Search Results - "Prchal, Lukáš"
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Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer’s Disease
Published in Journal of medicinal chemistry (22-04-2021)“…The multifactorial nature of Alzheimer’s disease (AD) is a reason for the lack of effective drugs as well as a basis for the development of…”
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2
The Antibacterial Effects of New N-Alkylpyridinium Salts on Planktonic and Biofilm Bacteria
Published in Frontiers in microbiology (20-10-2020)“…An increasing microbial resistance to known antibiotics raises a demand for new antimicrobials. In this study the antimicrobial properties of a series of new N…”
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3
An efficient synthesis and cytotoxic profile of D-ribo-phytosphingosine and its analogues
Published in Tetrahedron (21-08-2023)“…In this paper we describe the efficient synthesis of d-ribo-phytosphingosine and its analogues commencing from the easily available l-erythrose chiron, which…”
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Sertraline as a new potential anthelmintic against Haemonchus contortus: toxicity, efficacy, and biotransformation
Published in Veterinary research (Paris) (11-12-2021)“…Haemonchus contortus is a parasitic nematode of ruminants which causes significant losses to many farmers worldwide. Since the drugs currently in use for the…”
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Albendazole in environment: faecal concentrations in lambs and impact on lower development stages of helminths and seed germination
Published in Environmental science and pollution research international (01-07-2016)“…Albendazole (ABZ), widely used benzimidazole anthelmintic, administered to animals enters via excrements into environment and may impact non-target organisms…”
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Assessing the Anthelmintic Candidates BLK127 and HBK4 for Their Efficacy on Haemonchus contortus Adults and Eggs, and Their Hepatotoxicity and Biotransformation
Published in Pharmaceutics (30-03-2022)“…As a widely distributed parasitic nematode of ruminants, Haemonchus contortus has become resistant to most anthelmintic classes, there has been a major demand…”
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Biotransformation of anthelmintics and the activity of drug-metabolizing enzymes in the tapeworm Moniezia expansa
Published in Parasitology (01-04-2015)“…The sheep tapeworm Moniezia expansa is very common parasite, which affects ruminants such as sheep, goats as well as other species. The benzimidazole…”
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The metabolism of flubendazole and the activities of selected biotransformation enzymes in Haemonchus contortus strains susceptible and resistant to anthelmintics
Published in Parasitology (01-09-2012)“…Haemonchus contortus is one of the most pathogenic parasites of small ruminants (e.g. sheep and goat). The treatment of haemonchosis is complicated because of…”
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9
Reliable reference gene selection for quantitative real time PCR in Haemonchus contortus
Published in Molecular and biochemical parasitology (01-06-2015)“…[Display omitted] •Eleven candidate reference genes were evaluated in Haemonchus contortus adults.•Comparisons were made between sexes, isolates and…”
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Metabolism of drugs and other xenobiotics in giant liver fluke (Fascioloides magna)
Published in Xenobiotica (01-02-2016)“…1. Giant liver fluke Fascioloides magna is a dangerous parasite, which infects herbivores. It was imported to Europe from North America and started to spread…”
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11
Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics
Published in Veterinary parasitology (06-07-2012)“…Drug entry into the body of a helminth is a key factor in the efficacy of anthelmintics. The present project was designed to study the ex vivo uptake and…”
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12
Ivermectin environmental impact: Excretion profile in sheep and phytotoxic effect in Sinapis alba
Published in Ecotoxicology and environmental safety (01-03-2019)“…Ivermectin (IVM), a macrocylic lactone from the avermectin family, is a potent broad-spectrum anthelmintic drug widely used in veterinary as well as human…”
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13
Morphing cholinesterase inhibitor amiridine into multipotent drugs for the treatment of Alzheimer's disease
Published in Biomedicine & pharmacotherapy (01-04-2024)“…The search for novel drugs to address the medical needs of Alzheimer's disease (AD) is an ongoing process relying on the discovery of disease-modifying agents…”
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14
Charged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2022)“…The organophosphorus antidotes, so-called oximes, are able to restore the enzymatic function of acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) via…”
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BODIPY-labelled acetylcholinesterase reactivators can be encapsulated into ferritin nanovehicles for enhanced bioavailability in the CNS
Published in Biomedicine & pharmacotherapy (01-11-2023)“…The BODIPY-labelled oxime reactivator was prepared and used to study its biodistribution into central nervous system. The newly synthesized oxime was found to…”
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The Impact of Dextran Sodium Sulfate-Induced Gastrointestinal Injury on the Pharmacokinetic Parameters of Donepezil and Its Active Metabolite 6- O -desmethyldonepezil, and Gastric Myoelectric Activity in Experimental Pigs
Published in Molecules (Basel, Switzerland) (09-04-2021)“…Gastrointestinal side effects of donepezil, including dyspepsia, nausea, vomiting or diarrhea, occur in 20-30% of patients. The pathogenesis of these…”
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Structure-Guided Design of N -Methylpropargylamino-Quinazoline Derivatives as Multipotent Agents for the Treatment of Alzheimer's Disease
Published in International journal of molecular sciences (23-05-2023)“…Alzheimer's disease (AD) is a complex disease with an unknown etiology. Available treatments, limited to cholinesterase inhibitors and -methyl-d-aspartate…”
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Benzothiazolyl Ureas are Low Micromolar and Uncompetitive Inhibitors of 17β-HSD10 with Implications to Alzheimer's Disease Treatment
Published in International journal of molecular sciences (17-03-2020)“…Human 17β-hydroxysteroid dehydrogenase type 10 is a multifunctional protein involved in many enzymatic and structural processes within mitochondria. This…”
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Development of versatile and potent monoquaternary reactivators of acetylcholinesterase
Published in Archives of toxicology (01-03-2021)“…To date, the only treatments developed for poisoning by organophosphorus compounds, the most toxic chemical weapons of mass destruction, have exhibited limited…”
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Wide-Antimicrobial Spectrum of Picolinium Salts
Published in Molecules (Basel, Switzerland) (11-05-2020)“…Nosocomial infections, which greatly increase morbidity among hospitalized patients, together with growing antibiotic resistance still encourage many…”
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