N-(4-乙氧苯基)苯甲酰胺衍生物的合成与抗炎抗变态反应生物活性

目的以一类新药乙氧苯柳胺为先导化合物,合成取代苯甲酰苯胺衍生物并探讨其抗炎、抗变态反应生物活性。方法以取代苯甲酸为起始原料,通过氯化、缩合、电子等排、拼合和Mannich反应等制备目标化合物;用元素分析、IR1、H NMR光谱等方法确证目标化合物化学结构。结果设计并合成了10个目标化合物,其中7个化合物(LX001~LX005、LX008、LX010)尚未见文献报道;合成的目标化合物具有不同程度的抗炎、抗变态反应活性,其中LX002、LX004、LX010均具有较强的抗炎作用,LX002有较明显的抗变态反应活性。结论N(4乙氧苯基)苯甲酰胺衍生物具有较强抗炎作用和抗变态反应活性。

Synthesis and anti-inflammatory and antiall-ergic activities of N-(4-ethoxyphenyl) benzamide derivatives and analogues

Objective To design and synthesize etofesalamide derivatives and analogues, and to assay their anti-inflammatory and antiallergic activities. Methods Starting from substituted benzoic acid, the target compounds were synthesizd via chlorination, condensation, reduction and Mannich reaction etc. The effects of these compounds on ear swelling induced by xylene in mice were evaluated. The effects of the target compounds on delay-type hypersensitivity induced by 2, 4-dinitrochlorobenzene in mice were screened. Results Ten target compounds were synthesized and 7 of them were not reported in literatures. The structures of all the target compounds were confirmed by ^1H-NMR, IR and elemental analysis. Most compounds had potent anti-inflammatory and antiallergic activities. Conclusions Etofesalamide derivatives and analogues have good anti-inflammatory and antiallergic activities.