Geronikaki A A, Hadjipavlou-Litina D J, Tzaki M
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Greece.
Arzneimittelforschung. 2000 Mar;50(3):266-71. doi: 10.1055/s-0031-1300197.
Eight thienyl and 1,3-thiazolyl-aminoketones were synthesised and tested as anti-inflammatory agents. pKa and log P were theoretically calculated. The compounds were tested for antioxidant activity, as hydroxyl radical scavengers, as superoxide anion scavengers and for their ability to interact with 1,1-diphenyl-2-picryl hydrazyl stable free radical (DPPH). The effects of the synthesised compounds on inflammation were studied using the carrageenan induced mice paw oedema model. Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesised compounds.
合成了八种噻吩基和1,3 - 噻唑基氨基酮，并作为抗炎剂进行了测试。从理论上计算了pKa和log P值。测试了这些化合物作为羟基自由基清除剂、超氧阴离子清除剂的抗氧化活性以及它们与1,1 - 二苯基 - 2 - 苦基肼基稳定自由基（DPPH）相互作用的能力。使用角叉菜胶诱导的小鼠爪肿胀模型研究了合成化合物对炎症的影响。抗炎和抗氧化活性均取决于合成化合物的某些结构特征。
