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Structure-antimycobacterial activity relationships in the series of dinitrophenyl-substituted heterocycles
Mašek, Zdeněk ; Roh, Jaroslav (advisor) ; Krátký, Martin (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Author: Zdeněk Mašek Supervisor: doc. PharmDr. Jaroslav Roh, Ph.D. Title of diploma thesis: Structure-antimycobacterial activity relationships in the series of dinitrophenyl-substituted heterocycles Tuberculosis is an infectious disease with an increasing number of cases each year. Resistance of the pathogen, namely Mycobacterium tuberculosis, to the treatment, even against combined therapy keeps increasing. In 2020, tuberculosis was the second most common cause of death by infectious disease after COVID-19 (it claimed 1.5 million lives) and it is also estimated that with COVID-19 weakening the population, these numbers will only grow. The aim of this work was to develop derivatives of previously studied 1H-tetrazoles and 1,3,4-oxadiazoles, with a sterically hindered sulfur atom (Fig. I), which may protect them from metabolic oxidation and therefore possibly increase their activity against resistant strains of M. tuberculosis as well as other mycobacterial strains and to increase biological halftime of these potential antituberculosis drugs. We prepared two test series, namely 1H-tetrazole series and 1,3,4-oxadiazole series both containing 4 compounds, whose antimycobacterial activities were...
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