Piras S, Loriga M, Paglietti G, Demontis M P, Varoni M V, Fattaccio M C, Anania V
Istituto di Chimica Farmaceutica e Tossicologica dell'Università di Sassari, Muroni.
Farmaco. 1996 Aug-Sep;51(8-9):569-77.
Thirty compounds possessing quinoxaline structure bearing either substituted arylmethylmercapto-, arylmethylsulfinyl group or a piperazinyl moiety in position 2 were prepared in order to evaluate an antiulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole and ranitidine at the dose of 100 mg/kg after oral administration. Among the compounds of the first group one third showed a moderate activity being about half potent as omeprazole whereas in the second group compound 5b exibited an activity superior to that of ranitidine accompanied with the lowest incidence of lesions and mortality and another compound (5i) was equiactive as ranitidine.
制备了30种具有喹喔啉结构的化合物，这些化合物在2位带有取代的芳基甲基巯基、芳基甲基亚磺酰基或哌嗪基部分，以便与奥美拉唑和雷尼替丁在口服给药100mg/kg剂量后比较，评估其在大鼠幽门结扎模型中的抗溃疡和胃保护活性。在第一组化合物中，三分之一表现出中等活性，约为奥美拉唑活性的一半；而在第二组中，化合物5b表现出优于雷尼替丁的活性，同时病变和死亡率发生率最低，另一种化合物（5i）与雷尼替丁活性相当。
