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Pyrazine derivates as potential drugs III.
Bielesz, Stanislav ; Doležal, Martin (advisor) ; Chlupáčová, Marta (referee)
Derivates of pyrazine as potential drugs III Degree paper Stanislav Bielesz Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Chemistry and Drug Control, Heyrovského 1203, Hradec Králové The aim of this degree paper was to synthetise a series of derivates of pyrazine-2-carboxylic acid. In the concrete it was the series of substituated 3-phenylaminopyrazine-2,5- dicarboxamides. The substances were synthetised by common synthesis, they were characterised by their physiochemical properties (melting point, lipophility), IR spectroscopy and 1 H and 13 C NMR spectroscopy. The synthetised substancies were tested in USA for anti-tubercular activity by TAACF. The results of in vitro testing were good, but not enough for the further testing in vivo. They were also tested on the Faculty of Pharmacy against fungi. No activity was found.
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Pyrazine derivates as potential drugs III.
Bielesz, Stanislav ; Doležal, Martin (advisor) ; Chlupáčová, Marta (referee)
Derivates of pyrazine as potential drugs III Degree paper Stanislav Bielesz Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Chemistry and Drug Control, Heyrovského 1203, Hradec Králové The aim of this degree paper was to synthetise a series of derivates of pyrazine-2-carboxylic acid. In the concrete it was the series of substituated 3-phenylaminopyrazine-2,5- dicarboxamides. The substances were synthetised by common synthesis, they were characterised by their physiochemical properties (melting point, lipophility), IR spectroscopy and 1 H and 13 C NMR spectroscopy. The synthetised substancies were tested in USA for anti-tubercular activity by TAACF. The results of in vitro testing were good, but not enough for the further testing in vivo. They were also tested on the Faculty of Pharmacy against fungi. No activity was found.
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Chalcones and their analogues as potential drugs.
Chlupáčová, Marta ; Hartl, Jiří (advisor) ; Kuneš, Jiří (referee) ; Čižmárik, Jozef (referee)
1 SUMMARY This dissertation thesis deals with searching for potential drugs, particularly with preparation and biological activity study of natural compounds derivatives - chalcones. The work includes preparation of intermediates - 5-alkylated pyrazin-2-carbonitriles and 1-pyrazinyl-2-ethanones. Substituted chalcones, several series of pyrazine analogues of chalcones and Michael adducts of chalcones with different thiols were prepared as final products. In this part of the work, known reaction methodologies were used. Products were identified by melting point, resp. boiling point, IR, NMR spectra. Their purity was checked by elemental analysis. In the case of liquids, elemental analysis could not be performed, and MS spectra were recorded instead. In total were prepared 22 intermediates (9 of them have been described in our department) 62 final products (19 of them have been already described) 1 by-product 57 Unknown compounds were prepared. Synthesis of 12 compounds was not successful. The final products were tested for their antimycobacterial, antifungal, antialgal, and antiaggregating effects. The chalcones were examined for the ability to inhibit one of the cysteine protease - papain and this part of the work continued in a preliminary kinetic study of reaction addition of chalcones with thiol-...
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