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Preparation of Quaternary ammonium salts of triterpenoids
Biedermann, David ; Šarek, Jan (advisor) ; Klinot, Jiří (referee) ; Drašar, Pavel (referee) ; Kasal, Alexander (referee)
) Conclusion CONCLUSIONS This doctoral thesis was focused onto the synthesis if new quaternary ammonium salts oÍ. triterpenoids Ířom lupane, oleanane and ursane family for in vilro assessment of ťollowing biological activities: anti-HIV, antimicrobial, antiinflammatory and cýotoxic. Results are summed up in Íbllowing points: 1' Author co-operated pilot project of industrial isolation of betulin (1a) from approximately 400 kg of birch bark. Futhermore, research of side products and optimisation of preparation of bromoethyl-esters triterpenic acids was concluded. 2' Precursors for preparation of quaternary ammonium esters, bromoethyl-esters 2a, 3f, 3i, l1b, I2b, 14a,15a, and chloroethyl-ester 39, were slmthesised. 3' Six series of compounds, each consisting of three quaternary salts and one tertiary amine, were synthesised from betulinic acid (1b), oleanolic acid (1c), ursolic acid (1c), oxoac id, 3e, platanic acid (11a) a dihydrobetulinic acid (12a). Experimetal procedures are suitable for bulk syntheses. other quaternary salts of triterpenoids were also prepared. 4. oxoacid 3e was derivatised to yield group of heterocyclic hydrochlorides 6a, 6b,ód' 6f and group of heterocyclic salts 6c,6e,69. 5. All new cornpound s were assesed in vitro for cýotoxic activity against T-lymfoblatic leukemia CEM in research...
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Electrochemistry of Flavonolignans and their Interactions with DNA and Proteins
Pyszková, M. ; Zatloukalová, M. ; Biedermann, David ; Křen, Vladimír ; Ulrichová, J. ; Ramešová, Šárka ; Sokolová, Romana ; Vacek, J.
Electrochemical oxidation of flavonolignans silybin, silydianin, silychristin and their 2,3-dehydroderivatives, was studied using ex situ and in situ cyclic and square wave voltammetry at pyrolytic graphite electrode. The pilot results presented here could be used for further investigation of mechanism of oxidation and reactivity of flavonolignans to DNA and proteins.
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