Parallel Synthesis and Yeast Growth Inhibition Screening of Succinamic Acid Libraries

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• 作者：Pedro Serrano ; Josefina Casas ; Amadeu Llebaria ; Martine Zucco ; Gilbert Emeric ; Antonio Delgado
• 刊名：Journal of Combinatorial Chemistry
• 出版年：2007
• 出版时间：July 2007
• 年：2007
• 卷：9
• 期：4
• 页码：635 - 643
• 全文大小：241K
• 年卷期：v.9,no.4(July 2007)
• ISSN：1520-4774

文摘

Libraries of succinamic acid derivatives resulting from the condensation of a series of succinic acid derivativeswith amines are reported as putative khafrefungin analogues. A total of 480 compounds derived from theinitial condensation of 8 scaffolds with 60 different amines have been synthesized using automated technologywith the help of scavenger resins. A simple acetate hydrolysis of five of the above sublibraries affordedadditional 300 compounds for a total of 780 compounds. Around 55% of the library members showedpurities higher than 70% (HPLC-ELS-MS) thus proving the generality of this approach. Results on growthinhibition of the yeast Saccharomyces cerevisiae in the presence of selected library members are also reportedas a preliminary evaluation of the antifungal activity.