1. Academic Validation
  2. Functionalised isocoumarins as antifungal compounds: Synthesis and biological studies

Functionalised isocoumarins as antifungal compounds: Synthesis and biological studies

  • Bioorg Med Chem Lett. 2016 Jan 1;26(1):235-9. doi: 10.1016/j.bmcl.2015.08.086.
Milena Simic 1 Nikola Paunovic 1 Ivan Boric 1 Jelena Randjelovic 1 Sandra Vojnovic 2 Jasmina Nikodinovic-Runic 2 Marina Pekmezovic 3 Vladimir Savic 4
Affiliations

Affiliations

  • 1 University of Belgrade, Faculty of Pharmacy, Department of Organic Chemistry, Vojvode Stepe 450, 11221 Belgrade, Serbia.
  • 2 University of Belgrade, Institute of Molecular Genetics and Genetic Engineering, Laboratory for Microbial Molecular Genetics and Ecology, Vojvode Stepe 444a, P.P. Box 23, 11010 Belgrade, Serbia.
  • 3 University of Belgrade, Faculty of Medicine, National Reference Medical Mycology Laboratory, Institute of Microbiology and Immunology, Dr Subotica 1, 11000 Belgrade, Serbia.
  • 4 University of Belgrade, Faculty of Pharmacy, Department of Organic Chemistry, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: vladimir.savic@pharmacy.bg.ac.rs.
Abstract

A series of novel 3-substituted isocoumarins was prepared via Pd-catalysed coupling processes and screened in vitro for Antifungal activity against Candida species. The study revealed Antifungal potential of isocoumarins possessing the azole substituents, which, in some cases, showed biological properties equal to those of clinically used voriconazole. Selected compounds were also screened against voriconazole resistant Candida krusei 6258 and a clinical isolate Candida parapsilosis CA-27. Although the activity against these targets needs to be improved further, the results emphasise additional potential of this new class of Antifungal compounds.

Keywords

Antifungal compounds; Candida species; Isocoumarin derivatives.

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