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"Drug Delivery" systems for nuclear medicine
Kučka, Jan ; Lešetický, Ladislav (advisor) ; Smrček, Stanislav (referee) ; Hampl, František (referee) ; Hampl, Richard (referee)
5. SummarY in Czech (Souhrn) Podařilo se stabilně vilzat skvantitativním ýěŽkem '''At na potenciálně ořímopouŽitelnýnosič,kteýdobřeodolávásilnéradio|ysevyvolanécr- ;;il; zllAt. íIavícse poáařilo částečněozřejmit chování ,''At vůči redukčněoxidačnímp.o""'ů. a stabilizovat jej v chemické formě astatidu vhodné pro značenízvoleného systému. Byly připraveny a charalÍerizovány modelové rozpustné systémy nuuizě.,e^ pio cílenímakromo1ekul do kostní tkáně a za|oŽené na statisticlcýc.h kopolymerech N-l2-(hydroxypropyl)].methakrylamidu , Ínono,n"."* obsahujítímhydroxybisfosfonátové skupiny. Byla prokázána rychlá a účinnáadsorpce cílěnýchpolymerů na in vitro model kostní tkáně hydroxyapatit (většiná polymeru je nasorbována během 1 minuty inkubace; u ruao- piípadůbylo nasorbováno za tuto dobu přes 80 % polymeru). MnoŽstvípolymeruadsorbovanéhonahydroxyapatitjesilnězávislé |r"á"usirn na.obsahu hydroxybisfosfonáj9Úch skupin v polymeru. Byly irip.uu"ny systémy ousátru.ji modelová léčívavázaná na polyrner stabilní .u,nioi"tou, nya.oíyti"ty sicpitelnou hydrazonovou vazbou. Na pol1mer uvi" """a'*ó "n".i"té kancerostatikum (doxorubicin), radiodiagnostikum |úin)u model radioterapeutika ('25|. Byl připraven, charakterizován,.. omačen a in vivo otestován termoresponsivní systémnesoucí 1311 u 90y. Byla pozorována dobrá...
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Structure-Antifungal Activity Relationships in Substituted Butenolides
Šenel, Petr ; Pour, Milan (advisor) ; Hampl, František (referee) ; Doležal, Martin (referee)
Within the framework of this Thesis, several series of 3-(4-bromophenyl)-2,5- -dihydrofuran-2-ones with various substituents at C(5) derived from in vitro antifungally active 3-(4-bromophenyl)-5-acetyloxymethyl-2,5-dihydrofuran-2-one were prepared with the aim of further development of potential antifungals based on this lead. Primarily, we focused on the synthesis of furanones bearing alkylidene or alkoxymethyl/aryloxymethyl moiety in position 5. We found that 5-acyloxymethyl and 5-aryloxymethyl furanone derivatives undergo elimination leading to 3-(4-bromophenyl)-5-methylene-2,5-dihydrofuran-2-one under the antifungal screening conditions. This compound initiates fungal cell membrane disruption and is responsible for the antifungal activity of the former. The 5-alkoxymethyl analogues are unable to undergo the elimination process and are therefore inactive. The antifungal activity of 5- alkylidene furanones depends on the substitution of alkylidene side chain. Some of the target compounds displayed interesting cytostatic activities against HeLa S3 and CCRF-CEM cells (IC50 < 5 µmol.L-1 ). Furthermore, syntheses of 4-substituted or 4,5-disubstituted-3-(4-bromophenyl)-2,5- -dihydrofuran-2-ones were carried out. Some of the prepared derivatives possessed notable antifungal or antimicrobial activity.
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Synthesis of human ω-O-acylceramides and evaluation of their effects on barrier properties of skin lipid membranes
Opálka, Lukáš ; Vávrová, Kateřina (advisor) ; Hampl, František (referee) ; Kučerka, Norbert (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic chemistry Candidate: Mgr. Lukáš Opálka Supervisor: doc. PharmDr. Kateřina Vávrová, Ph.D. Title of doctoral thesis: Synthesis of human ω-O-acylceramides and evaluation of their effects on barrier properties of skin lipid membranes The main objective of this work was to synthesize and study human acylceramides (acylCer, ceramides of the EO type) with the focus on the relationships between the acylCer concentration , structure of their polar head, their ability to form lamellar phases and permeability of model lipid membranes. Another objective was to synthesize ceramide-1-phosphates for the study of their signaling role in skin barrier and an analogue of ganglioside GM1 with shorter acyl chain as a standard for analysis of these lipids. Ceramides (Cer) belong to the family of sphingolipids. They are the central molecules in sphingolipid metabolism, they participate on cell regulatory processes and the formation of human skin lipid barrier. The main skin barrier is situated in the stratum corneum (SC), which is the uppermost layer of skin. The purpose of SC is to maintain homeostasis of the inner environment and to prevent the penetration of exogenous substances, allergens and bacteria to the...
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