摘要
一系列衍生物从是 Trichoderma 出租车 sp 生产的抗真菌的代谢物的 trichodermin (1 ) 被综合。nov。他们的结构被 1H NMR 证实， MS 光谱。他们的抗真菌的活动在 vitro 被评估。初步的结构活动关系(SAR ) 结果显示双契约， epoxide 一半和酉旨组是主要 pharmacophore 元素， C4 位置的立体化学也起了一个关键作用，并且混合物 1e 鈥 ? g 显示了对比 1 的 Magnaporthe grisea 的更强壮的抗真菌的活动。
A series of derivatives were synthesized from trichodermin（1） which was an antifungal metabolite produced by Trichoderma taxi sp.nov.Their structures were confirmed by ~1H NMR,MS spectrum.Their antifungal activities were evaluated in vitro.The preliminary structure activity relationships（SAR） results indicated that the double bond,epoxide moiety and ester group were main pharmacophore elements,the stereochemistry of C4 position played a key role as well,and the compounds 1e-1g displayed stronger antifungal activity against Magnaporthe grisea than 1.
基金
supported by National Natural Science Foundation of China(No.30700532)
the Science and Technology Project of Zhejiang province(No.2008C02007-3)
