Ismaili Lhassane, Nadaradjane Arulraj, Nicod Laurence, Guyon Catherine, Xicluna Alain, Robert Jean-François, Refouvelet Bernard
Equipe Sciences séparatives et Biopharmaceutique (2SB), Laboratoire de chimie thérapeutique, Faculté de Medecine et de Pharmacie, 4, place Saint Jacques - 25030 Besançon Cedex, France.
Eur J Med Chem. 2008 Jun;43(6):1270-5. doi: 10.1016/j.ejmech.2007.07.012. Epub 2007 Aug 2.
New hexahydropyrimido[5,4-c]quinoline-2,5-diones and 2-thioxohexahydropyrimido[5,4-c]quinoline-5-ones were prepared in two steps from ethyl 4-phenyl-6-methyl-2-oxo tetrahydropyrimidine-5-carboxylates or 4-phenyl-6-methyl-2-thioxotetrahydropyrimidine-5-carboxylates, previously prepared by Biginelli reaction using appropriate aldehyde, urea derivatives and ethyl acetoacetate. Their antioxidant properties were evaluated by two methods: scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals and scavenging effect on hydroxyl radicals. The results show that the compounds containing thiourea moiety have better activity.
新型六氢嘧啶并[5,4-c]喹啉-2,5-二酮和2-硫代六氢嘧啶并[5,4-c]喹啉-5-酮由4-苯基-6-甲基-2-氧代四氢嘧啶-5-羧酸乙酯或4-苯基-6-甲基-2-硫代四氢嘧啶-5-羧酸乙酯分两步制备，上述乙酯先前通过使用适当醛、尿素衍生物和乙酰乙酸乙酯的Biginelli反应制备。通过两种方法评估了它们的抗氧化性能：对2,2-二苯基-1-苦基肼基（DPPH）自由基的清除作用和对羟基自由基的清除作用。结果表明，含有硫脲部分的化合物具有更好的活性。
