The synthesis and antioxidant, antinociceptive and antiedematogenic activities of sulfonamides derived from carvacrol-a druglike natural product-are reported. The compounds showed promising antioxidant activity, and sulfonamide derived from morpholine () demonstrated excellent antinociceptive and antiedematogenic activities, with no sedation or motor impairment. The mechanism that underlies the carvacrol and derived sulfonamides' relieving effects on pain has not yet been fully elucidated, however, this study shows that the antinociceptive activity can be partially mediated by the antagonism of glutamatergic signaling. Compound presented promising efficacy and was predicted to have an appropriate medicinal chemistry profile. Thus, derivative is an interesting starting point for the design of new leads for the treatment of pain and associated inflammation and prooxidative conditions.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8650121 | PMC |
http://dx.doi.org/10.3389/fphar.2021.788850 | DOI Listing |
Neurochem Res
January 2025
Wuxi School of Medicine, Jiangnan University, Wuxi, 214122, China.
Trehalose has neuroprotective effects in neurodegenerative diseases. This study aimed to explore the impact of trehalose on traumatic brain injury (TBI) by investigating its role in neuroprotection. The TBI mice model was established utilizing the cortical impact technique followed by trehalose treatment.
View Article and Find Full Text PDFFish Physiol Biochem
January 2025
Department of Biological Sciences, College of Science, University of Jeddah, P.O. Box 80327, Jeddah 21589, Saudi Arabia.
High cadmium (Cd) concentrations pose a threat to aquatic life globally. This study examined the efficiency of adding purslane (Portulaca oleracea L.) leaf powder (PLP) to Oreochromis niloticus diets on Cd's negative effects.
View Article and Find Full Text PDFNat Prod Res
January 2025
Department of Medical Microbiology, Faculty of Medicine, Erciyes University, Kayseri, Turkey.
Drone larvae (DL) has many biological activities thanks to the bioactive components it contains, but there are very few studies on its antimicrobial activity. The aim of this research was to determine the antifungal activity of DL (raw and lyophilised) water and ethanol extracts against fluconazole (FLU) sensitive and resistant yeast strains. The 87 fungal strains obtained from clinical samples were identified by phenotypic and molecular methods, and broth microdilution test was used for antifungal activity.
View Article and Find Full Text PDFPest Manag Sci
January 2025
Laboratorio de Bioproducción, Bioinsumos, INIA Las Brujas, Canelones, Uruguay.
Background: Biological control methods involving entomopathogenic fungi like Beauveria bassiana have been shown to be a valuable approach in integrated pest management as an environmentally friendly alternative to control pests and pathogens. Identifying genetic determinants of pathogenicity in B. bassiana is instrumental for enhancing its virulence against insects like the resistant soybean pest Piezodorus guildinii.
View Article and Find Full Text PDFChemistryOpen
January 2025
Department of Chemistry, Faculty of Sciences, University of Guilan, Rasht, 4193833697, Iran.
The inhibition of acetylcholinesterase (AChE), an enzyme responsible for the inactivation and decrease in acetylcholine in the cholinergic pathway, has been considered an attractive target for small-molecule drug discovery in Alzheimer's disease (AD) therapy. In the present study, a series of TZD derivatives were designed, synthesized, and studied for drug likeness, blood-brain barrier (BBB) permeability, and adsorption, distribution, metabolism, excretion, and toxicity (ADMET). Additionally, docking studies of the designed compounds were performed on AChE.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!