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N-Arylsulfonylated C-Homoaporphines as a New Class of Antiplatelet and Antimicrobial Agents.
ACS Med Chem Lett
January 2025
Laboratory of Organic and Medicinal Chemistry, Department of Chemistry, Malaviya National Institute of Technology, Jawaharlal Nehru Marg, Jaipur 302017, India.
A series of novel N-arylsulfonylated C-homoaporphine alkaloids were synthesized under microwave irradiation and evaluated for their antiplatelet and antimicrobial activities. Among the series, compounds , , , , , , , , and demonstrated highly potent (∼3-fold) platelet aggregation inhibitory activity than acetylsalicylic acid (IC = 21.34 μg/mL).
View Article and Find Full Text PDFAnti-furfurative comparison of Kesh Kanti-Herbal Shampoos and synthetic shampoos against Malassezia furfur for dandruff management.
AMB Express
January 2025
Drug Discovery and Development Division, Patanjali Research Foundation, NH-58, Near Bahadrabad, Haridwar, 249405, Uttarakhand, India.
Malassezia furfur is the primary etiological agent of dandruff (Pityriasis capitis). Although herbal shampoos are preferred for their natural, mild ingredients over synthetic counterparts, they are often perceived as less effective in managing flaky scalp conditions or furfuration causing dandruff. The study compares the antifungal efficacy of herbal and synthetic shampoos against M.
View Article and Find Full Text PDFMenthol-based Novel Ultra-Deformable Vesicle: Formulation, Optimization and Evaluation of an Antifungal Drug.
AAPS PharmSciTech
January 2025
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576107, India.
The current study aims to establish a novel ultra-deformable vesicular system to enhance the drug penetration across the skin by preparing the ketoconazole-loaded menthosomes. It was achieved through regular thin-film evaporation & hydration techniques. To examine the effect of formulation parameters on menthosome characteristics, a 2 full factorial design was used using Design-Expert® software.
View Article and Find Full Text PDFMolecular modeling studies, in vitro antioxidant and antimicrobial assay and BSA affinity of novel benzyl-amine derived scaffolds as CYP51B inhibitors.
Mol Divers
December 2024
Institute for Information Technologies, University of Kragujevac, Jovana Cvijica bb, 34000, Kragujevac, Serbia.
New scaffolds derived from benzylamine were prepared, characterized, and tested for their antimicrobial, antioxidant activities and binding interactions with BSA. Structure-activity relationship analysis revealed that compounds incorporating both benzylamine and quinoline or pyridine moieties (specifically 3a and 3d) demonstrated potent antifungal activity, surpassing that of the standard drug Ketoconazole against Penicillium italicum. Molecular docking studies confirmed significant inhibitory activity against the CYP51B enzyme-an essential component of fungal cell walls.
View Article and Find Full Text PDFParacetamol metabolism by endothelial cells - Potential mechanism underlying intravenous paracetamol-induced hypotension.
Pharmacol Res
January 2025
Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 3, Copenhagen N 2200, Denmark. Electronic address:
It was shown previously that a metabolite of acetaminophen (APAP), N-acetyl-p-benzoquinone imine (NAPQI), is a potent vasodilator, which could underlie the hypotension observed when APAP is administered intravenously. However, it is unknown whether APAP metabolism to NAPQI is possible in the vasculature. In this study, we examine the hypothesis that APAP is metabolized by cytochrome P450 enzymes within the endothelium, which may be accelerated in critically ill patients by the presence of elevated myeloperoxidase (MPO).
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