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Charles University, Faculty of Pharmacy in Hradec Králové Department of: Department of Organic and Bioorganic Chemistry Candidate: Mgr. Rudolf Vosátka Supervisior: prof. RNDr. Jarmila Vinšová, CSc. Consultant: PharmDr. Mgr. Martin Krátký, Ph.D. Title of Doctoral Thesis: Design and synthesis of new potentially antibacterial active compounds Tuberculosis (TB) and its resistant forms are one of the most often causes of death worldwide. It is therefore a matter of interest for many scientific groups, as well as a notable global risk of increasing resistance of bacteria and fungi, which must also be dealt with. The introduction of doctoral thesis deals with the TB in terms of epidemiology, pathogenesis, Mycobacterium tuberculosis and its current treatment, as well as its resistance problems. This work also present four basic structures, which then form the basic building blocks for the experimental part. It is triclosan, a direct inhibitor of mycobacterial enoyl-ACP reductase, antimicrobial highly effective salicylanilides, isoniazid as one of the most important antituberculotic drugs and p-aminosalicylic acid, which is a second line antituberculotic agent. The experimental part deals with variations of these structures leading to biological response, respectively antimycobacterial, antibacterial,... |
