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AMIDOXIMES AS SYNTHETIC INTERMEDIATES AND POTENTIAL DRUGS I. Michaela Horká Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control In the theoretical part of this diploma thesis, biological activities of amidoximes are resumed. They have been studied mainly as prodrugs that are reduced to active compounds - amidines. Some amidoximes reached clinical trials but due to their significant undesirable effects have not been developed further. Methodical part deals with various synthetic procedures for the preparation of amidoximes. In the frame of the experimental part, four 5-alkylpyrazine-2-carbonitriles were synthesized at first. Using hydroxylamine hydrochloride, the nitriles were converted to corresponding amidoximes: N'-hydroxy-5-propylpyrazine-2-carboximidamide N'-hydroxy-5-isopropylpyrazine-2-carboximidamide N'-hydroxy-5-pentylpyrazine-2-carboximidamide N'-hydroxy-5-hexylpyrazine-2-carboximidamide None of the obtained products have been reported yet. They were characterized by melting points, IR, NMR spectra. Their purity was checked by elemental analysis. The compounds were tested for antifungal and antibacterial activity but were found non-effective. This is probably due to the fact that in vitro their bioactivation... |
