Farmaceutická fakulta v Hradci Králové
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Poslední příspěvky
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Novel Quinazolinones Active against Multidrug-Resistant Mycobacterium Tuberculosis: Synthesis, Antimicrobial Evaluation, and in Silico Exploration of Penicillin-Binding Protein 1A as a Potential Target
původní článek
open access
vydavatelská verze
2025
,Wiley-VCH-Verl.
,ChemMedChem
,20
(13)
Quinazolinone derivatives have emerged as promising scaffolds in antimicrobial drug discovery. This work focuses on the design, synthesis, and evaluation of novel quinazolinone-based compounds and predicts their potential ...
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Antimicrobial and Antiproliferative Properties of 2-Phenyl-N-(Pyridin-2-yl)acetamides
původní článek
open access
vydavatelská verze
2025
,Blackwell Munksgaard
,Chemical Biology and Drug Design
,105
(1)
Infectious diseases, including bacterial, fungal, and viral, have once again gained urgency in the drug development pipeline after the recent COVID-19 pandemic. Tuberculosis (TB) is an old infectious disease for which ...
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Dexamethasone Acetate-Loaded PLGA Nanospheres Targeting Liver Macrophages
původní článek
open access
vydavatelská verze
2025
,Wiley-VCH-Verl.
,Macromolecular Bioscience
,25
(2)
Glucocorticoids are potent anti-inflammatory drugs, although their use is associated with severe side effects. Loading glucocorticoids into suitable nanocarriers can significantly reduce these undesirable effects. Macrophages ...
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Investigating the Mechanism of Antimycobacterial and Antiproliferative Activity of (E)-N'-Benzylidenepyrazine-2-Carbohydrazides and their Derivatives
původní článek
open access
vydavatelská verze
2025
,Wiley-VCH-Verl.
,ChemMedChem
,20
(18)
A series of 33 (E)-N'-benzylidenepyrazine-2-carbohydrazides and their derivatives were synthesized and tested for biological activity. Benzylidene derivatives with 2-OH substitution on the phenyl ring (18: R = 2-OH, 21: R ...
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The discovery of a new nonbile acid modulator of Takeda G protein-coupled receptor 5: An integrated computational approach
původní článek
open access
vydavatelská verze
2025
,Wiley-VCH-Verl.
,Archiv der Pharmazie
,358
(1)
The Takeda G protein-coupled receptor 5 (TGR5), also known as GPBAR1 (G protein-coupled bile acid receptor), is a membrane-type bile acid receptor that regulates blood glucose levels and energy expenditure. These essential ...
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A new bactericidal chlorinated derivative containing 2-aminooxazole potentiates antibacterial action of colistin against multidrug-resistant acinetobacter baumannii
původní článek
open access
vydavatelská verze
2025
,Springer
,Medical Microbiology and Immunology
,214
(1)
This comprehensive study provides insight into the antibacterial action of a recently published 2-chloro-N-(oxazol-2-yl)isonicotinamide (AB15), intending to assess its potential as a candidate adjuvant molecule to support ...
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Scaffold Hopping in Tuberculosis Drug Discovery: Principles, Applications, and Case Studies
přehledový článek
open access
vydavatelská verze
2025
,ACS Publications
,Journal of Medicinal Chemistry
,68
(20)
Tuberculosis (TB) imposes a major global health challenge, aggravated by the emergence of drug-resistant Mycobacterium tuberculosis (Mtb) strains. Scaffold hopping, a medicinal chemistry approach that modifies the molecular ...
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Advanced polymer nanofibers for the online extraction coupled with liquid chromatography for the determination of emerging fluorinated contaminants in surface water
původní článek
open access
vydavatelská verze
2026
,Elsevier B.V.
,Talanta
,298
(February 2026)
Advanced polyacrylonitrile, polypropylene, polyhydroxybutyrate, polycaprolactone, and poly(vinylidene difluoride) nanofibers, including composite materials containing carbon nanoparticle additives, combined micro/nanofibers, ...
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Effects of prenatal cannabinoid use on the monoamine system in the fetoplacental unit: A systematic review of animal and human studies
přehledový článek
open access
vydavatelská verze
2025
,Elsevier
,Drug and Alcohol Dependence
,268
(March)
Background: The rapid increase in cannabis use during pregnancy - up by 170 % between 2009 and 2016 - raises pressing concerns about its effects on fetal health, particularly on the delicate monoamine system within the ...
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5-(3,5-Dinitrophenyl)-1,3,4-oxadiazol-2-amine derivatives, their precursors, and analogues: Synthesis and evaluation of novel highly potent antitubercular agent
původní článek
open access
postprint
2025
,PLoS One
,20
(5)
Drug resistance is a growing problem for many pathogens, including mycobacteria. Small heterocyclic molecules are among the leading scaffolds for developing potential antimycobacterial agents. Therefore, based on the ...
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Alkaloids from the genus Vinca L. (Apocynaceae): a comprehensive biological and structural review
přehledový článek
open access
vydavatelská verze
2025
,SPRINGER
,Phytochemistry Reviews
,24
(5)
This review provides a comprehensive overview of the alkaloids in the genus Vinca L. (Apocynaceae), which is renowned for its rich content of monoterpene indole alkaloids and widespread occurrence in Europe, northwest ...
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Structural Insights and Functional Impact of the MmpL3 Inhibitor C215
abstrakt v konferenčním sborníku
open access
vydavatelská verze
2024
,Praha
,Česká společnost chemická
,Czech Chemical Society Symposium Series
,22
(6)
Tuberculosis TB is a globally prevalent infectious disease caused by Mycobacterium tuberculosis (Mtb). We developed a straightforward synthesis of C215 and its derivatives and established a basic pharmacological profile.
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Enhancing the Antimycobacterial Efficacy of Pyridine-4-Carbohydrazide: Linkage to Additional Antimicrobial Agents via Oxocarboxylic Acids
původní článek
open access
vydavatelská verze
2025
,Royal Society of Chemistry
,RSC Medicinal Chemistry
,16
(2)
This study evaluates the antimycobacterial potential of novel "mutual" bioactive amides, combining pyridine-4-carbohydrazide (isoniazid, INH) with various antimicrobial agents (sulphonamides, 4-aminosalicylic acid, ...
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Revolutionizing tuberculosis treatment: Breakthroughs, challenges, and hope on the horizon
přehledový článek
open access
preprint
2025
,Acta Pharmaceutica Sinica B
,15
(3)
Tuberculosis (TB), an infectious disease caused by the bacterium Mycobacterium tuberculosis (Mtb), was responsible for the deaths of approximately 1.3 million people in 2022. In addition, 7.5 million new cases of TB have ...
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Cannabidiol disrupts tryptophan metabolism in the human term placenta
původní článek
open access
vydavatelská verze
2024
,Toxicology
,505
(June)
The increasing use of cannabis during pregnancy raises concerns about its impact on fetal development. While cannabidiol (CBD) shows therapeutic promise, its effects during pregnancy remain uncertain. We investigated CBD's ...
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Metformin inhibits OCT3-mediated serotonin transport in the placenta
původní článek
open access
vydavatelská verze
2024
,Biomedicine & Pharmacotherapy
,179
(October)
Proper fetal development requires tight regulation of serotonin concentrations within the fetoplacental unit. This homeostasis is partly maintained by the placental transporter OCT3/SLC22A3, which takes up serotonin from ...
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Developmental expression of catecholamine system in the human placenta and rat fetoplacental unit
původní článek
open access
vydavatelská verze
2024
,Scientific Reports
,14
(1)
Catecholamines norepinephrine and dopamine have been implicated in numerous physiological processes within the central nervous system. Emerging evidence has highlighted the importance of tightly regulated monoamine levels ...
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Geldanamycin, a Naturally Occurring Inhibitor of Hsp90 and a Lead Compound for Medicinal Chemistry
přehledový článek
open access
vydavatelská verze
2024
,Journal of Medicinal Chemistry
,67
(20)
Geldanamycin remains a driver in the medicinal chemistry of heat shock protein 90 (Hsp90) inhibition, even half a century after its original isolation from nature. This Perspective focuses on the properties of the benzoquinone ...
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Lipid Monolayer on Cell Surface Protein Templates Functional Extracellular Lipid Assembly
původní článek
open access
vydavatelská verze
2024
,WILEY-V C H VERLAG GMBH
,Small
,20
(26)
When the ancestors of men moved from aquatic habitats to the drylands, their evolutionary strategy to restrict water loss is to seal the skin surface with lipids. It is unknown how these rigid ceramide-dominated lipids ...
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Rapid method for screening of both calcium and magnesium chelation with comparison of 21 known metal chelators
původní článek
open access
vydavatelská verze
2024
,Journal of Biological Inorganic Chemistry
,29
(7-8)
The aim of this study was to develop an affordable, rapid but sensitive and precise method for determining the degree of chelation of calcium and magnesium ions. Spectrophotometric method using o-cresolphthalein complexone ...
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