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Synthesis of tetrazoles as anticuberculotics
Vicherek, Petr ; Čonka, Patrik (advisor) ; Klimešová, Věra (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Petr Vicherek Supervisor: RNDr. Patrik Čonka, Ph.D. Title of diploma thesis: Synthesis of tetrazoles as antituberculotics Although significant progress in therapy of tuberculosis has been made since effective drugs were discovered in the second half of the 20th century, it is still widespread and refractory curable disease. The situation is complicated with growing appearance of resistant strains and for that reason it is necessary to search for new potential antituberculotics. The aim of this work was to continue with synthesis of antimycobacterial-efficient structures based on tetrazole. Firstly, we synthesised derivates of 1-aryl-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazole by the method of Williamson's synthesis, when the reaction of 1-aryl-1H-tetrazol-5-thiol with 3,5-dinitrobenzylchloride was performed. Conditions of the reactions were further optimalised. We prepared by the same way derivates of 1-fenyl-5-[(3,4,5- trimethoxybenzyl)sulfanyl]-1H-tetrazole afterwards, as analogues of previous tetrazoles missing the electron withdrawing 3,5-dinitrosubstitution. Furthermore, we concentrated on synthesis of substituted 1,5-diphenyl-1H-tetrazoles. Substituted...
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Synthesis of tetrazoles as anticuberculotics
Vicherek, Petr ; Čonka, Patrik (advisor) ; Klimešová, Věra (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Petr Vicherek Supervisor: RNDr. Patrik Čonka, Ph.D. Title of diploma thesis: Synthesis of tetrazoles as antituberculotics Although significant progress in therapy of tuberculosis has been made since effective drugs were discovered in the second half of the 20th century, it is still widespread and refractory curable disease. The situation is complicated with growing appearance of resistant strains and for that reason it is necessary to search for new potential antituberculotics. The aim of this work was to continue with synthesis of antimycobacterial-efficient structures based on tetrazole. Firstly, we synthesised derivates of 1-aryl-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazole by the method of Williamson's synthesis, when the reaction of 1-aryl-1H-tetrazol-5-thiol with 3,5-dinitrobenzylchloride was performed. Conditions of the reactions were further optimalised. We prepared by the same way derivates of 1-fenyl-5-[(3,4,5- trimethoxybenzyl)sulfanyl]-1H-tetrazole afterwards, as analogues of previous tetrazoles missing the electron withdrawing 3,5-dinitrosubstitution. Furthermore, we concentrated on synthesis of substituted 1,5-diphenyl-1H-tetrazoles. Substituted...
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