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Parallel synthesis and yeast growth inhibition screening of succinamic acid libraries

AuthorsSerrano, Pedro; Casas Brugulat, Josefina; Llebaria, Amadeu; Zucco, Martine; Emeric, Gilbert; Delgado Cirilo, Antonio
KeywordsYeast growth inhibition
Succinamic acid libraries
Antifungal activity
Issue Date31-May-2007
PublisherAmerican Chemical Society
CitationJournal of Combinatorial Chemistry 9(4): 635-643 (2007)
AbstractLibraries 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.
Description9 pages, 9 figuras.-- PMID: 17536867 [PubMed].
Publisher version (URL)http://dx.doi.org/10.1021/cc070026n
Appears in Collections:(IQAC) Artículos
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