摘要
为了寻找新的高活性抑菌化合物,以天名精内酯酮为起始原料,先用硼氢化钠选择性地对其4-位羰基进行还原,得到天名精内酯醇,并以此为原料设计合成了6个未见报道的天名精内酯酮酯类衍生物(a^f),其结构经过核磁共振谱、红外光谱、高分辨质谱等方法确证。采用悬滴法测定了合成衍生物对黄瓜炭疽病菌孢子萌发的抑制作用,结果表明,目标化合物对黄瓜炭疽病菌有一定的抑菌活性,其中异丁酸酯(f)衍生物活性最好,比天名精内酯酮和天名精内酯醇分别提高了3倍和10倍,烯丙酸酯(d)衍生物活性比天名精内酯醇提高了1倍左右,正丁酸酯(e)衍生物的活性和天名精内酯醇相当,其余衍生物的活性则比天名精内酯醇有所下降。4-位基团的改变对衍生物的抑菌活性有较大的影响。
The research is to find new compounds with antifungal activity.Carabrone was deoxidized to be carabrol and six new carabrone ester analogues were synthesized using NaBH4 as catalyst.Their structures were confirmed by NMR,IR,HRMS spectral data.Bioassay results indicated that isobutyl ester analogue exhibited three folds higher antifugal activity than carabrone and ten folds than carabrol against Colletotrichum lagenarium,The allyl ester analogue expressed one fold higher antifugal activity than carabrol,The butyl ester analogue expressed comparative antifugal activity to carabrol,and the other ester analogues showed lower antifugal activity than carabrol.The change of bit-4 has an important impact on the antifungal activity of the analogues.
出处
《西北农业学报》
CAS
CSCD
北大核心
2009年第2期283-286,共4页
Acta Agriculturae Boreali-occidentalis Sinica
基金
陕西省自然科学基金(14210123)
西北农林科技大学校科研基金(06ZR019)
