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View article: Platinum-group metal half-sandwich complexes with C-glucopyranosyl 1,2,3-triazoles and isoxazoles as ligands: synthesis and evaluation as antineoplastic and antimicrobial agents
Platinum-group metal half-sandwich complexes with C-glucopyranosyl 1,2,3-triazoles and isoxazoles as ligands: synthesis and evaluation as antineoplastic and antimicrobial agents Open
Half-sandwich complexes of platinum-group metals are a widely studied subgroup of organometallic compounds with promising anticancer and antimicrobial properties. Recently, we have published a set of polyhapto arene/arenyl Ru(II), Os(II), …
View article: Platinum-group metal half-sandwich complexes of sugar-isoxazol(in)e conjugates – synthesis and evaluation of their antineoplastic and antimicrobial activities
Platinum-group metal half-sandwich complexes of sugar-isoxazol(in)e conjugates – synthesis and evaluation of their antineoplastic and antimicrobial activities Open
Platinum-group metal half-sandwich complexes are considered to be potential replacements of the clinically widely used platins which have several side effects and tend to cause resistance to develop. In our previous works, we used a range …
View article: Regioselective Synthesis of 5-Substituted 3-(β-d-Glycopyranosyl)isoxazoles and -isoxazolines by 1,3-Dipolar Cycloaddition as Potential Anticancer Agents and Glycogen Phosphorylase Inhibitors
Regioselective Synthesis of 5-Substituted 3-(β-d-Glycopyranosyl)isoxazoles and -isoxazolines by 1,3-Dipolar Cycloaddition as Potential Anticancer Agents and Glycogen Phosphorylase Inhibitors Open
Anhydro-aldose oximes were employed to generate in situ nitrile oxides via a halogenation/base-induced elimination sequence in the presence of NCS and Et3N, which were then used in 1,3-dipolar cycloadditions with alkenes and alkynes to aff…
View article: Impact of intense rainfall event on the physicochemical and microbiological characteristics of an urban stream
Impact of intense rainfall event on the physicochemical and microbiological characteristics of an urban stream Open
Extreme weather events, including sudden and intense rainfall, have become increasingly frequent due to the growing impact of climate change. This rapid influx of water often carries a variety of pollutants, including nutrients, heavy meta…
View article: Correlation between NDVI and soil sensor data collected by UAV
Correlation between NDVI and soil sensor data collected by UAV Open
The development of UAVs and the reduction in the weight of payload-bearing devices is making remote sensing of crops possible. This technology is cheaper, more time-efficient and produces higher resolution images in a non-destructive way. …
View article: Water management strategies for lettuce cultivation in soil and soilless systems under controlled conditions
Water management strategies for lettuce cultivation in soil and soilless systems under controlled conditions Open
The growing demand for sustainable food production requires innovative farming techniques that optimise water use and minimise environmental impacts. This experiment tested the cultivation of lettuce (Lactuca sativa L.) in a greenhouse env…
View article: Design and Synthesis of 3-(β-d-Glucopyranosyl)-4-amino/4-guanidino Pyrazole Derivatives and Analysis of Their Glycogen Phosphorylase Inhibitory Potential
Design and Synthesis of 3-(β-d-Glucopyranosyl)-4-amino/4-guanidino Pyrazole Derivatives and Analysis of Their Glycogen Phosphorylase Inhibitory Potential Open
Glycogen phosphorylase (GP) is a key regulator of glucose levels and, with that, an important target for the discovery of novel treatments against type 2 diabetes. β-d-Glucopyranosyl derivatives have provided some of the most potent GP inh…
View article: Glycopyranosylidene-Spiro-Morpholinones: Evaluation of the Synthetic Possibilities Based on Glyculosonamide Derivatives and a New Method for the Construction of the Morpholine Ring
Glycopyranosylidene-Spiro-Morpholinones: Evaluation of the Synthetic Possibilities Based on Glyculosonamide Derivatives and a New Method for the Construction of the Morpholine Ring Open
Glycosylidene-spiro-morpholin(on)es are scarcely described skeletons in the literature. In this work, we have systematically explored the synthetic routes towards such morpholinones based on the reactions of O-peracylated hept-2-ulopyranos…
View article: Examination of compost maturity using reflectance
Examination of compost maturity using reflectance Open
Composting is one of the most popular recycling processes for organic waste. Composting plays an important role in waste and by-product management and is becoming increasingly important in both sustainable energy management and circular ec…
View article: Investigation of a supercell merger leading to the EF4 tornado in the Czech Republic on June 24, 2021 using radar data and numerical model outputs
Investigation of a supercell merger leading to the EF4 tornado in the Czech Republic on June 24, 2021 using radar data and numerical model outputs Open
An unprecedented deadly and destructive EF4 tornado struck the Czech Republic across Břeclav and Hodonín districts on June 24, 2021. On this day, several supercells developed in Central Europe, however, in Austria and the Czech Republic re…
View article: Structure activity relationship of the binding of p-coumaroyl glucose to glycogen phosphorylase and its effect on hepatic cell metabolic pathways
Structure activity relationship of the binding of p-coumaroyl glucose to glycogen phosphorylase and its effect on hepatic cell metabolic pathways Open
The binding of p-coumaroyl glucose to glycogen phosphorylase (GP; a pharmaceutical target for the development of antihyperglycaemic drugs) has been studied by kinetics, and X-ray crystallography while its effect to HepG2 cells metabolism h…
View article: Dual-Target Compounds against Type 2 Diabetes Mellitus: Proof of Concept for Sodium Dependent Glucose Transporter (SGLT) and Glycogen Phosphorylase (GP) Inhibitors
Dual-Target Compounds against Type 2 Diabetes Mellitus: Proof of Concept for Sodium Dependent Glucose Transporter (SGLT) and Glycogen Phosphorylase (GP) Inhibitors Open
A current trend in the quest for new therapies for complex, multifactorial diseases, such as diabetes mellitus (DM), is to find dual or even multi-target inhibitors. In DM, the sodium dependent glucose cotransporter 2 (SGLT2) in the kidney…
View article: Examination and statistical evaluation of physico-chemical parameters of windrow composting
Examination and statistical evaluation of physico-chemical parameters of windrow composting Open
The treatment and utilization of plant and animal waste and by-products from agriculture is very diverse. Traditional environmental management practices for waste management have been retained through soil conservation and the applied of r…
View article: Identification of <i>C</i>-β-<scp>d</scp>-Glucopyranosyl Azole-Type Inhibitors of Glycogen Phosphorylase That Reduce Glycogenolysis in Hepatocytes: <i>In Silico</i> Design, Synthesis, <i>in Vitro</i> Kinetics, and <i>ex Vivo</i> Studies
Identification of <i>C</i>-β-<span>d</span>-Glucopyranosyl Azole-Type Inhibitors of Glycogen Phosphorylase That Reduce Glycogenolysis in Hepatocytes: <i>In Silico</i> Design, Synthesis, <i>in Vitro</i> Kinetics, and <i>ex Vivo</i> Studies Open
Several C-β-d-glucopyranosyl azoles have recently been uncovered as among the most potent glycogen phosphorylase (GP) catalytic site inhibitors discovered to date. Toward further exploring their translational potential, ex vivo experiments…
View article: New syntheses towards <i>C</i>-glycosyl type glycomimetics
New syntheses towards <i>C</i>-glycosyl type glycomimetics Open
Glycomimetics are compounds that resemble carbohydrate molecules in their chemical structure and/or biological effect. A large variety of compounds can be designed and synthesized to get glycomimetics, however, C -glycosyl derivatives repr…
View article: Synthesis of New C- and N-β-d-Glucopyranosyl Derivatives of Imidazole, 1,2,3-Triazole and Tetrazole, and Their Evaluation as Inhibitors of Glycogen Phosphorylase
Synthesis of New C- and N-β-d-Glucopyranosyl Derivatives of Imidazole, 1,2,3-Triazole and Tetrazole, and Their Evaluation as Inhibitors of Glycogen Phosphorylase Open
The aim of the present study was to broaden the structure-activity relationships of C- and N-β-d-glucopyranosyl azole type inhibitors of glycogen phosphorylase. 1-Aryl-4-β-d-gluco-pyranosyl-1,2,3-triazoles were prepared by copper catalyzed…
View article: A multidisciplinary study of 3-(β- d -glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors
A multidisciplinary study of 3-(β- d -glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors Open
3-(β-d-Glucopyranosyl)-5-substituted-1,2,4-triazoles have been revealed as an effective scaffold for the development of potent glycogen phosphorylase (GP) inhibitors but with the potency very sensitive to the nature of the alkyl/aryl 5-sub…
View article: Glucopyranosylidene-Spiro-Thiazolinones: Synthetic Studies and Determination of Absolute Configuration by TDDFT-ECD Calculations
Glucopyranosylidene-Spiro-Thiazolinones: Synthetic Studies and Determination of Absolute Configuration by TDDFT-ECD Calculations Open
Reactions of O-peracylated C-(1-bromo-β-d-glucopyranosyl)formamides with thioamides furnished the corresponding glucopyranosylidene-spiro-thiazolin-4-one. While O-debenzoylations under a variety of conditions resulted in decomposition, dur…
View article: Glycogen phosphorylase inhibition improves beta cell function
Glycogen phosphorylase inhibition improves beta cell function Open
Background and Purpose Glycogen phosphorylase (GP) is the key enzyme for glycogen degradation. GP inhibitors (GPi‐s) are glucose lowering agents that cause the accumulation of glucose in the liver as glycogen. Glycogen metabolism has impli…
View article: Coupling of anhydro-aldose tosylhydrazones with hydroxy compounds and carboxylic acids: a new route for the synthesis of C-β-<scp>d</scp>-glycopyranosylmethyl ethers and esters
Coupling of anhydro-aldose tosylhydrazones with hydroxy compounds and carboxylic acids: a new route for the synthesis of C-β-<span>d</span>-glycopyranosylmethyl ethers and esters Open
Cross couplings of O-peracylated 2,6-anhydro-aldose tosylhydrazones (C-(β-D-glycopyranosyl)formaldehyde tosylhydrazones) with alcohols, phenols, and carboxylic acids were studied under thermic or photolytic conditions in the presence of K3…