Parallel synthesis and yeast growth inhibition screening of succinamic acid libraries |
| |
Authors: | Serrano Pedro Casas Josefina Llebaria Amadeu Zucco Martine Emeric Gilbert Delgado Antonio |
| |
Affiliation: | 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. |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|