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在12%乙腈-0.02mol/L磷酸盐缓冲溶液,pH7.4,10℃条件下,以紫外检测方法测定了22个硫乙内酰脲衍生物[(±)5-氨基酸残基-3-邻取代苯基-2-硫代-乙内酰脲(o-取代-PTH-AA)]的水解开环速率与水解半衰期。初步构效关系研究表明,镇痛活性较好的化合物应具有较大的水溶性、较快的水解速率及与脑啡肽酶最佳结合的化学结构。
Twenty-two thiohydantoin derivatives, [(±) 5-amino acid residue-3- O-substituted phenyl-2-thio-hydantoin (o-substituted-PTH-AA)]. Preliminary structure-activity relationship studies have shown that compounds with better analgesic activity should have a greater water-soluble, faster hydrolysis rate and the best combination with enkephalin chemical structure.