Publication detail

Novel Derivatives of Substituted 6-Fluorobenzothiazole Salicylic Amides: Synthesis, Antibacterial Activity and Cytotoxicity.

Authors: Pejchalová Marcela | Královec Karel | Odehnalová Hana | Jadrná Simona | Pejchal Vladimír

Year: 2019

Type of publication: ostatní - přednáška nebo poster

Page from-to: nestránkováno

Titles:

Language	Name	Abstract	Keywords
eng	Novel Derivatives of Substituted 6-Fluorobenzothiazole Salicylic Amides: Synthesis, Antibacterial Activity and Cytotoxicity.	The starting compound (R)-1-(6-fluorobenzothiazol-2-yl)-3-methylbutan-1-amine was prepared as the corresponding hydrochloride. A series of novel 6-fluorobenzothiazole salicylicamides was synthesized by condensation reaction. The structures of prepared salicylic amides were confirmed by 1H, 13C and 19F NMR spectra, high resolution mass spectrometry and elemental analyses. The optical activities were confirmed by optical rotation measurements. All compounds have been screened for antimicrobial activities using two fold serial microdilution methods. AMPICILLIN, AMOXICILLIN, TETRACYCLINE, PENICILLIN G, LINCOSAMIDE A and ERYTHROMYCIN were used as comparative standard drug under the same protocol. Interesting values of MIC were obtained in selected derivatives against Staphylococcus aureus, testing has been therefore extended to MRSA and to toxinogenic strains of Staphylococcus aureus. In addition, the cytotoxicity of most active compounds was investigated against cancer cell line (Jurkat) and one type of normal lung fibroblast cells (MRC-5) by XTT tetrazolium salt reduction assay, propidium iodide flow cytometry assay and xCELLigence system allowing a label-free assessment of the cells proliferation.	(R)-1-(6-fluorobenzothiazol-2-yl)-3-methylbutan-1-amine; salicylicamides; antimicrobial activities

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