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以脱氢枞酸为原料,依次通过酯化反应、乙酰化反应和四组分串联反应合成了11个新型含吡啶环的脱氢枞酸衍生物(化合物4a~4k)。利用FT-IR、1HNMR和ESI-MS对上述化合物进行了结构表征。采用四甲基偶氮唑蓝比色法(MTT比色法)测试了上述化合物对人体单纯疱疹病毒I型(HSV-1)的体外抗病毒活性。结果表明,该系列衍生物具有一定的抗病毒活性,对HSV-1的半数有效浓度EC50在10~25μmol/m L之间,化合物4g的抗病毒活性最强,其EC50为12.1μmol/m L。初步构效关系分析表明,将吡啶环结构引入到脱氢枞酸骨架中可以提高衍生物的抗病毒活性。
Eleven new dehydroabietic acid derivatives containing pyridine ring (compounds 4a ~ 4k) were synthesized by dehydroabietic acid as the raw material, followed by esterification, acetylation and four - component series reactions. The above compounds were characterized by FT-IR, 1HNMR and ESI-MS. In vitro anti-viral activity of the above compounds against human herpes simplex virus type 1 (HSV-1) was tested using tetramethylzirconyl blue colorimetry (MTT colorimetric method). The results showed that the derivatives of this series had certain antiviral activity. The EC50 of HSV-1 was between 10 ~ 25μmol / m L and the anti-virus activity of compound 4g was the strongest with an EC50 of 12.1μmol / m L . The preliminary structure-activity relationship analysis showed that the introduction of the pyridine ring structure into the dehydroabietic acid backbone can increase the antiviral activity of the derivative.