Abstract

Synthesis and investigation of antimicrobial activity of fifteen novel thiazoles containing cyclohexene moiety are presented. Among the derivatives, compounds 3a–3d, 3f, 3n, and 3o showed very strong activity against the reference Candida spp. strains with MIC = 0.015–3.91 µg/ml. The activity of these compounds is similar and even higher than the activity of nystatin used as positive control. Compounds 3d, 3f, 3n, 3o showed the highest activity with very strong effect towards most of yeasts isolated from clinical materials with MIC = 0.015–7.81 µg/ml. The cytotoxicity studies for the most active compounds showed that Candida spp. growth was inhibited at noncytotoxic concentrations for the mammalian L929 fibroblast. In addition, a good correlation was obtained between lipophilicity of compounds determined using reversed phase thin-layer chromatography and their antifungal activity.

Highlights

  • IntroductionThe incidence of Invasive Fungal Infection is increasing worldwide

  • Nowadays, the incidence of Invasive Fungal Infection is increasing worldwide

  • Candida spp. growth was inhibited at noncytotoxic concentrations for the mammalian L929 fibroblast

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Summary

Introduction

The incidence of Invasive Fungal Infection is increasing worldwide. They are mostly caused by yeasts belonging to Candida spp., especially Candida albicans, but Supplementary information The online version of this article University of Lublin, Chodźki 1, Lublin 20-093, Poland The mortality rate of bloodstream infections caused by these yeasts was reported to be as high as

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