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Parallel synthesis and yeast growth inhibition screening of succinamic acid libraries

Academic Article
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Overview

authors

  • Serrano-Navarro, Pedro
  • Casas, J.
  • Llebaria, A.
  • Zucco, M.
  • Emeric, G.
  • Delgado, A.

publication date

  • July 2007

journal

  • Journal of Combinatorial Chemistry  Journal

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.

subject areas

  • Acetylation
  • Amines
  • Anhydrides
  • Animals
  • Antifungal Agents
  • Databases, Factual
  • Drug Evaluation, Preclinical
  • Glycolipids
  • Molecular Structure
  • Saccharomyces cerevisiae
  • Sphingolipids
  • Succinic Acid
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Identity

International Standard Serial Number (ISSN)

  • 1520-4766

Digital Object Identifier (DOI)

  • 10.1021/cc070026n

PubMed ID

  • 17536867
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Additional Document Info

start page

  • 635

end page

  • 643

volume

  • 9

issue

  • 4

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