- An efficient method for the synthesis of 6, 7-bis(alkylthio- or alkylamino-substituted)quinoline-5, 8-diones via nucleophilic addition/oxidation of alkylthio and alkylamino derivatives to quinoline-5, 8-dione
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A new variety of 6, 7-bis(alkylthio- or alkylamino-substituted)quinoline-5, 8-diones were prepared by the addition of mercaptans or amino nucleophiles to quinoline-5, 8-dione after subsequent oxidation with NaIO4. The core quinoline-5, 8-dione intermediate was prepared from the oxidation of 5-quinolinol or 8-quinolinol by [bis(trifluoroacetoxy)iodo]benzene, PIFA, in the presence of water and acetonitrile as solvents. No good leaving groups were utilized to insert the alkylthio or alkylamino groups into the quinoline ring. The synthesized compounds will be tested for their anti-inflammatory, anti-bacterial and tuberculostatic inhibition activities at a later stage.{figure presented}.
- Odens, Herman H.,Silva, Trevor S.,Olusola, Candace N.,Odens, Herman H.,Howe, Victoria A.,Wijatyk, Anna I.
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- The anti-cancer, anti-inflammatory and tuberculostatic activities of a series of 6,7-substituted-5,8-quinolinequinones
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A variety of 6,7-substituted-5,8-quinolinequinones were synthesised and assessed for their anti-tumour and anti-inflammatory activities, and their ability to inhibit the growth of Mycobacterium bovis BCG. In particular, the introduction of a sulfur group
- Mulchin, Benjamin J.,Newton, Christopher G.,Baty, James W.,Grasso, Carole H.,Martin, William John,Walton, Michaela C.,Dangerfield, Emma M.,Plunkett, Catherine H.,Berridge, Michael V.,Harper, Jacquie L.,Timmer, Mattie S.M.,Stocker, Bridget L.
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experimental part
p. 3238 - 3251
(2010/07/08)
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