Farmaceutická fakulta v Hradci Králové
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METABOLOMIC ANALYSIS OF THE HUMAN PLACENTA REVEALS PERTURBATIONS IN AMINO ACIDS, PURINE METABOLITES, AND SMALL ORGANIC ACIDS IN SPONTANEOUS PRETERM BIRTH
(2024)Spontaneous preterm delivery presents one of the most complex challenges in obstetrics and is a leading cause of perinatal morbidity and mortality. Although it is a common endpoint for multiple pathological processes, the ... -
Pathological shifts in tryptophan metabolism in human term placenta exposed to LPS or poly I:C
(2024)Maternal immune activation during pregnancy is a risk factor for offspring neuropsychiatric disorders. Among the mechanistic pathways by which maternal inflammation can affect fetal brain development and programming, those ... -
N-Pyrazinylhydroxybenzamides as biologically active compounds: a hit-expansion study and antimicrobial evaluation
(2023)Background: The development of novel antimicrobial drugs is an essential part of combatting the uprising of antimicrobial resistance. Proper hit-to-lead development is crucially needed. Methods & results: We present a ... -
Novel sulfonamide derivatives as a tool to combat methicillin-resistant Staphylococcus aureus
(2024)Increasing resistance in Staphylococcus aureus has created a critical need for new drugs, especially those effective against methicillin-resistant strains (methicillin-resistant Staphylococcus aureus [MRSA]). Sulfonamides ... -
Large-Scale Development of Antibacterial Scaffolds: Gentamicin Sulfate-Loaded Biodegradable Nanofibers for Gastrointestinal Applications
(2023)The ever-increasing demands of modern medicine drive the development of novel drug delivery materials. In particular, nanofibers are promising for such materials due to their favorable properties. However, most development ... -
Novel pyrimidine-1,3,4-oxadiazole hybrids and their precursors as potential antimycobacterial agents
(2023)Background: Molecular hybridization and isostery are proven approaches in medicinal chemistry, and as such we used them to design novel compounds that we investigated as potential antimycobacterials to combat drug-resistant ... -
Both Nitro Groups Are Essential for High Antitubercular Activity of 3,5-Dinitrobenzylsulfanyl Tetrazoles and 1,3,4-Oxadiazoles through the Deazaflavin-Dependent Nitroreductase Activation Pathway
(2024)3,5-Dinitrobenzylsulfanyl tetrazoles and 1,3,4-oxadiazoles, previously identified as having high in vitro activities against both replicating and nonreplicating mycobacteria and favorable cytotoxicity and genotoxicity ... -
Fabrication and characterization of new levan@CBD biocomposite sponges as potential materials in natural, non-toxic wound dressing applications
(2023)Wound healing is a complex process; therefore, new dressings are frequently required to facilitate it. In this study, porous bacterial levan-based sponges containing cannabis oil (Lev@CBDs) were prepared and fully ... -
Francisella tularensis Glyceraldehyde-3-Phosphate Dehydrogenase Is Relocalized during Intracellular Infection and Reveals Effect on Cytokine Gene Expression and Signaling
(2023)Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) is known for its multifunctionality in several pathogenic bacteria. Our previously reported data suggest that the GAPDH homologue of Francisella tularensis, GapA, might also ... -
Derivatives of Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Hepatic Stage of Plasmodium berghei Infection In Vitro
(2023)The incidence rate of malaria and the ensuing mortality prompts the development of novel antimalarial drugs. In this work, the activity of twenty-eight Amaryllidaceae alkaloids (1-28) belonging to seven different structural ... -
Natural Alkaloids as Multi-Target Compounds towards Factors Implicated in Alzheimer's Disease
(2023)Alzheimer's disease (AD) is the most common cause of dementia in elderly people; currently, there is no efficient treatment. Considering the increase in life expectancy worldwide AD rates are predicted to increase enormously, ... -
Characterization of a human placental clearance system to regulate serotonin levels in the fetoplacental unit
(2023)Background Serotonin (5-HT) is a biogenic monoamine with diverse functions in multiple human organs and tissues. During pregnancy, tightly regulated levels of 5-HT in the fetoplacental unit are critical for proper placental ... -
Antimycobacterial pyridine carboxamides: From design to in vivo activity
(2023)Tuberculosis is the number one killer of infectious diseases caused by a single microbe, namely Mycobacterium tuberculosis (Mtb). The success rate of curing this infection is decreasing due to emerging antimicrobial ... -
2,6-Disubstituted 7-(naphthalen-2-ylmethyl)-7H-purines as a new class of potent antitubercular agents inhibiting DprE1
(2023)Phenotypic screening of an in-house library of small molecule purine derivatives against Mycobacterium tuberculosis (Mtb) led to the identification of 2-morpholino-7-(naphthalen-2-ylmethyl)-1,7-dihydro-6H-purin-6-one 10 ... -
Novel 4-aminosalicylic acid analogues active against multidrug-resistant tuberculosis
(2022)Spread of drug-resistant Mycobacterium tuberculosis (Mtb.), together with latent tuberculosis (TB), COVID-19 co-infection and increasing prevalence of non-tuberculous mycobacteria (NTM), is a serious threat for public ... -
Development of antimicrobial agents with activity against drug-resistant bacteria
(2022)Tuberculosis (TB) is a widespread infectious disease predominantly caused by Mycobacterium tuberculosis (M. tuberculosis). The discovery and widespread use of antimicrobials effective against TB starting in the middle of ... -
Insight into the Antibacterial Action of Iodinated Imine, an Analogue of Rafoxanide: a Comprehensive Study of Its Antistaphylococcal Activity
(2023)In this study, we have focused on a multiparametric microbiological analysis of the antistaphylococcal action of the iodinated imine BH77, designed as an analogue of rafoxanide. Its antibacterial activity against five ... -
Improving the antimicrobial activity of old antibacterial drug mafenide: Schiff bases and their bioactivity targeting resistant pathogens
(2023)Background: Increasing rates of acquired resistance have justified the critical need for novel antimicrobial drugs. One viable concept is the modification of known drugs. Methods & results: 21 mafenide-based compounds were ... -
Monoterpene indole alkaloids from Vinca minor L. (Apocynaceae): Identification of new structural scaffold for treatment of Alzheimer's disease
(2022)One undescribed indole alkaloid together with twenty-two known compounds have been isolated from aerial parts of Vinca minor L. (Apocynaceae). The chemical structures of the isolated alkaloids were determined by a combination ...