Sep 16, 2019   10:55 a.m. Ľudomila, Ľudmila
Academic information system

Summary of topics offered - Department of Organic Chemistry (IOCP FCFT)


Basic information

Type of work: Dissertation thesis
Topic: Syntéza glykozylovaných dusíkatých heterocyklov ako možných predlôh na vývoj liekov proti civilizačným ochoreniam
Title of topic in English: Synthesis of glycosylated nitrogen heterocycles as potential hits for drug design against civilization diseases
State of topic: approved (prof. Ing. Tibor Gracza, DrSc. - Chairperson of Departmental Board)
Thesis supervisor: doc. Ing. Ladislav Petruš, DrSc.
Faculty: Faculty of Chemical and Food Technology
Supervising department: Department of Organic Chemistry - IOCP FCFT
Max. no. of students: --
Academic year:2019/2020
Proposed by: doc. Ing. Ladislav Petruš, DrSc.
External educational institution: Institute of Chemistry of the Slovak Academy of Sciences
Annotation: Chemická syntéza hydrolýze odolných disacharidových mimetík dvojitou reduktívnou amináciou dikarbonylových derivátov monosacharidov s C-glykozylovanými metylamínmi, ktoré sú teraz ľahko dostupné z glykozylovaných nitrometánov vo všetkých ich tautomérnych štruktúrach. Voľba špecifických glykozylových zvyškov v získaných N-glykozyl-metylovaných iminocukroch by mohla významne zvýšiť ich inhibičnú selektivitu na jednotlivé glykozidové hydrolázy. Následná derivatizácia takýchto disacharidových iminocukrov s terminálne aktivovanými alkylfosfonátmi ich umožňuje premeniť aj na potenciálne špecifické inhibítory glykozylových transferáz. Takéto deriváty iminocukrov by sa mohli stať predlohami pre vývoj liekov na kontrolu nežiadúcich porúch glykozylácie spôsobujúcich mnohé závažné ochorenia ako aj na účinnú ochranu proti patogénnym mikroorganizmom a vírusom.
Annotation in English: Chemical synthesis of hydrolysis-resistant disaccharide mimetics by double reductive amination of dicarbonyl derivatives of monosaccharides with C-glycosyl methylamines, which nowadays are easily available from glycosyl nitromethanes in all their tautomeric structures. The choice of specific glycosyl moieties in obtained N-glycosylmethylated iminosugars could significantly increase their inhibition selectivities to individual glycoside hydrolases. Subsequent derivatization of these disaccharidic iminosugars with terminally activated alkylphosphonates also enables to transform them to potential specific inhibitors of glycosyl transferases. These derivatives of iminosugars could become the patterns for discovery of drugs for controlling glycosylations disorders causing several serious diseases as well as for efficient protection against pathogenic microorganisms and viruses.



Limitations of the topic

To sign up for a topic it is necessary to fulfil one of the following restrictions

Limit to study programme
The table shows limitations of study programme, field, track the student has to be enrolled in to be able to register for a given topic.

ProgrammeTrackTrack
D-ORGCH Organic Chemistry-- not entered -- -- not entered --
D-ORGCHxA Organic Chemistry-- not entered -- -- not entered --