| Summary: | Title of diploma thesis: Pyrazine derivatives as potential drugs V. Presented by: Radka Krejcarová Supervisor of diploma thesis: doc. PharmDr. Martin Doležal, Ph.D Researches focused on the importance of tuberculosis in the world nowadays pointed to the fact that tuberculosis is the third most common infectious disease in the world, and is still increasing share of multi-drug resistant strains. In the thesis we focused on the synthesis of potential antituberculotics derived from pyrazine. From the initial 6-chloropyrazine-2-carboxylic acid were synthesized a series of seven esters of this acid, which are still not described in chemical literature. Two different methods were used to this synthesis. A microwave reactor was used for this synthesis. All products were characterized by TLC, IR, 1 H and 13 C NMR spectra. The calculated log P values of the newly prepared substances are given. Subsequently, a series of substances was subjected to in vitro biological evaluation. Information on the antifungal and antibacterial activity of newly prepared compounds were measured at the Department of Biological and Medical Sciences FaF Charles University in Hradec Králové. The final products are also subject of antimycobacterial screening in the international search programme TAACF (Tuberculosis Antimicrobial...
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