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Experimental and computational analysis of lipophilicity and plasma protein binding properties of potent tacrine based cholinesterase inhibitors.
J Chromatogr B Analyt Technol Biomed Life Sci
January 2025
University of Belgrade-Institute of Chemistry, Technology and Metallurgy, Department of Chemistry, Njegoševa 12, 11000 Belgrade, Republic of Serbia. Electronic address:
The lipophilicity of thirteen tacrine/piperidine-4-carboxamide derivatives was assessed using reversed-phase thin-layer chromatography (RP-TLC) with MeOH and acetonitrile (ACN) as organic modifiers. Among the parameters evaluated, the R and C values obtained using MeOH were identified as the most reliable for characterizing the lipophilicity of the investigated compounds. The observed differences in lipophilicity among the derivatives resulted from a delicate interplay of substituent effects (hydrophobicity, polarity, steric hindrance, and electronic effects), positional influence, and characteristics of the organic modifier.
View Article and Find Full Text PDFIN SILICO AND IN VITRO ASSESSMENT OF ANTI-Leishmania infantum ACTIVITY OF A NOVEL CYCLOHEXYL-1,2,4-OXADIAZOLE DERIVATIVE.
Mol Biochem Parasitol
January 2025
Post-graduate Program in Pharmaceutical Sciences, Federal University of Ceará, Fortaleza - CE, Brazil; Fundação Oswaldo Cruz, Fiocruz, Fiocruz Ceará, Eusébio - CE, Brazil; Northeast Network of Biotechnology (RENORBIO), State University of Ceará (UECE), Fortaleza - CE, Brazil.
Globally, an estimated 1 billion people reside in endemic areas, and over 12 million individuals are infected with leishmaniasis. Despite its prevalence, leishmaniasis continues to be a neglected disease, mainly affecting underdeveloped countries. In Brazil, the available treatments are pentavalent antimonials and Amphotericin B, which are outdated, toxic, require prolonged parenteral administration and have limited efficacy.
View Article and Find Full Text PDFAlkaloid Profile, Anticholinesterase and Antioxidant Activities, and Sexual Propagation in (Amaryllidaceae).
Plants (Basel)
January 2025
Instituto de Biotecnología, Facultad de Ingeniería, Universidad Nacional de San Juan, Av. Libertador General San Martín 1109 (O), San Juan CP5400, Argentina.
, a recently described endemic species from southern Peru, belongs to the Amaryllidaceae family and is known for its diversity of alkaloids. Amaryllidoideae have been studied for their diverse biological activities, particularly for their properties in treating neurodegenerative diseases. This work examines the alkaloidal profile using GC-MS and UPLC-MS/MS of alkaloid-enriched extracts obtained from the leaves and bulbs of and their inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes.
View Article and Find Full Text PDFThiamine and Thiamine Pyrophosphate as Non-Competitive Inhibitors of Acetylcholinesterase-Experimental and Theoretical Investigations.
Molecules
January 2025
Chair and Department of Biochemistry and Pharmacogenomics, Medical University of Warsaw, 1 Banacha Str., 02-097 Warsaw, Poland.
Vitamin B (thiamine) plays an important role in human metabolism. It is essential for the proper growth and development of the body and has a positive effect on the functioning of the digestive, cardiovascular, and nervous systems. Additionally, it stimulates the brain and improves the psycho-emotional state.
View Article and Find Full Text PDFResveratrol-Based Carbamates as Selective Butyrylcholinesterase Inhibitors: Design, Synthesis, Computational Study and Biometal Complexation Capability.
Molecules
January 2025
Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Trg Marka Marulića 19, HR-10 000 Zagreb, Croatia.
Considering our previous experience in the design of new cholinesterase inhibitors, especially resveratrol analogs, in this research, the basic stilbene skeleton was used as a structural unit for new carbamates designed as potentially highly selective butyrylcholinesterase (BChE) inhibitors with excellent absorption, distribution, metabolism, excretion and toxicity ADMET properties. The inhibitory activity of newly prepared carbamates - was tested toward the enzymes acetylcholinesterase (AChE) and BChE. In the tested group of compounds, the leading inhibitors were and , which achieved excellent selective inhibitory activity for BChE with IC values of 0.
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