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Metabolism and efficacy of new potential anthelmintics
Zajíčková, Markéta ; Skálová, Lenka (advisor) ; Várady, Marián (referee) ; Vadlejch, Jaroslav (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Mgr. Markéta Zajíčková Supervisor: Prof. RNDr. Lenka Skálová, Ph.D. Consultant: PharmDr. Ivan Vokřál, Ph.D. Title of Dissertation Thesis: Metabolism and efficacy of new potential anthelmintics Overpopulation of gastrointestinal nematodes represents global health and economical problem. Therefore, suitable solution in the form of effective anthelmintic treatment is needed. Several anthelmintics with distinct mechanism of action are available on the market, however, the widespread resistance limits their efficacy. As a consequence, finding a new possible alternative becomes important. In present dissertation thesis, the novel anthelmintic candidates were selected and their effect against model parasitic nematode Haemonchus contortus was examined. The studies encompassed three approaches within the field of drug discovery: new molecular entity identification and structure modification, drug repurposing, and medicinal plants screening. Newly synthesized compounds designated as BLK127, HBK4 and BLK127 derivatives, already known antipsychotic drug sertraline (SRT) and the extracts from eight European ferns species from genus Dryopteris, Athyrium and Blechnum were the subjects of our interests. Two...
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Metabolism and efficacy of new potential anthelmintics
Zajíčková, Markéta ; Skálová, Lenka (advisor) ; Várady, Marián (referee) ; Vadlejch, Jaroslav (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Mgr. Markéta Zajíčková Supervisor: Prof. RNDr. Lenka Skálová, Ph.D. Consultant: PharmDr. Ivan Vokřál, Ph.D. Title of Dissertation Thesis: Metabolism and efficacy of new potential anthelmintics Overpopulation of gastrointestinal nematodes represents global health and economical problem. Therefore, suitable solution in the form of effective anthelmintic treatment is needed. Several anthelmintics with distinct mechanism of action are available on the market, however, the widespread resistance limits their efficacy. As a consequence, finding a new possible alternative becomes important. In present dissertation thesis, the novel anthelmintic candidates were selected and their effect against model parasitic nematode Haemonchus contortus was examined. The studies encompassed three approaches within the field of drug discovery: new molecular entity identification and structure modification, drug repurposing, and medicinal plants screening. Newly synthesized compounds designated as BLK127, HBK4 and BLK127 derivatives, already known antipsychotic drug sertraline (SRT) and the extracts from eight European ferns species from genus Dryopteris, Athyrium and Blechnum were the subjects of our interests. Two...
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Advances in the discovery and testing of anthelmintics
Nguyen, Thuy Linh ; Skálová, Lenka (advisor) ; Lamka, Jiří (referee) ; Várady, Marián (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Training Workplace Department of Biochemical Sciences Doctoral Degree Program Xenobiochemistry and Pathobiochemistry Candidate Mgr. Thuy Linh Nguyen Supervisor Prof. RNDr. Lenka Skálová, Ph.D. Advisor Assoc. Prof. Ing. Petra Matoušková, Ph.D. Title of Doctoral Thesis Advances in the discovery and testing of anthelmintics The parasitic nematodes cause a considerable problem in human and animal health worldwide. The group of gastrointestinal nematodes is responsible for economic losses in livestock production. The treatment relies on the use of a limited number of anthelmintics, but their efficacy is hampered due to widespread drug resistance. Given the need for new drugs, the present thesis focuses on discovering novel compounds with potential anthelmintic effects and on the development of testing methods. Based on the literature search, we presented the possible approaches in the current development of new anthelmintics and evaluated their advantages and disadvantages in a review article. For the experiments, we used a model organism Haemonchus contortus, which is one of the most important gastrointestinal pathogens of small ruminants. The primary phenotypic screening of a small compound library against larvae identified two 'hit' compounds...
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Advances in the discovery and testing of anthelmintics
Nguyen, Thuy Linh ; Skálová, Lenka (advisor) ; Lamka, Jiří (referee) ; Várady, Marián (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Training Workplace Department of Biochemical Sciences Doctoral Degree Program Xenobiochemistry and Pathobiochemistry Candidate Mgr. Thuy Linh Nguyen Supervisor Prof. RNDr. Lenka Skálová, Ph.D. Advisor Assoc. Prof. Ing. Petra Matoušková, Ph.D. Title of Doctoral Thesis Advances in the discovery and testing of anthelmintics The parasitic nematodes cause a considerable problem in human and animal health worldwide. The group of gastrointestinal nematodes is responsible for economic losses in livestock production. The treatment relies on the use of a limited number of anthelmintics, but their efficacy is hampered due to widespread drug resistance. Given the need for new drugs, the present thesis focuses on discovering novel compounds with potential anthelmintic effects and on the development of testing methods. Based on the literature search, we presented the possible approaches in the current development of new anthelmintics and evaluated their advantages and disadvantages in a review article. For the experiments, we used a model organism Haemonchus contortus, which is one of the most important gastrointestinal pathogens of small ruminants. The primary phenotypic screening of a small compound library against larvae identified two 'hit' compounds...
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