A5074806923- Drug Transport and Resistance Mechanisms
- Synthesis and biological activity
- Radiopharmaceutical Chemistry and Applications
- Synthesis and Biological Evaluation
- Chemical synthesis and alkaloids
- Cholinesterase and Neurodegenerative Diseases
- Phenothiazines and Benzothiazines Synthesis and Activities
- Pregnancy and Medication Impact
- Pneumocystis jirovecii pneumonia detection and treatment
- Tuberculosis Research and Epidemiology
- HIV/AIDS drug development and treatment
- Computational Drug Discovery Methods
- Cancer therapeutics and mechanisms
- Pharmacogenetics and Drug Metabolism
- Hepatitis B Virus Studies
- Pharmacological Effects and Toxicity Studies
- Neuroendocrine Tumor Research Advances
- Antimicrobial agents and applications
- Hops Chemistry and Applications
- Economic and Fiscal Studies
- Quinazolinone synthesis and applications
- Multicomponent Synthesis of Heterocycles
- Protein purification and stability
- Peptidase Inhibition and Analysis
- HER2/EGFR in Cancer Research
Charles University
2010-2020
University of Hradec Králové
2020
University of Vienna
2009
Alzheimer´s disease (AD) is a progressive neurodegenerative dementia which currently represents one of the biggest threats for human kind. The cure still unknown and various hypotheses (cholinergic, amyloidal, oxidative, vascular etc.) are investigated in order to understand pathophysiology on this basis find an effective treatment. Tacrine, first approved drug AD treatment, has been reported be multitargeted drug, however it was withdrawn from market particularly due its hepatotoxicity. Its...
The development of novel antimicrobial agents represents a timely research topic. Eighteen salicylanilide 4-(trifluoromethyl)benzoates were evaluated against Mycobacterium tuberculosis, M. avium and kansasii, eight bacterial strains including methicillin-resistant Staphylococcus aureus (MRSA) for the inhibition mycobacterial isocitrate lyase. Some compounds further screened drug-resistant tuberculosis their cytotoxicity. Minimum inhibitory concentrations (MICs) all within 0.5–32 μmol/L, with...
Background and Purpose The organic cation transporter 1 (OCT1) transports cationic drugs into hepatocytes. high hepatic expression of OCT1 is controlled by the HNF4α USF transcription factors. Pregnane X receptor (PXR) mediates induction principal xenobiotic metabolizing enzymes transporters in liver. Here, we have assessed down‐regulation PXR activation. Experimental Approach We used primary human hepatocytes related cell lines to measure activity, assaying MPP + accumulation. Western...
5-Chloropyrazinamide (5-Cl-PZA) is an inhibitor of mycobacterial fatty acid synthase I with a broad spectrum antimycobacterial activity in vitro. Some N-phenylpyrazine-2-carboxamides different substituents on both the pyrazine and phenyl core possess significant vitro against Mycobacterium tuberculosis. To test structures combining 5-Cl-PZA anilide motifs series thirty 5-chloro-N-phenylpyrazine-2-carboxamides various R ring were synthesized screened M. tuberculosis H37Rv, kansasii two...
Entecavir (ETV) is one of the most potent agents for treatment hepatitis B viral infection. The drug principally eliminated by kidney. goal this study was to investigate potential ETV interact in vitro with renal SLC transporters hOAT1, hOCT2, hCNT2 and hCNT3. Potential drug-drug interactions at antiviral drugs known be excreted kidney (adefovir, tenofovir, cidofovir) as well transporter-dependent cytotoxicity were also examined. Interactions selected along studied several...
1. Some flavonoids contained in the common diet have been shown to interact with important membrane uptake transporters, including organic anion transporting polypeptides (OATPs). OATP2B1 and OATP1A2 expressed apical of human enterocytes may significantly contribute intestinal absorption drugs, e.g. statins. This study is aimed at an evaluation inhibitory potency selected food honey (namely galangin, myricetin, pinocembrin, pinobanksin, chrysin fisetin) toward hOATP2B1 hOATP1A2 as well...
Amphotericin B (AmB) is excreted via the renal excretion route. This process may result in nephrotoxicity. However, relevant information on precise mechanisms not available. The aim of study was to analyze possible interaction AmB or its prodrug deoxycholate (AmB-DOC) with typical organic anion transporters (OATs) and cation (OCTs), using cellular organ models. transport systems were then investigated terms drug-drug interactions AmB-DOC antivirals that might potentially be used...
This work presents synthesis and antimicrobial evaluation of nineteen 6-alkylamino-N-phenylpyrazine-2-carboxamides. Antimycobacterial activity was determined against Mycobacterium tuberculosis H37Rv, M. kansasii two strains avium. Generally, the antimycobacterial increased with prolongation simple alkyl chain culminated in compounds heptylamino substitution (3e, 4e) MIC = 5-10 μm H37Rv. On contrary, derivatives modified (containing e.g. terminal methoxy or hydroxy group) as well...
Abstract A new series of hybrid compounds were designed, consisting anti-AChE and BuChE activity components with an anti-inflammatory component. 9-amino-1,2,3,4-tetrahydroacridine indomethacin derivatives synthesized. All created using alkyldiamine different chain lengths as a linker. Various biological activities evaluated, including inhibitory against AChE BuChE. The tested showed high cholinesterases. IC 50 values for all ranging from 10 nM to 7 µM. potency inhibition was much higher than...
Monoclonal antibodies are used in the therapy of various diseases. Thanks to their high specific uptake target tissues, these can be utilized targeted radioimmunotherapy as carriers radioisotopes tumors. However, important characteristics such binding and stability organism may affected by structural parameters. This study has focused on potential influence selected chelators radiochemical quality vitro receptor capacity two modified monoclonal antibodies—cetuximab panitumumab, both ligands...
In vivo metabolism of the radiolabelled receptor‐specific peptides has been described; however, information regarding pharmacokinetic behaviour degradation products within body is very scarce. The present study was designed to obtain new knowledge on disposition and elimination low‐molecular radiometabolites in organism reveal potential involvement selected membrane transport mechanisms cellular uptake radiometabolites, especially kidney. compared pharmacokinetics two radiometabolites: a...