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在已知某些硫乙内酰脲(PTH-AA)的镇痛作用与脑啡肽酶抑制关系的认识基础上,以DL-氨基酸和含氟取代硫代异氰酸苯酯为原料,合成了17个硫乙内酰脲衍生物:(±)5-氨基酸残基-3-取代苯基-2-硫代-乙内酰脲(简称取代-PTH-AA)。经小白鼠热板试验发现,3-CF_3-PTH-Ala(YZ_1)(100 mg/kg,ip)、3-Cl-4-F-PTH-Ala(YZ_8)(100 mg/kg,ip)和3-Cl-4-F-PTH-Arg-HCl(YZ_(15)(100 mg/kg,ip)具有较强的镇痛作用,与盐酸吗啡(40 mg/kg,ip)相当。
Based on the understanding of the relationship between the analgesic effect of some thiohydantoin (PTH-AA) and the inhibition of neprilysin, DL-amino acids and fluorine-substituted phenylthioisocyanates were used as starting materials to synthesize Seventeen thiohydantoin derivatives: (±) 5-amino acid residue 3-substituted phenyl-2-thio-hydantoin (abbreviated as -PTH-AA). The results of the hot plate test in mice showed that 3-CF_3-PTH-Ala (100 mg / kg, ip) and 3-Cl-4-F-PTH- 3-Cl-4-F-PTH-Arg-HCl (YZ_ (15) (100 mg / kg, ip) had a strong analgesic effect comparable to morphine hydrochloride (40 mg / kg, ip)