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View article: Identification and Characterization of a Small-Molecule Inhibitor of the <i>Pseudomonas aeruginosa</i> SOS Response
Identification and Characterization of a Small-Molecule Inhibitor of the <i>Pseudomonas aeruginosa</i> SOS Response Open
The SOS response is among the most conserved pathways that promote antibiotic resistance onset in bacteria. This study aimed to identify and characterize small-molecule inhibitors of the SOS response in the opportunistic pathogen Pseudo…
View article: New derivatives bearing alkyl phosphonic acid moieties as a promising scaffold against drug-resistant H69AR small cell lung cancer models
New derivatives bearing alkyl phosphonic acid moieties as a promising scaffold against drug-resistant H69AR small cell lung cancer models Open
Small cell lung cancer (SCLC), although less common than non-small cell lung cancer (NSCLC), is an aggressive and lethal form of lung cancer. Even if it was diagnosed and started being treated early, it still contributes to poor survival r…
View article: Synthesis and Biological Evaluation of β-Phenylalanine Derivatives Containing Sulphonamide and Azole Moieties as Antiproliferative Candidates in Lung Cancer Models
Synthesis and Biological Evaluation of β-Phenylalanine Derivatives Containing Sulphonamide and Azole Moieties as Antiproliferative Candidates in Lung Cancer Models Open
In this study, a series of novel β-phenylalanine derivatives were synthesised and evaluated for their anticancer activity. The 3-(4-methylbenzene-1-sulfonamido)-3-phenylpropanoic acid (2) was prepared using β-phenylalanine as a core scaffo…
View article: Synthesis and Characterization of Sulfonamide‐Imidazole Hybrids with In Vitro Antiproliferative Activity against Anthracycline‐Sensitive and Resistant H69 Small Cell Lung Cancer Cells
Synthesis and Characterization of Sulfonamide‐Imidazole Hybrids with In Vitro Antiproliferative Activity against Anthracycline‐Sensitive and Resistant H69 Small Cell Lung Cancer Cells Open
A series of novel sulfonamide‐imidazole hybrid derivatives are synthesized, and their antiproliferative properties are evaluated. The global challenge of cancer, highlighted by rising morbidity and mortality rates, is further intensified b…
View article: Synthesis of novel N-substituted β-amino acid derivatives bearing 2-hydroxyphenyl moieties as promising antimicrobial candidates targeting multidrug-resistant Gram-positive pathogens
Synthesis of novel N-substituted β-amino acid derivatives bearing 2-hydroxyphenyl moieties as promising antimicrobial candidates targeting multidrug-resistant Gram-positive pathogens Open
The increasing prevalence of antimicrobial resistance among ESKAPE group pathogens presents a significant challenge in the healthcare sector, contributing to higher morbidity and mortality rates globally. Thus, it is essential to develop n…
View article: Identification of 3-[(4-Acetylphenyl)(4-Phenylthiazol-2-Yl)Amino]Propanoic Acid Derivatives as Promising Scaffolds for the Development of Novel Anticancer Candidates Targeting SIRT2 and EGFR
Identification of 3-[(4-Acetylphenyl)(4-Phenylthiazol-2-Yl)Amino]Propanoic Acid Derivatives as Promising Scaffolds for the Development of Novel Anticancer Candidates Targeting SIRT2 and EGFR Open
Background: A series of novel polysubstituted thiazole derivatives were synthesized, and their antiproliferative properties were evaluated using both 2D and 3D lung cancer models. Methods: The compounds were obtained via esterification, ox…
View article: Identification and characterization of a small-molecule inhibitor of the <i>Pseudomonas aeruginosa</i> SOS response
Identification and characterization of a small-molecule inhibitor of the <i>Pseudomonas aeruginosa</i> SOS response Open
The SOS response is among the most conserved pathways that promote the acquisition of antibiotic resistance in bacteria. This study aimed to identify and characterize small-molecule inhibitors of the SOS response system in the opportunisti…
View article: 3,3′-((3-Hydroxyphenyl)azanediyl)dipropionic Acid Derivatives as a Promising Scaffold Against Drug-Resistant Pathogens and Chemotherapy-Resistant Cancer
3,3′-((3-Hydroxyphenyl)azanediyl)dipropionic Acid Derivatives as a Promising Scaffold Against Drug-Resistant Pathogens and Chemotherapy-Resistant Cancer Open
The synthesis and antimicrobial and anticancer activity of 3,3′-((3-hydroxyphenyl)azanediyl)dipropionic acid derivatives (2–25) against drug-resistant bacterial pathogens and FaDu head and neck cancer cells were investigated. The derivativ…
View article: Synthesis and In Vitro Anticancer Activity of Pyrrolidone Derivatives Bearing 3,4,5-Trimethoxyphenyl Moiety as a Promising Anticancer Scaffold
Synthesis and In Vitro Anticancer Activity of Pyrrolidone Derivatives Bearing 3,4,5-Trimethoxyphenyl Moiety as a Promising Anticancer Scaffold Open
A series of 5-oxo-1-(3,4,5-trimethoxyphenyl)pyrrolidine-3-carboxylic acid derivatives–hydrazones, N-ethylhydrazones, pyrrole, pyrazole, oxadiazole, and triazole were synthesized and evaluated for their anticancer activity using human A549 …
View article: Synthesis of Novel N-Substituted β-Amino Acid Derivatives Bearing 2-Hydroxyphenyl Moieties as Promising Antimicrobial Candidates Targeting Multidrug-Resistant Gram-Positive Pathogens
Synthesis of Novel N-Substituted β-Amino Acid Derivatives Bearing 2-Hydroxyphenyl Moieties as Promising Antimicrobial Candidates Targeting Multidrug-Resistant Gram-Positive Pathogens Open
The increasing prevalence of antimicrobial resistance among ESKAPE group pathogens presents a significant challenge in the healthcare sector, contributing to higher morbidity and mortality rates globally. Thus, it is essential to develop n…
View article: Synthesis and Antimicrobial Evaluation of 2-[2-(9H-Fluoren-9-ylidene)hydrazin-1-yl]-1,3-thiazole Derivatives
Synthesis and Antimicrobial Evaluation of 2-[2-(9H-Fluoren-9-ylidene)hydrazin-1-yl]-1,3-thiazole Derivatives Open
Fluorenyl-hydrazonothiazole derivatives 2–7 were synthesized by the Hantzsch reaction from 2-(9H-fluoren-9-ylidene)hydrazine-1-carbothioamide (1) and the corresponding α-halocarbonyl compounds in THF or 1,4-dioxane solvent. A base catalyst…
View article: Identification of 3-((4-Hydroxyphenyl)amino)propanoic Acid Derivatives as Anticancer Candidates with Promising Antioxidant Properties
Identification of 3-((4-Hydroxyphenyl)amino)propanoic Acid Derivatives as Anticancer Candidates with Promising Antioxidant Properties Open
Various cancer-associated morbidities remain a growing global health challenge, resulting in a significant burden on healthcare systems worldwide due to high mortality rates and a frequent lack of novel therapeutic options for advanced and…
View article: Multiple roles for hypoxia inducible factor 1-alpha in airway epithelial cells during mucormycosis
Multiple roles for hypoxia inducible factor 1-alpha in airway epithelial cells during mucormycosis Open
During pulmonary mucormycosis, inhaled sporangiospores adhere to, germinate, and invade airway epithelial cells to establish infection. We provide evidence that HIF1α plays dual roles in airway epithelial cells during Mucorales infection. …
View article: Screening of Small-Molecule Libraries Using SARS-CoV-2-Derived Sequences Identifies Novel Furin Inhibitors
Screening of Small-Molecule Libraries Using SARS-CoV-2-Derived Sequences Identifies Novel Furin Inhibitors Open
SARS-CoV-2 is the pathogen responsible for the most recent global pandemic, which has claimed hundreds of thousands of victims worldwide. Despite remarkable efforts to develop an effective vaccine, concerns have been raised about the actua…
View article: Development of rabbit models of ventilator-associated bacterial pneumonia produced by carbapenem-resistant <i>Pseudomonas aeruginosa</i>
Development of rabbit models of ventilator-associated bacterial pneumonia produced by carbapenem-resistant <i>Pseudomonas aeruginosa</i> Open
Ventilator-associated bacterial pneumonia (VABP) is among the most intractable of carbapenem-resistant Gram-negative bacterial infections. New antimicrobial agents are critically needed for the treatment of VABP. However, current conventio…
View article: Exploring the potential of bis(thiazol-5-yl)phenylmethane derivatives as novel candidates against genetically defined multidrug-resistant Staphylococcus aureus
Exploring the potential of bis(thiazol-5-yl)phenylmethane derivatives as novel candidates against genetically defined multidrug-resistant Staphylococcus aureus Open
Antimicrobial resistance (AMR) represents an alarming global challenge to public health. Infections caused by multidrug-resistant Staphylococcus aureus ( S . aureus ) pose an emerging global threat. Therefore, it is crucial to develop nove…
View article: Synthesis of 3-((4-Hydroxyphenyl)amino)propanoic Acid Derivatives as Promising Scaffolds for the Development of Antimicrobial Candidates Targeting Multidrug-Resistant Bacterial and Fungal Pathogens
Synthesis of 3-((4-Hydroxyphenyl)amino)propanoic Acid Derivatives as Promising Scaffolds for the Development of Antimicrobial Candidates Targeting Multidrug-Resistant Bacterial and Fungal Pathogens Open
Infections caused by multidrug-resistant bacterial and fungal pathogens represent a significant global health concern, contributing to increased morbidity and mortality rates. Therefore, it is crucial to develop novel compounds targeting d…
View article: Understanding the Immunomodulatory Effects of Bovine Colostrum: Insights into IL-6/IL-10 Axis-Mediated Inflammatory Control
Understanding the Immunomodulatory Effects of Bovine Colostrum: Insights into IL-6/IL-10 Axis-Mediated Inflammatory Control Open
Bovine colostrum (COL), the first milk secreted by lactating cows postpartum, is a rich source of bioactive compounds that exert a significant role in the survival, growth, and immune development of neonatal calves. This study investigated…
View article: Understanding the Immunomodulatory Effects of Bovine Colostrum: Insights into IL-6/IL-10 Axis-Mediated Inflammatory Control
Understanding the Immunomodulatory Effects of Bovine Colostrum: Insights into IL-6/IL-10 Axis-Mediated Inflammatory Control Open
Bovine colostrum (COL), the first milk secreted by lactating cows postpartum, is a rich source of bioactive compounds that exert significant role on the survival, growth, and immune development of neonatal calves [9,10]. This study investi…
View article: Synthesis and characterization of sulphanilamide and benzimidazole pharmacophores containing γ-amino acid derivatives as dual antimicrobial and anticancer agents
Synthesis and characterization of sulphanilamide and benzimidazole pharmacophores containing γ-amino acid derivatives as dual antimicrobial and anticancer agents Open
A series of -amino acid derivatives with sulfanilamide and benzimidazole pharmacophores in the structures were synthesized and evaluated for antibacterial and anticancer activity.Hydrazones with 5-nitrofur-2-yl and 5-nitrothien-2-yl moiet…
View article: Synthesis of 1-(2-Hydroxyphenyl)- and (3,5-Dichloro-2-hydroxyphenyl)-5-oxopyrrolidine-3-carboxylic Acid Derivatives as Promising Scaffolds for the Development of Novel Antimicrobial and Anticancer Agents
Synthesis of 1-(2-Hydroxyphenyl)- and (3,5-Dichloro-2-hydroxyphenyl)-5-oxopyrrolidine-3-carboxylic Acid Derivatives as Promising Scaffolds for the Development of Novel Antimicrobial and Anticancer Agents Open
Increasing antimicrobial resistance among Gram-positive pathogens and pathogenic fungi remains one of the major public healthcare threats. Therefore, novel antimicrobial candidates and scaffolds are critically needed to overcome resistance…
View article: Synthesis of Novel Benzenesulfonamide-Bearing Functionalized Imidazole Derivatives as Novel Candidates Targeting Multidrug-Resistant Mycobacterium abscessus Complex
Synthesis of Novel Benzenesulfonamide-Bearing Functionalized Imidazole Derivatives as Novel Candidates Targeting Multidrug-Resistant Mycobacterium abscessus Complex Open
Infections caused by drug-resistant (DR) Mycobacterium abscessus (M. abscessus) complex (MAC) are an important public health concern, particularly when affecting individuals with various immunodeficiencies or chronic pulmonary diseases. Ra…
View article: The Influence of Feeding with Colostrum and Colostrum Replacer on Major Blood Biomarkers and Growth Performance in Dairy Calves
The Influence of Feeding with Colostrum and Colostrum Replacer on Major Blood Biomarkers and Growth Performance in Dairy Calves Open
Bovine colostrum (BC) is the first milk produced by lactating cows after parturition. BC is rich in various amino acids, proteins, and fats essential for the nutrition of the neonate calves. Despite the evident beneficial effect of BC on c…
View article: Synthesis and Development of N-2,5-Dimethylphenylthioureido Acid Derivatives as Scaffolds for New Antimicrobial Candidates Targeting Multidrug-Resistant Gram-Positive Pathogens
Synthesis and Development of N-2,5-Dimethylphenylthioureido Acid Derivatives as Scaffolds for New Antimicrobial Candidates Targeting Multidrug-Resistant Gram-Positive Pathogens Open
The growing antimicrobial resistance to last-line antimicrobials among Gram-positive pathogens remains a major healthcare emergency worldwide. Therefore, the search for new small molecules targeting multidrug-resistant pathogens remains of…
View article: Efficacy of Cefiderocol in Experimental Stenotrophomonas maltophilia Pneumonia in Persistently Neutropenic Rabbits
Efficacy of Cefiderocol in Experimental Stenotrophomonas maltophilia Pneumonia in Persistently Neutropenic Rabbits Open
Stenotrophomonas maltophilia is an important cause of pneumonia in immunocompromised patients. Cefiderocol is a parenteral siderophore cephalosporin with potent in vitro activity against S. maltophilia .
View article: Molecular Epidemiology of Group B Streptococci in Lithuania Identifies Multi-Drug Resistant Clones and Sporadic ST1 Serotypes Ia and Ib
Molecular Epidemiology of Group B Streptococci in Lithuania Identifies Multi-Drug Resistant Clones and Sporadic ST1 Serotypes Ia and Ib Open
Streptococcus agalactiae (Group B Streptococcus, GBS) is a leading cause of neonatal infections. Yet, detailed assessment of the genotypic and phenotypic factors associated with GBS carriage, mother-to-baby transmission, and GBS infection …
View article: Low Anterior Resection Syndrome: What Have We Learned Assessing a Large Population?
Low Anterior Resection Syndrome: What Have We Learned Assessing a Large Population? Open
Our goal was to assess the rate of symptoms commonly included in LARS score in a large general population. The study was based on a population-based design. We disseminated LARS scores through community online platforms and general practit…
View article: Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity
Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity Open
The 1-(4-acetamidophenyl)-5-oxopyrrolidine carboxylic acid was applied for synthesizing derivatives bearing azole, diazole, and hydrazone moieties in the molecule. Modification of an acetamide fragment to the free amino group afforded comp…
View article: Mechanistic Insights to Combating NDM- and CTX-M-Coproducing Klebsiella pneumoniae by Targeting Cell Wall Synthesis and Outer Membrane Integrity
Mechanistic Insights to Combating NDM- and CTX-M-Coproducing Klebsiella pneumoniae by Targeting Cell Wall Synthesis and Outer Membrane Integrity Open
Metallo-β-lactamase (MBL)-producing Gram-negative bacteria cause infections associated with high rates of morbidity and mortality. Currently, a leading regimen to treat infections caused by MBL-producing bacteria is aztreonam combined with…
View article: Synthesis of Novel Aminothiazole Derivatives as Promising Antiviral, Antioxidant and Antibacterial Candidates
Synthesis of Novel Aminothiazole Derivatives as Promising Antiviral, Antioxidant and Antibacterial Candidates Open
It is well-known that thiazole derivatives are usually found in lead structures, which demonstrate a wide range of pharmacological effects. The aim of this research was to explore the antiviral, antioxidant, and antibacterial activities of…