Syntéza a design potenciálně antimikrobiálně aktivních sloučenin

Kozic, Ján

University: Charles University in Prague Faculty: Faculty of Pharmacy in Hradec Králové Department: Department of Inorganic and Organic Chemistry Candidate: Ing. et Mgr. Ján Kozic Supervisor: Prof. RNDr. Jarmila Vinšová, CSc. Title of Doctoral Thesis: Synthesis and Design of Potentially Antibacterial Active Compounds This work deals with the synthesis of benzanilides and their analogues as the potentially antimycobacterial active compounds. In the theoretical part of the work there is a description of tuberculosis (TBC) as a mycobacterial infectious disease and a short characteristic of recent antituberculotic drugs. The most important features of both, which determine the imperfection of recent antitubeculotics and the long-term multidrug TBC treatment, are emphasised. Further, some of the potential targets, useful for the development of new and more effective antituberculotics, are reviewed. Finally, there is a short overview of biological properties of benzanilides and thiobenzanilides and a more in depth characteristic of stereochemical properties of these compounds. In the experimental part of the work there are presented 100 benzanilide derivatives and their analogues. Ninety-two of these compounds are original, which have not been described in literature yet. For all of the compounds there...

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