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Amidoximes as intermediates for the synthesis of potential drugs
Katirtzi, Anastasia ; Opletalová, Veronika (advisor) ; Kučerová, Marta (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Student: Anastasia Katirtzi Supervisor: Assoc. Prof. RNDr. Veronika Opletalová, Ph.D. Title of Diploma Thesis: Amidoximes as intermediates for the synthesis of potential drugs The current thesis is focused on the O-acylation of pyrazine amidoximes and their cyclization to the corresponding 3,5-disubstituted- 1,2,4-oxadiazoles. 5-unsubstituted and 5-butylpyrazine amidoximes were acylated by acetic anhydride, trimethylacetic anhydride and 2,3-pyrazinecarboxylic anhydride as acylating agents in toluene. Formation of oxadiazoles was achieved in xylene, using acetic anhydride for acylation. Identification of the products was done by melting points, NMR and IR spectra, and their purity was proved by elemental analysis Furthermore, amidoximes and their derivatives were subjected to biological assay in order to evaluate their in vitro antifungal and antibacterial properties. Unfortunatelly, amidoximes and 1,2,4-oxadiazoles were inactive. For the esters, biological results will be available later.
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