May 22, 2019   1:22 a.m. Júlia, Juliana
Academic information system

Summary of topics offered - Faculty of Chemical and Food Technology


Basic information

Type of work: Dissertation thesis
Topic: Deriváty kyseliny 1-indoloctovej ako inhibítory aldózareduktázy: hodnotenie biologickej aktivity
Title of topic in English: Indole-1-acetic acid derivatives as aldose reductase inhibitors: evaluation of biological activity
State of topic: approved (prof. Ing. Albert Breier, DrSc. - Chairperson of Departmental Board)
Thesis supervisor: Ing. Milan Štefek, PhD.
Faculty: Faculty of Chemical and Food Technology
Supervising department: Institute of Biochemistry and Microbiology - FCFT
Max. no. of students: --
Academic year:2019/2020
Proposed by: Ing. Milan Štefek, PhD.
External educational institution: Centrum experimentálnej medicíny Slovenskej akadémie vied
Annotation: Inhibítory aldózareduktázy (AR) majú predpoklad uplatniť sa v terapii diabetických komplikácií ( DK) a chronického zápalu. Deriváty kyseliny 1-indoloctovej predstavujú skupinu účinných inhibítorov aldózareduktázy, avšak kvôli nežiaducim efektom nenašli klinické využitie. Nedávno sme identifikovali 5-karboxy-3-merkapto-1,2,4-triazino-[5,6-b]indol ako účinný inhibitor AR. Látka je predmetom patentovej ochrany ako sľubná nosná štruktúra pre dizajn vysoko efektívnych inhibítorov AR. Cieľom projektu je pokračovať vo vývoji nových derivátov kyseliny 1-indoloctovej ako inhibítorov AR so zameraním na liečbu DK a chronického zápalu. Nové deriváty budú podrobené skríningu na inhibičnú aktivitu a selektivitu v podmienkach in vitro na úrovni izolovaného enzýmu. Najúčinnejšie z nich sa podrobia predklinickému hodnoteniu ex vivo na orgánovej úrovni izolovaných očných šošoviek potkana a in vivo za podmienok experimentálneho diabetu potkanov.
Annotation in English: Aldose reductase inhibitors (ARIs) have been developed as potential remedies to treat diabetic complications (DC) and chronic inflammation. Indole-1-acetic acids represent a group of efficient ARIs, yet they have not been used clinically owing to their side effects. Recently 5-carboxy-3-mercapto-1,2,4-triazino-[5,6-b]indole was identified as efficient ARI. The compound is a subject of patent protection as a promising scaffold for development of powerful ARIs. The aim of the project is to continue in developing of novel indole-1-acetic acid derivatives as AR inhibitors aimed at treatment of DCs. The new derivatives will be subjected to the screening for ARI activities in vitro at the level of isolated enzyme. The most promising compounds will pass a pre-clinical evaluation ex vivo at the organ level of isolated rat lenses and in vivo under conditions of experimental diabetes of rats.



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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-BICH Biochemistry-- not entered -- -- not entered --