Merck

New small-size peptides possessing antifungal activity.

Bioorganic & medicinal chemistry (2009-12-05)
Francisco M Garibotto, Adriana D Garro, Marcelo F Masman, Ana M Rodríguez, Paul G M Luiten, Marcela Raimondi, Susana A Zacchino, Csaba Somlai, Botond Penke, Ricardo D Enriz
ABSTRACT

The synthesis, in vitro evaluation, and conformational study of a new series of small-size peptides acting as antifungal agents are reported. In a first step of our study we performed a conformational analysis using Molecular Mechanics calculations. The electronic study was carried out using Molecular electrostatic potentials (MEPs) obtained from RHF/6-31G calculations. On the basis of the theoretical predictions three small-size peptides, RQWKKWWQWRR-NH(2), RQIRRWWQWRR-NH(2), and RQIRRWWQW-NH(2) were synthesized and tested. These peptides displayed a significant antifungal activity against human pathogenic strains including Candida albicans and Cryptococcus neoformans. Our experimental and theoretical results allow the identification of a topographical template which can serve as a guide for the design of new compounds with antifungal properties for potential therapeutic applications against these pathogenic fungi.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Ketoconazole, 99.0-101.0% (EP, titration)