Serrano Pedro, Casas Josefina, Llebaria Amadeu, Zucco Martine, Emeric Gilbert, Delgado Antonio
Research Unit on Bioactive Molecules, Departament de Química Orgànica Biologica, Institut d'Investigacions Químiques i Ambientals de Barcelona, Jordi Girona 18-26, 08034 Barcelona, Spain.
J Comb Chem. 2007 Jul-Aug;9(4):635-43. doi: 10.1021/cc070026n. Epub 2007 May 31.
Libraries of succinamic acid derivatives resulting from the condensation of a series of succinic acid derivatives with amines are reported as putative khafrefungin analogues. A total of 480 compounds derived from the initial condensation of 8 scaffolds with 60 different amines have been synthesized using automated technology with the help of scavenger resins. A simple acetate hydrolysis of five of the above sublibraries afforded additional 300 compounds for a total of 780 compounds. Around 55% of the library members showed purities higher than 70% (HPLC-ELS-MS) thus proving the generality of this approach. Results on growth inhibition of the yeast Saccharomyces cerevisiae in the presence of selected library members are also reported as a preliminary evaluation of the antifungal activity.
据报道，一系列琥珀酸衍生物与胺缩合得到的琥珀酰胺酸衍生物库是假定的卡弗芬净类似物。借助清除树脂，利用自动化技术合成了总共480种由8种支架与60种不同胺初始缩合得到的化合物。上述五个子库进行简单的乙酸盐水解又得到了300种化合物，总计780种化合物。约55%的库成员纯度高于70%（HPLC-ELS-MS），从而证明了该方法的通用性。作为抗真菌活性的初步评估，还报道了在选定库成员存在下对酿酒酵母生长抑制的结果。
