Original title: Syntetické studie vedoucí k látkám interagujícím s CAR receptory
Translated title: Synthetic studies leading to CAR receptors ligands
Authors: Palša, Norbert ; Špulák, Marcel (advisor) ; Roh, Jaroslav (referee)
Document type: Master’s theses
Year: 2018
Language: slo
Abstract: [eng] [cze]
Charles University Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Candidate: Norbert Palša Supervisor: PharmDr. Marcel Špulák, PhD. Title of the Diploma Thesis: Synthetic studies leading to CAR receptor agonists CAR, which belongs to the family of xenobiotic nuclear receptors, affects xenobiotic and endogenic metabolic processes via metabolic enzyme genes expression. Since up to this day there is no available agonist which would activate CAR strictly without having an effect on similar nuclear receptors, thus, the effort to find such a compound is still ongoing. The aim of this diploma thesis was the synthesis of quinazoline derivatives, which, after previous preparation of 2-(3-methoxyphenyl)quinazoline-4-ol, a CAR agonist model compound, proved to be a promising group of chemical species with potential CAR activation effect - target compounds included amides of carboxylic acids via reaction with 2-aminobenzonitrile, derivatives of quinazoline-4-ol, quinazoline-4-thiol, 4-methoxyquinazoline and 3-methyl-3,4-dihydroquinazoline-4-one. Univerzita Karlova Farmaceutická fakulta v Hradci Králové Katedra organické a bioorganické chemie Kandidát: Norbert Palša Školiteľ: PharmDr. Marcel Špulák, PhD. Názov diplomovej práce: Syntetické štúdie vedúce k látkam interagujúcim s CAR receptormi CAR ako jeden z xenobiotických nukleárnych receptorov ovplyvňuje rad xenobiotických, ako aj telu vlastných metabolických dejov cestou expresie génov metabolických enzýmov. Keďže doteraz nebol objavený striktný CAR agonista, ktorý by neovplyvňoval aj príbuzné receptory, je snaha o nájdenie takejto zlúčeniny. Diplomová práca bola zameraná na syntézu derivátov chinazolínu, ktoré boli po predchádzajúcej príprave 2-(3-metoxyfenyl)chinazolín-4-olu, ako modelovej molekuly ligandu CAR, nádejnou skupinou látok s potenciálnym aktivačným účinkom na CAR - konkrétnymi syntetizovanými látkami boli amidy karboxylových kyselín pripravené reakciou s 2-aminobenzonitrilom, deriváty chinazolín-4-olu, chinazolín-4-tiolu, 4-metoxychinazolínu a 3-metyl-3,4-dihydrochinazolín-4-ónu.

Institution: Charles University Faculties (theses) (web)
Document availability information: Available in the Charles University Digital Repository.
Original record: http://hdl.handle.net/20.500.11956/102088

Permalink: http://www.nusl.cz/ntk/nusl-388291


The record appears in these collections:
Universities and colleges > Public universities > Charles University > Charles University Faculties (theses)
Academic theses (ETDs) > Master’s theses