2-芳香酰氨基蝶啶类化合物的合成及其对NOS活性的调节作用

Synthesis and NOS regulative effect of 2-arylacylated amino pteridines

目的：合成新的2-芳香酰氨基蝶啶类化合物，寻找具有NOS调节功能的化合物。方法：以2-氨基-4-二乙胺基-6-芳基蝶啶为母核，对其2位氨基进行芳香酰化并测定目标化合物对iNOS活性的影响。结果与结论：合成了16个2位氨基芳香酰化的蝶啶类化合物（P-1 - P-16），所有化合物均未见文献报道，其结构经IR、UV、^1H NMR、MS和元素分析鉴定。初步药理实验表明：母核（5a-e）2位氨基芳香酰化后，对iNOS活性具有抑制或激活作用，其中P-2、P-7和P-9在-定浓度下可以替代BH4的功能，它们的最小有效浓度分别达到83．32μmol／L，81．98μmol／L和79.70μmol／L。

Aim：To synthesize a series of 2-arylacylated amino pteridine compounds in order to find the NOS regulatois. Mothods：2-amino of 2-amino-4-dimethylamino-4-arylpteridines were modified by arylaeylation and their effects on iNOS activity were evalued. Results and Conclusion： A series of 2-arylacylated amino pteridine compounds（P-1 - P-16） have been synthesized and their structures were confirmed by IR, UV, ^1H NMR, MS and EA. Pharmacological evaluation showed that arylacylation of 2-amino of mother compounds（5a - c）could lead to inhibition or activation of iNOS activity. Three compounds,P-2,P-7 and P-9 on the setting concentrations had the same effect on iNOS as BH4 and their minimum effective concentrations were 83.32 μmol/L, 81.98 μmol/L and 79.70 μmol/L respectively.