抗菌抗病毒化合物的研究——鱼腥草素衍生物的合成

癸酰乙醛(n-壬基-β-酮醛)为清热解毒中草药鱼腥草的有效成分之一,其亚硫酸氢钠加成物(鱼腥草素)已在临床上用为抗菌消炎药物。这一事实导致我们合成了一些癸酰乙醛衍生物,目的为寻找更有效的抗病毒、抗菌药物。其中鱼腥草素异菸腙虽无抗病毒作用,但在体内、体外皆具有显著的抗结核活性,初步临床试验亦证明有一定的治疗效果。将甲壬酮与甲酸乙酯在金属钠存在下在无水苯中反应,形成的β-酮醛与相应的氨基化合物缩合,即获得所需要的最终产物。

Studies on antimicrobial and antiviral compounds--synthesis of derivatives of decanoyl acetaldehyde (author's transl)

Decanoylacetaldehyde (n-Nonyl-β-oxo-aldehyde) is an antibacterial constituent of the Chinese medicinal plant Yü Xing Cao, Houttuynia cordata Thunb), its sodium bisulfite addition compound has been used clinically for the treatment of some infectious diseases. These facts led us to synthesize a number of derivatives of decanoylacetaldehyde in order to obtain more active antimicrobial and antiviral agents. Among them decanoylacetaldehyde bisisonicotinoyl hydrazone(6)showed marked tuberculostatic activity in vitro as well as in vivo, and exhibited definite therapeutic efficacy in primary clinical trial.The derivatives were prepared by condensing methylnonylketone with ethylformate in dry benzene in the presence of sodium, the resulting β-oxo-aldehyde was condensed with corresponding amino compounds to afford the final products.