytotoxicity against cancer cells with photoirradiation.

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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

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Quinoxaline, found in antitumor quinoxaline antibiotics, was found to cleave double stranded DNA at the 5? side guanine of 5?-GG-3? site on irradiation with long wavelength UV light without any additive; furthermore, a bis(quinoxaline-carbohydrate) hybrid system was very effective for DNA cleavage.

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An exceptional oxidizing behavior of sodium cyanoborohydride is observed where electron-withdrawing heterocyclic aldehydes are directly converted to their corresponding esters on treatment of sodium cyanoborohydride in methanol. The spectral analysis and single-crystal structure confirm the formation of esters. Taylor & Francis Group, LLC.

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Azole-N-acetonitrile derivatives were utilized as synthons for an ambident carbonyl moiety via a strategy relying upon sequential base-mediated S NAr substitution of a 2-halo heterocycle, in situ oxidation, and amine displacement. This strategy allows prompt and efficient synthesis of N-containing heteroaryl amides directly from the corresponding halides via a one-pot process.

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The present invention is directed to tetrahydroquinoxaline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer’s disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

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A series of pyrazine and quinoxaline derivatives have been synthesized, and their activity against M. tuberculosis (Mtb) and Mycobacterium avium (MAC) are reported. The 4-acetoxy-benzyl ester of pyrazinoic acid and 4?-acetoxybenzyl 2-quinoxalinecarboxylate showed excellent activity against Mtb (MIC ranges of less than 1-6.25 mug/mL) but only modest activity against MAC (MICs of 4-32 mug/mL).

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A catalyst made in situ from the (cyclooctadiene)iridium chloride dimer, [Ir(COD)Cl]2, and the monodentate phosphoramidite ligand (S)-PipPhos was used in the enantioselective hydrogenation of 2- and 2,6-substituted quinoxalines. In the presence of piperidine hydrochloride as additive full conversions and enantioselectivities of up to 96% are obtained.

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Benzofuroxan (1) reacts with phosphorus ylide 2 to give benzimidazole derivatives 8 and 10, whereas reaction of 1 with ylide 12 furnishes quinoxaline 17 via an initial Wittig-type reaction.Similarly the reaction between the furoxano<3,4-b>quinoxalines 19a or 19b and the ylide 2 yielded compounds 22a and 22b, respectively.In these reactions as well as in the reactions of the above furoxans with other phosphorus ylides, a significant deoxygenation of the furoxans to furazans with subsequent oxidation of the ylides is generally observed.

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For the first time, the asymmetric hydrogenation of quinoxaline-2-carboxylates was performed successfully. The best catalysts are based on iridium complexes modified by chiral phosphorous ligands. Accelerated examination of ligands and catalysts has been undertaken by using a Chemspeed workstation, which enables carrying out, in parallel, eight independent catalytic reactions at the laboratory scale. Tetrahydroquinoxaline-2-carboxylates could be obtained with high yields and up to 74% ee.

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