ArticleEuropean journal of drug metabolism and pharmacokinetics2017
Pharmacokinetic Studies of Oxathio-Heterocycle Fused Chalcones.
Article in European journal of drug metabolism and pharmacokinetics, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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Who cites it
4 citing papers in PubMed, 12 citations in OpenAlex.
- Pharmacokinetic evaluation of Chalcone derivatives with antimalarial activity in New Zealand White Rabbits.BMC research notes · 2021Article
- An overview of the potential anticancer properties of cardamonin.Exploration of targeted anti-tumor therapy · 2020Review
- Biocatalytic hydrogenation of the C=C bond in the enone unit of hydroxylated chalcones-process arising from cyanobacterial adaptations.Applied microbiology and biotechnology · 2018Article
- Highly effective, regiospecific reduction of chalcone by cyanobacteria leads to the formation of dihydrochalcone: two steps towards natural sweetness.Microbial cell factories · 2017Article
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectivesChalcone constitutes one of the most used molecular frameworks in medicinal chemistry and its derivatives exhibit a broad spectrum of biological activities. Low absolute bioavailability, poor distribution, intensive metabolism and elimination of chalcones are the main problems in designing new drugs based on their structure. One of the fundamental steps in evaluation of drug candidates is a comparative analysis of pharmacokinetic parameters. The aim of the studies was the pharmacokinetic characterization of the selected oxathio-heterocycle fused chalcones.
methodsThe pharmacokinetic parameters of 19 compounds were reported. The analyzed chalcones were examined after a single intravenous administration to forty 7-week-old mature male rats of Wistar stock. Pharmacokinetic analysis was performed independently using SHAM (slopes, highest, amounts, and moments) and the two-compartment model. Basic physiochemical parameters were calculated. The bioanalytical methods were validated in terms of repeatability, linearity, accuracy, precision, and selectivity.
resultsThe pharmacokinetics of the examined group of chalcones are compatible with the two-compartment model. The physicochemical characteristics of this group are quite homogeneous. The kinetics of the examined chalcones are indicative of a distribution to the tissue compartment with the predominance of a rate constant from central to peripheral compartments (k
conclusionsThe presented group of compounds may form a starting point for studies into drugs treating autoimmune diseases of the gastro-intestinal tract.
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