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Synthesis and evaluation of potential biologically active rhodanine derivatives and analogues
Šimková, Adéla ; Krátký, Martin (advisor) ; Matouš, Petr (referee)
The topic of this thesis is the synthesis of rhodanine derivatives and evaluation of their biological activity, particularly as potential cholinesterases inhibitors. This group of compounds is important for treatment of many diseases, e.g., Alzheimer's disease or myasthenia gravis. All synthetized compounds are based on structure of rhodanine (2-thioxothiazolidine- 4-one), which is an important heterocyclic compound with a wide spectrum of biological properties. Its structure can be modified in many ways, which can be used in the development of new drugs. Its derivatives have been shown to have, for example, anti-inflammatory, anticancer, antibacterial and antifungal activities, as well as inhibitory activity against several enzymes, e.g., cholinesterases. Seventeen compounds were synthesized in sufficient amount for characterisation and assessment of biological activity (7-93 %). Most of them are amides based on the structure of 2-thioxothiazolidine-4-one and thiazolidine-2,4-dione, that were prepared by carbodiimide- mediated coupling, other derivatives are based on the structure of 2-thioxothiazolidine-4-one and from 2,4-dioxothiazolidine-3-acetic acid. These compounds were prepared by Knoevenagel condensation in glacial acetic acid. All compounds were tested for their inhibitory activity...
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Synthesis and evaluation of potential biologically active rhodanine derivatives and analogues
Šimková, Adéla ; Krátký, Martin (advisor) ; Matouš, Petr (referee)
The topic of this thesis is the synthesis of rhodanine derivatives and evaluation of their biological activity, particularly as potential cholinesterases inhibitors. This group of compounds is important for treatment of many diseases, e.g., Alzheimer's disease or myasthenia gravis. All synthetized compounds are based on structure of rhodanine (2-thioxothiazolidine- 4-one), which is an important heterocyclic compound with a wide spectrum of biological properties. Its structure can be modified in many ways, which can be used in the development of new drugs. Its derivatives have been shown to have, for example, anti-inflammatory, anticancer, antibacterial and antifungal activities, as well as inhibitory activity against several enzymes, e.g., cholinesterases. Seventeen compounds were synthesized in sufficient amount for characterisation and assessment of biological activity (7-93 %). Most of them are amides based on the structure of 2-thioxothiazolidine-4-one and thiazolidine-2,4-dione, that were prepared by carbodiimide- mediated coupling, other derivatives are based on the structure of 2-thioxothiazolidine-4-one and from 2,4-dioxothiazolidine-3-acetic acid. These compounds were prepared by Knoevenagel condensation in glacial acetic acid. All compounds were tested for their inhibitory activity...
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The characteristic of the games of top women's teams at the vollejball World Cup 2010
Šimková, Adéla ; Buchtel, Jaroslav (advisor) ; Vorálek, Rostislav (referee)
6 ABSTRAKT 1. NAME The characteristic of the games of top women's teams at the volleyball World Cup 2010 2. SUBJECT The characteristic of vollejball, The feature of women's teams at the volleyball World Cup 2010 3. THE GOAL OF WORK Characteristics performance of the game selected volleyball team women's at the World Cup 2010 in Japan, based on the success of the selected gaming activities of individuals. 4. RESULTS After meeting the goals to characterize and compare the results of selected teams, a success in selected gaming activities of the individual. 5. KEY WORDS volleyball, the top volleyball, individual playing activities, World Championships,
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Synthesis and evaluation of potential antimicrobial agents
Šimková, Adéla ; Krátký, Martin (advisor) ; Matouš, Petr (referee)
The topic of this bachelor thesis is an alarming global problem of acquired resistance of methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Staphylococcus aureus, vancomycin-intermediate susceptible Staphylococcus aureus and vancomycin- resistant enterococci strains, their limited current treatment options for infections caused by these pathogens, synthesis and evaluation of potential antimicrobial compounds active also against these resistant Gram-positive strains. The development of novel drugs against drug-resistant pathogens is challenging. Designed compounds are based on sulfa drug mafenide, which is used in the treatment of topical infections caused by Gram-positive and Gram-negative bacteria. The targeted imines were prepared from mafenide acetate and carbonyl compounds in one step. Most of these novel compounds are derivatives of salicylaldehyde, furthermore, derivates of 5- nitrothiophene-2-carbaldehyde and isatin were also synthesized. Thirteen compounds were prepared with good yields (50-95%). All these compounds were tested against Gram-positive (including MRSA) and Gram-negative bacteria, mycobacteria, and fungi by the broth microdilution method. The lowest minimum inhibitory concentration (MIC) values against bacteria, fungi as well as the highest...
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The characteristic of the games of top women's teams at the vollejball World Cup 2010
Šimková, Adéla ; Buchtel, Jaroslav (advisor) ; Vorálek, Rostislav (referee)
6 ABSTRAKT 1. NAME The characteristic of the games of top women's teams at the volleyball World Cup 2010 2. SUBJECT The characteristic of vollejball, The feature of women's teams at the volleyball World Cup 2010 3. THE GOAL OF WORK Characteristics performance of the game selected volleyball team women's at the World Cup 2010 in Japan, based on the success of the selected gaming activities of individuals. 4. RESULTS After meeting the goals to characterize and compare the results of selected teams, a success in selected gaming activities of the individual. 5. KEY WORDS volleyball, the top volleyball, individual playing activities, World Championships,
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