Antifungal Activity of a Library of Cyclitols and Related Compounds

Ana      Bellomo; Ana      Bertucci; Victoria   de la   Sovera; Gonzalo      Carrau; Marcela      Raimondi; Susana      Zacchino; Helio   A.   Stefani; David      Gonzalez

Abstract

The antifungal activity of a library of 32 cyclitols and derivatives, including 6 previously unreported cyclitol amino acid conjugates, was studied against the clinically important yeasts Candida albicans, Candida tropicalis and Cryptococcus neoformans along with Saccharomyces cerevisiae. Bioautography followed by standardized microbroth dilution methods were used and allowed to identify an azidoinositol glycoside (11) and an azidoconduritol linked to an aromatic aldehyde (18) as promising compounds. The results suggest the relevance of exploring synthetic cyclitolic structures as potential antifungal leaders.

Keywords: Inositols, Conduritols, Chemoenzymatic, Antifungal activity, Bioautography, Amino acid conjugates.

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Letters in Drug Design & Discovery

Title:Antifungal Activity of a Library of Cyclitols and Related Compounds

Volume: 11 Issue: 1

Author(s): Ana Bellomo, Ana Bertucci, Victoria de la Sovera, Gonzalo Carrau, Marcela Raimondi, Susana Zacchino, Helio A. Stefani and David Gonzalez

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Keywords: Inositols, Conduritols, Chemoenzymatic, Antifungal activity, Bioautography, Amino acid conjugates.

Abstract: The antifungal activity of a library of 32 cyclitols and derivatives, including 6 previously unreported cyclitol amino acid conjugates, was studied against the clinically important yeasts Candida albicans, Candida tropicalis and Cryptococcus neoformans along with Saccharomyces cerevisiae. Bioautography followed by standardized microbroth dilution methods were used and allowed to identify an azidoinositol glycoside (11) and an azidoconduritol linked to an aromatic aldehyde (18) as promising compounds. The results suggest the relevance of exploring synthetic cyclitolic structures as potential antifungal leaders.

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Bellomo Ana, Bertucci Ana, Sovera de la Victoria, Carrau Gonzalo, Raimondi Marcela, Zacchino Susana, Stefani A. Helio and Gonzalez David, Antifungal Activity of a Library of Cyclitols and Related Compounds, Letters in Drug Design & Discovery 2014; 11 (1) . https://dx.doi.org/10.2174/15701808113109990036