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Study of thiol addition to biliverdine, the synthesis of labelled bilirubine
Felklová, Veronika ; Lešetický, Ladislav (advisor) ; Smrček, Stanislav (referee)
Biliverdin and bilirubin are bile pigments which are degradation products of heme. Biliverdin (BV) is greenish-blue pigment and is reduction product of tetrapyrrolic core of heme by influence of the hemoxygenase (HO). The final product of this degradation is yellowish-brown pigment bilirubin (BR) which forms from BV thanks to the biliverdinreduktase (BVR). Normal and slightly raised level of bilirubin in plasma has cytoprotective effects whereas high levels are cytotoxic often. In severe unconjugated hyperbilirubinemia cases (newborn children) unconjugated bilirubin (UCB) accumulates in central nervous system (CNS) and causes bilirubin-induced neurologic dysfunction (BIND). Unfortunately there is a limitation for finding UCB pathophysiology caused by difficult determination of UCB content and distribution in tissues and biological fluids. So the main purpose of this thesis is to find and integrate isolated methods which will serve as the basis of finding bilirubin distribution. This progress would have a significant effect on studies of bilirubin neurotoxicity on newborn children. This method is based on radioactive labeling of UCB. Preferentially atom C 10 used for binding suitable functional group (thiols) because conformation of indicated bilirubin shouldn't change in this position. And then the...
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Antituberculosis Agents and Their Antimicrobial Effects.
Novotná, Eva ; Waisser, Karel (advisor) ; Kvasničková, Eva (referee) ; Lešetický, Ladislav (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Organic and Inorganic Chemistry Candidate: Mgr. Eva Petrlíková Supervisor: Prof. RNDr. Karel Waisser, DrSc. Title of Doctoral Thesis: Antituberculosis Agents and Their Antimicrobial Effects. The dissertation focuses on the preparation of antimycobacterially active compounds. Some of the prepared compounds were also screened for the in vitro antibacterial and antifungal activity. The prepared compounds included sulfur derivatives of 3-benzyl-2H-1,3-benzoxazine- 2,4(3H)-diones, N-(pyridylmethyl)salicylamides, sulfur derivatives of 3-(4-alkylphenyl)- 2H-1,3-benzoxazine-2,4(3H)-diones, N-benzylthiosalicylamides, benzaldehyde- Sbenzylisothiosemicarbazones, salicylaldehyde-S-benzylisothiosemicarbazones, derivatives of 1,2-bis(9H-fluoren-9-ylidene)-N,N'-diarylethane-1,2-diamine, and hybrid molecules of cholesterol and terpenes. The highest antimycobacterial activity was exerted by 3-benzyl-2H-1,3-benzoxazine- 2,4(3H)-dithione and 3-(3,4-dichlorobenzyl)-2H-1,3-benzoxazine-2,4(3H)-dithione, 3-(4- secbutylphenyl)- 7-methyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-one, N-(4-methylbenzyl) thiosalicylamide and 4-methyl-N-(4-methylbenzyl)thiosalicylamide. Salicylaldehyde- S-(4-chlorobenzyl)isothiosemicarbazone was the most active...
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Synthesis of isotopically labeled ketamine
Stuchlíková, Lucie ; Lešetický, Ladislav (advisor) ; Smrček, Stanislav (referee)
In this work were synthesized ketamine isotopomers. Ketamine is used in human medicine and veterinary sectors. It has very broad spectrum of pharmacological effects: anesthetic, analgesic, hallucinogenic, bronchodilator, cardiovascular and antidepressive, which is currently in the research. At first was synthesized precursor of ketamine, N- desmethylketamine which was subsequently labeled the deuterium, tritium and carbon- 14. For the determination of purity and identity mass spectrometry and nuclear magnetic resonance spectroscopy were used. KEY WORDS synthesis of ketamine, ketamine, N-desmethylketamine, nor-ketamine, isotopically labeled ketamine, deuterium, tritium, carbon-14.
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