Pejchalová, MarcelaHavelek, RadimKrálovec, KarelRůžičková, ZdeňkaPejchal, Vladimír2018-02-272018-02-2720171054-2523https://hdl.handle.net/10195/70283A new series of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl) ethyl]-3-substituted phenyl diamides were synthesized in vitro as potential antifungal agents. Chemical structures of the synthesised compounds were substantiated by IR, H-1, C-13, F-19 nuclear magnetic resonance spectra, high resolution mass spectrometry, elemental analysis and also by X-ray diffraction. In addition, the cytotoxicity of the most active compounds was investigated against cancer cell line (Jurkat) and one type of normal lung fibroblast cells (MRC-5) by (2,3-bis-(2-methoxy4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide) tetrazolium salt reduction assay, propidium iodide flow cytometry assay and xCELLigence system allowing a label-free assessment of the cells proliferation. Compounds indicated as 11e, 11g, 11j, 11n and 11o, were the best of the series, showing minimum inhibitory concentration values of 6.25-50 mu g/mL against pathogenic strains Candida albicans HE 169, Candida tropicalis 31/HK and Candida parapsilosis p69. Moreover compounds 11e, 11g, 11j and 11o did not show any cytotoxic effect against human Jurkat and MRC-5 cells.p. 1847-1862engopen accessBenzothiazole derivativesDiamideCandidaAntifungal activityCytotoxicityBenztiazolové derivátydiamidyCandidaantifungální aktivitacytotoxicitaarticle10.1007/s00044-017-1894-x0004066020000022-s2.0-8501745750439879278