Thesis (Selection of subject)

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2-(Fosfonomethoxy)ethyl deriváty 3-hydroxypyrazin-2-karboxamidu

Thesis title in Czech:	2-(Fosfonomethoxy)ethyl deriváty 3-hydroxypyrazin-2-karboxamidu
Thesis title in English:	2-(Phosphonomethoxy)ethyl derivatives of 3-hydroxypyrazine-2-carboxamide
Key words:	acyklické nukleosidfosfonáty, syntéza, T-1105, 3-hydroxypyrazin-2-karboxamid, antivirální aktivita, SARS-CoV-2, favipiravir
English key words:	acyclic nucleoside phosphonates, synthesis, T-1105, 3-hydroxypyrazine-2-carboxamide, antiviral activity, SARS-CoV-2, favipiravir
Academic year of topic announcement:	2019/2020
Thesis type:	Bachelor's thesis
Thesis language:	čeština
Department:	Department of Organic Chemistry (31-270)
Supervisor:	doc. RNDr. Jindřich Jindřich, CSc.
Author:	hidden - assigned by the advisor
Date of registration:	18.11.2019
Date of assignment:	26.11.2019
Date of electronic submission:	22.08.2021
Date of proceeded defence:	07.09.2021
Opponents:	Ing. Ondřej Baszczyňski, Ph.D.

Preliminary scope of work

Bakalářská práce se zabývá přípravou acyklických nukleosidfosfonátů odvozených od heterocyklické báze T-1105 (3-hydroxypyrazin-2-karboxamid). Tato báze je stabilnějším analogem T-705 (6-fluor-3-hydroxypyrazin-2-karboxamid, taktéž favipiravir). Obě látky vykazují antivirální aktivitu proti řadě RNA virů. Přepokládá se, že cílové sloučeniny jsou také biologicky aktivní, což bude dál zkoumáno na spolupracujícím pracovišti v Belgii.
Byly navrženy postupy pro přípravu 2-(fosfonomethoxy)ethyl derivátu T-1105, a jeho proléčiva s pivaloyloxymethyl skupinami pro zvýšení biologické dostupnosti látky.

Preliminary scope of work in English

The bachelor thesis deals with the preparation of acyclic nucleoside phosphonates derived from the heterocyclic base T-1105 (3-hydroxypyrazine-2-carboxamide). This base is a more stable analogue of T-705 (6-fluoro-3-hydroxypyrazine-2-carboxamide, also favipiravir). Both substances show antiviral activity against a number of RNA viruses. The target compounds are also thought to be biologically active, which will be further investigated at a collaborating site in Belgium.
Procedures have been proposed for the preparation of 2- (phosphonomethoxy)ethyl derivative T-1105, and its prodrug with pivaloyloxymethyl groups to increase the bioavailability of the substance.