摘要
本文选择氯苯扎利二钠（ＣＣＡ）为先导化合物，设计并合成了Ｎ－取代苯基邻氨基苯甲酸衍生物，并经ＩＲ，ＭＳ，元素分析等证实。合成中发现Ｕｌｌｍａｎｎ反应有竞争性的反应产物，初步考察了反应性能；研究了目标化合物的免疫促进作用，发现其中ＳＱ１（１μｍｏｌ／Ｌ）和ＳＱ４（０．０１μｍｏｌ／Ｌ）对ＣｏｎＡ诱导的小鼠脾淋巴细胞的增殖反应均有促进作用；其强度与ＣＣＡ相当；ＳＱ４（１μｍｏｌ／Ｌ）并能促进ＣｏｎＡ诱导小鼠淋巴细胞产生白细胞介素（ＩＬ－２），其作用较ＣＣＡ强（Ｐ＜０．０１），但其ＬＤ５０为１０７．９ｍｇ／ｋｇ（ｉｐ小鼠），明显大于ＣＣＡ，提示ＳＱ４的安全范围较狭。
It was reported that some N-substituted phenyl anthranilic acid derivatives were prepared and their immunostimulation effects were observed.Lobenzarit(CCA)was selected as the lead compound SQ1(1μmol/L)and SQ4(0.01μmol/L)obviously enhanced Con A-induced proliferatuve responses of splenocytes from mice.SQ4(1μmol/L) also increased ConA-induced interleukin-2(IL-2)of CCA.However,the ip LD50 of a single dose of SQ4 was found to be 107.9 mg/kg.These results suggested that the margin of safety of SQ4 was narrower than that of CCA.
出处
《中国药物化学杂志》
CAS
CSCD
1994年第4期235-239,244,共6页
Chinese Journal of Medicinal Chemistry
关键词
N-取代苯基
邻氨基苯甲酸
衍生物
消炎镇痛药
N-substituted phenyl derivatives
Immunostimulation effect
Proliferation of lymphocytes
Interleukin-2
