Zabska R, Jakóbiec T, Dobek R, Wilimowski M, Barczyńska J, Kedzierska-Goździk L, Wojewódzki W, Rutkowska M, Duś E, Szelag A
Department of Chemistry of Drug, Medical Academy, Wrocław, Poland.
Pol J Pharmacol Pharm. 1991 Jul-Aug;43(4):271-80.
Several new alpha-aminoderivatives of gamma-(p-chlorophenyl)-tetrahydrofuran-2-one were synthesized. alpha-Aminoderivatives of beta-(p-chlorobenzoyl)-propionic acid 2-13 were used as the substrates. After the reduction with NaBH4 at 10-12 degrees C and cyclization the compounds were converted into the appropriate derivatives of tetrahydrofuran-2-one 16-26. In pharmacological tests compounds 9 and 26 abolished the aggressiveness in isolated mice while compound 8 showed antiinflammatory activity.
合成了几种新的γ-（对氯苯基）-四氢呋喃-2-酮的α-氨基衍生物。使用β-（对氯苯甲酰基）-丙酸2-13的α-氨基衍生物作为底物。在10-12℃下用NaBH4还原并环化后，这些化合物转化为四氢呋喃-2-酮16-26的相应衍生物。在药理试验中，化合物9和26消除了分离小鼠的攻击性，而化合物8表现出抗炎活性。
