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Synthesis of Precursors for Biologically Active Lactones III.
Šipulová, Zuzana ; Kučerová, Marta (advisor) ; Kopecký, Kamil (referee)
OF DIPLOMA THESIS Synthesis of Precursors for Biologically Active Lactones III. Zuzana Šipulová Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Chemistry and Drug Control In the theoretical part of the diploma thesis, diseases caused by fungi (mycoses), their treatment and also antifungal and other effects of furan-2(5H)-one-containing agents are summarized. Methyl-(E)-2-brom-5-(2-nitrophenyl)pent-2-en-4-ynoate has been synthesized within the scope of the experimental work. Methyl-(E)-2-brom-5-phenylpent-2-en-4-ynoate has been also synthesized in the experimental work as a starting ester for methyl-(E)-2-(arylethynyl)-5-phenylpent-2-en- 4-ynoates which have been obtained via coupling with different alkynes. Syntheses of some derivates have been optimized by modification of reaction conditions. Methyl-(E)- 2-(arylethynyl)-5-phenylpent-2-en-4-ynoates can be used as starting compounds for synthesis of potential biological active lactones.
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In vitro Mechanism of Action of Selected Quinazoline Derivates on the Respiratory System
Šipulová, Zuzana ; Pourová, Jana (advisor) ; Hrdina, Radomír (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Zuzana Šipulová Consultant: PharmDr. Jana Pourová, Ph.D. Title of Thesis: In vitro mechanism of action of selected quinazoline derivates on the respiratory system Theoretical part of the thesis summarizes basic facts about asthma bronchiale, its therapeutic options, and bronchodilating effect of quinazoline-containing agents. In experimental work, bronchodilating effect of selected synthetic derivatives of quinazoline (VN 014, VN 015) as well as their mechanism of action have been studied. We focused on a beta agonist effect, and used salbutamol (beta agonist) as a standard drug. The classical method of isolated quinea pig trachea in vitro was employed. We have found that both tested substances show a bronchodilating effect. The mechanism of action of VN 014 is probably not beta agonistic. Derivative VN 015 did not react as a competitive beta agonist, exact mechanism is not possible to determine based on the results obtained.
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Synthesis of Precursors for Biologically Active Lactones III.
Šipulová, Zuzana ; Kučerová, Marta (advisor) ; Kopecký, Kamil (referee)
OF DIPLOMA THESIS Synthesis of Precursors for Biologically Active Lactones III. Zuzana Šipulová Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Chemistry and Drug Control In the theoretical part of the diploma thesis, diseases caused by fungi (mycoses), their treatment and also antifungal and other effects of furan-2(5H)-one-containing agents are summarized. Methyl-(E)-2-brom-5-(2-nitrophenyl)pent-2-en-4-ynoate has been synthesized within the scope of the experimental work. Methyl-(E)-2-brom-5-phenylpent-2-en-4-ynoate has been also synthesized in the experimental work as a starting ester for methyl-(E)-2-(arylethynyl)-5-phenylpent-2-en- 4-ynoates which have been obtained via coupling with different alkynes. Syntheses of some derivates have been optimized by modification of reaction conditions. Methyl-(E)- 2-(arylethynyl)-5-phenylpent-2-en-4-ynoates can be used as starting compounds for synthesis of potential biological active lactones.
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