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Design of ()-3-(5-Thienyl)carboxamido-2-aminopropanoic Acid Derivatives as Novel NMDA Receptor Glycine Site Agonists: Variation in Molecular Geometry to Improve Potency and Augment GluN2 Subunit-Specific Activity.
J Med Chem
January 2025
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, DK-2100, Denmark.
NMDA receptor ligands have therapeutic potential in neurological and psychiatric disorders. We designed ()-3-(5-thienyl)carboxamido-2-aminopropanoic acid derivatives with nanomolar agonist potencies at NMDA receptor subtypes (GluN12/A-D). These compounds are superagonists at GluN1/2C compared to glycine and partial to full agonists at GluN1/2A and GluN1/2D but display functional antagonism at GluN1/2B due to low agonist efficacy.
View Article and Find Full Text PDFCharacterization, Identification, and Biosafety Evaluation of Multifaceted Traits of Plant Growth-Promoting Endophytes for Ameliorating Productivity of Forage Sorghum.
Curr Microbiol
January 2025
School of Organic Farming, Punjab Agricultural University, Ludhiana, 141004, India.
Endophytes are bacteria that inhabit host plants for most of their life cycle without causing harm. In the study, 15 endophytic bacteria were isolated from 30 forage Sorghum plants and assessed for various plant growth-promoting (PGP) traits, such as phosphate solubilization, 1-aminocyclopropane-1-carboxylic acid (ACC) deaminase activity, ammonia production, siderophore production, gibberellic acid production, Indole-3-acetic acid (IAA) production, and zinc solubilization. One isolate, JJG_Zn, demonstrated multiple PGP activities and was identified as Enterobacter sp.
View Article and Find Full Text PDFEvaluation of Drug-Polymer and Drug-Drug Interaction in Cellulosic Multi-Drug Delivery Matrices.
Methods Protoc
January 2025
Department of Pharmacy and Biomedical Sciences, University of Central Lancashire, Preston PR1 2HE, UK.
Multi-drug delivery systems have gained increasing interest from the pharmaceutical industry. Alongside this is the interest in amorphous solid dispersions as an approach to achieve effective oral delivery of compounds with solubility-limited bioavailability. Despite this, there is limited information regarding predicting the behavior of two or more drugs (in amorphous forms) in a polymeric carrier and whether molecular interactions between the compounds, between each compound, and if the polymer have any effect on the physical properties of the system.
View Article and Find Full Text PDF1,2,3-Triazole-tethered fluoroquinolone analogues with antibacterial potential: synthesis and cytotoxicity investigations.
RSC Adv
January 2025
Department of Medicinal Chemistry, Institute of Medical Sciences, Banaras Hindu University Varanasi UP-221005 India
The antibacterial efficacy of some newly developed bis- and C3-carboxylic moieties of fluoroquinolone-linked triazole conjugates was studied. Twenty compounds from two different series of triazoles were synthesized using click chemistry and evaluated for their antibacterial activity against a Gram-positive strain, (ATCC29212), and its clinical isolate and a Gram-negative bacterial strain, (ATCC25922), and its clinical isolate. Among the compounds, 7, 9a, 9d, 9i, 10(a-d), and 10i showed excellent activity with MIC values of up to 6.
View Article and Find Full Text PDFSynthesis, X-Ray Structure, Characterization, Antifungal Activity, DFT, and Molecular Simulation of a Novel Pyrazole Carboxylic Acid.
Curr Top Med Chem
January 2025
Laboratory of Analytical and Molecular Chemistry, Faculty of Sciences Ben M'Sik, Hassan II University of Casablanca, B. P 7955 Casablanca, Morocco.
Background: The search for new antifungal agents is critical due to the rising resistance of fungal pathogens to existing treatments. This study focuses on the synthesis and evaluation of a novel compound, 1-benzyl-5-methyl-1H-pyrazole-3-carboxylic acid (compound L1), as a potential antifungal agent.
Methods: Compound L1 was synthesized and characterized using a range of analytical techniques, including 1H^1H1H NMR, 13C^{13}C13C NMR, FT-IR, GC-MS, and X-ray single crystal diffraction (XRD).
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