New small-size antifungal peptides: Design, synthesis and antifungal activity

Adriana D. Garro, Francisco M. Garibotto, Ana M. Rodriguez, Marcela Raimondi, Susana A. Zacchino, Andras Perczel, Csaba Somlai, Botond Penke, Ricardo D. Enriz

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

The synthesis, in vitro evaluation and conformational study of small-size peptides acting as antifungal agents are reported. These peptides displayed antifungal activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans. Among the peptides reported here, RQWRRWWQR-NH2 exhibited the strongest activity against Cryptococcus neoformans. Our results allowed us to reduce in size these bioactive peptides from 16 to 11 and to 9 amino acid residues in total. Despite their reduction, they still maintained and even enhanced the antifungal activity detected for penetratin. A conformational and electronic structure analysis on these peptides was also performed by using molecular mechanics calculations in conjunction with Molecular Electrostatic Potentials (MEP) maps.

Original languageEnglish
Pages (from-to)562-567
Number of pages6
JournalLetters in Drug Design and Discovery
Volume8
Issue number6
DOIs
Publication statusPublished - Jul 2011

Keywords

  • Antifungals
  • Conformational and Electronic Study
  • Molecular Electrostatic Potentials
  • Peptides

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery

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