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Fungal secondary metabollites with antiviral activity
Besedová, Alena ; Čmoková, Adéla (advisor) ; Kolařík, Miroslav (referee)
The past year 2020 has clearly shown how quickly some viral infections can reach pandemic proportions. Thus, there is still a need to discover new substances with antiviral activity. Such substances (eg. asteltoxin E, cytosporaquinone B) have been discovered in the past in several groups of fungi, however, their potential as a source of virostatic chemotherapeutics has not been much explored. The possible use of fungi as a source of substances with antiviral activity is also indicated by the use of some species (eg. Ganoderma linghzi, Lentinula edoles) in the alleviation or prevention of viral diseases in traditional medicine. In most cases, however, it was not possible to find substances responsible for this effect. Therefore, in my bachelor's thesis I will first analyse kinds of fungi traditionally used as treatment of viral infections in traditional medicine. I will also summarize the most important fungal substances for which antiviral activity has been demonstrated. The bachelor's thesis will provide a comprehensive overview of currently known secondary metabolites of fungi and their virostatic effects. The information summarized in the work may point to possible candidates in the fight against viral infections.
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Acyclic nucleosides of 3-hydroxypyrazine-2-carboxamide bases
Chaloupecká, Ema ; Jindřich, Jindřich (advisor) ; Smrček, Stanislav (referee)
This thesis deals with the preparation of acyclic nucleosides and nucleoside phosphonates of compounds T-705 (6-fluoro-3-hydroxypyrazine-2-carboxamide) and T-1105 (3-hydroxypyrazine-2-carboxamide). Acyclic nucleoside phosphonates are substances that can terminate viral RNA or DNA replication, and some of them are used in the treatment of viral diseases. T-705 and T-1105 have shown activity against the influenza virus, and T-705 has already been approved for its treatment in Japan. Since both compounds mimic natural nucleobases in the body, their acyclic nucleosides and nucleoside phosphonates also have the potential to be biologically active. Methods for the synthesis of 3-fluoro-2-(phosphonomethoxy)propyl and 3-hydroxy-2-(phosphonomethoxy)propyl derivatives of T-705 and T-1105, their prodrugs containing lipophilic groups for the improvement of the pharmacokinetic properties and also their phosphonate diphosphates, suitable for the biological activity measurements, have been proposed. Some of these derivatives were subsequently prepared. Key words: acyclic nucleosides, acyclic nucleoside phosphonates, T-705, T-1105, favipiravir, antiviral activity, influenza
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2-(Phosphonomethoxy)ethyl derivatives of 6-fluoro-3-hydroxypyrazine-2-carboxamide
Lamačová, Lucie Josefa ; Jindřich, Jindřich (advisor) ; Baszczyňski, Ondřej (referee)
This bachelor thesis deals with the preparation of derivatives of acyclic nucleoside phosphonates with nitrogenous base favipiravir. There are many examples of acyclic nucleoside phosphonates that are used as antiviral drugs due to their structure. Favipiravir shows antiviral activity against the influenza virus. The target compounds thus might have the potential to be biologically active, which will be tested in virological laboratories at KU Leuven in Belgium. First, the methods for preparation of 2-(phosphonomethoxy)ethyl derivative of favipiravir was designed, then for its diphosphate and a prodrug with pivaloyloxymethyl groups to increase the bioavailability of the compound. Thus, 2-(phosphonomethoxy)ethyl derivatives of favipiravir and its de-fluoro analogue were prepared. Key words: acyclic nucleoside phosphonates, T-705, favipiravir, T-1105, influenza, antiviral activity
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