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Charles University Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Pavel Sychra Supervisor: prof. PharmDr. Alexandr Hrabálek, CSc. Title of diploma thesis: Five-members N-heterocycles as potential antituberculotics Tuberculosis is widespread infectious disease predominantly caused by Mycobacterium tuberculosis. According to World Health Organization, 10.4 million new cases of tuberculosis and 1.8 million deaths from tuberculosis were registered worldwide only in 2015. In the previous work of our group it was found that 2,5- and 1,5-disubstituted tetrazoles and 2,5-disubstituted oxadiazoles bearing 3,5-dinitrobenzylsulfanyl fragment exhibited outstanding antimycobacterial activities. The aim of this work was to modify these lead structures by removing the methylsulfanyl linker and to prepare a series of 3,5-dinitrophenyl tetrazole and oxadiazole derivatives. Firstly, we prepared a series of 2- and 1-benzyl-5-(3,5-dinitrophenyl)-1H-tetrazoles by the reaction of 5-(3,5-dinitrophenyl)-1H-tetrazole with diversely substituted benzyl halide. In another part, we dealt with the preparation of tetrazole derivatives containing saturated nitrogen heterocycle. At first, it was necessary to prepare alkylating agents, which have been subsequently used for alkylation... |
