National Repository of Grey Literature 4 records found  Search took 0.00 seconds. 
Derivatives of N-acetylglucosamine-1-phosphate as potential inhibitors of UDP-GlcNAc pyrophosphorylase
Černá, Lucie ; Baszczyňski, Ondřej (advisor) ; Veselý, Jan (referee)
This bachelor thesis deals with the preparation of phosphonate derivatives of N-acetyl- ᴅ-glucosamine-1-phosphate (GlcNAc-1-P), the substrate for UDP-GlcNAc pyrophospho- rylase (UAP1) enzyme, which is responsible for the chitin synthesis in fungal cell walls. Structural analogs of GlcNAc-1-P could potentially inhibit UAP1 and; therefore, their synthesis may enable the development of new antifungal drugs. This work is mainly focused on the synthesis of diethyl (2-acetamido-1,2-dideoxy-β-ᴅ-glucopyranosyl)phosphonate which was selected as a key model compound. The goal was to find the most suitable synthetic route leading to the synthesis of phosphonate and phosphinate GlcNAc-1-P analogues. Two synthetic methods were studied: 1) Michael addition of H-phosphonates to 2-nitroglucals; and 2) nucleophilic substitution of activated GlcNAc substrates (trichloroacetimidate and bromide) by phosphorus nucleophiles. Keywords: GlcNAc-1-P, UDP-GlcNAc pyrophosphorylase, antifungal, inhibitor
Derivatives of 5-alkylpyrazine-2-carboxylic acid as potential anti-infectives
Halířová, Martina ; Zitko, Jan (advisor) ; Kučerová, Marta (referee)
DERIVATIVES OF 5-ALKYLPYRAZINE-2-CARBOXYLIC ACID AS POTENTIAL ANTI-INFECTIVES HALÍŘOVÁ MARTINA Department of Pharmaceutical Chemistry and Drug Analysis, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic In our previous study, we have demonstrated that 5-alkylamino-N- phenylpyrazine-2-carboxamides with longer alkyl chain (C5-C8) exerted micromolar growth inhibition activity against M. tuberculosis H37Rv. We speculated that the long alkylamino chain could facilitate the penetration of lipophilic mycobacterial cell envelope. To test this hypothesis, we performed the amino to methylene isosteric exchange and designed a series of 5-alkyl-N-phenylpyrazine-2-carboxamides. 5- Alkylpyrazine-2-carboxylic acids (5-Ak-POA) were prepared by homolytic alkylation of commercially available pyrazine-2-carbonitrile by respective alkanoic acid, followed by hydrolysis of the carbonitrile group. Final derivatives were prepared by CDI mediated coupling of 5-Ak-POA with corresponding aniline at RT. Final compounds were described by melting point, elementary analysis, IR spectroscopy and 1 H, 13 C NMR. Then they were tested in vitro for antimycobacterial activity against M. tuberculosis H37Rv and several non-tuberculous mycobacterial strains. Several compounds exerted MIC of 3.13-6.25 µg mL-1 ....
Derivatives of 5-alkylpyrazine-2-carboxylic acid as potential anti-infectives
Halířová, Martina ; Zitko, Jan (advisor) ; Kučerová, Marta (referee)
DERIVATIVES OF 5-ALKYLPYRAZINE-2-CARBOXYLIC ACID AS POTENTIAL ANTI-INFECTIVES HALÍŘOVÁ MARTINA Department of Pharmaceutical Chemistry and Drug Analysis, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic In our previous study, we have demonstrated that 5-alkylamino-N- phenylpyrazine-2-carboxamides with longer alkyl chain (C5-C8) exerted micromolar growth inhibition activity against M. tuberculosis H37Rv. We speculated that the long alkylamino chain could facilitate the penetration of lipophilic mycobacterial cell envelope. To test this hypothesis, we performed the amino to methylene isosteric exchange and designed a series of 5-alkyl-N-phenylpyrazine-2-carboxamides. 5- Alkylpyrazine-2-carboxylic acids (5-Ak-POA) were prepared by homolytic alkylation of commercially available pyrazine-2-carbonitrile by respective alkanoic acid, followed by hydrolysis of the carbonitrile group. Final derivatives were prepared by CDI mediated coupling of 5-Ak-POA with corresponding aniline at RT. Final compounds were described by melting point, elementary analysis, IR spectroscopy and 1 H, 13 C NMR. Then they were tested in vitro for antimycobacterial activity against M. tuberculosis H37Rv and several non-tuberculous mycobacterial strains. Several compounds exerted MIC of 3.13-6.25 µg mL-1 ....
|Preparation and characterization of micro- and nanoparticles with selected drugs
Sosková, Simona ; Bokrová, Jitka (referee) ; Márová, Ivana (advisor)
The presented bachelor thesis is focused on the way to prepare combined micro- and nanoparticles containing some natural extracts with antioxidant effects, ibuprofen as the anti-inflammatory and analgetic agent and clotrimazole as the agent with an antifungal effect. The theoretical part contains an introduction of the methods of liposome preparation and a review of encapsulation techniques, methods of particles characterization, and analysis of active substances content. Furthermore, the yeasts of the genus Candida and the methods of the antimicrobial activity determination are described. The mentioned components were encapsulated into liposomes, alginate and chitosan particles. The antioxidant activity of the extracts was determined spectrophotometrically. The encapsulation effectivity of active substances into particles and the long-term stability of encapsulated components were determined and compared too. The HPLC method was used for measuring of the concentration of drugs and spectrophotometric method was used to quantify the content of polyphenols. Prepared particles were characterized with DLS method (size) and zeta- potential (stability). Finally, antibacterial properties of prepared particles and extracts using the test system Candida glabrata were studied. The antimycotic effect of particles, disturbed liposomes and extracts was compared. Finally, potential utilization of prepared liposomes in a cosmetic or pharmaceutical product is proposed.

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