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Discovery of pyrazoline analogs as multi-targeting cholinesterase, β-secretase and Aβ aggregation inhibitors through lead optimization strategy.
Int J Biol Macromol
January 2025
Pharmaceutical Chemistry Research Laboratory I, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, India. Electronic address:
The multi-target directed ligands (MTDLs) strategy has been evolved as the propitious approach for the development of therapeutics for Alzheimer's disease (AD). In an earlier report, we described the novel series of chalcone derivatives bearing N-aryl piperazine scaffold as MTDLs for the treatment of AD. Herein, we report the lead optimization of the series culminating in potent, multi-targeting compounds (32-57), evaluated through in-vitro and in-vivo biological studies.
View Article and Find Full Text PDFExperimental 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 PDFPotential induction of apoptosis and acetylcholinesterase inhibition in Aedes mosquitoes by Streptomyces-derived ethyl acetate extract.
Trop Biomed
December 2024
Tropical Infectious Diseases Research and Education Centre (TIDREC), Higher Institution Centre of Excellence, Universiti Malaya, 50603, Kuala Lumpur, Malaysia.
The use of Streptomyces secondary metabolites for mosquito control has recently received positive attention. Accordingly, this study was performed to elucidate the cellular, genomic and biochemical responses of Aedes mosquitoes to Streptomyces sp. KSF103 ethyl acetate (EA) extract, a mixture previously characterized for its potential bioactivity.
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 PDFEvaluating the antioxidant, anti-inflammatory, and neuroprotective potential of fruiting body and mycelium extracts from edible yellow morel (Morchella esculenta L. Pers.).
J Food Sci
January 2025
Department of Biosciences, COMSATS University Islamabad (CUI), Park Road, Islamabad, Pakistan.
Scope: This study aimed to assess the antioxidant, anti-inflammatory, and acetylcholinesterase activities of fruiting bodies (FB) and mycelium (M) extracts of Morchella esculenta L. collected from various regions of Pakistan. The samples included Skardu fruiting body (SKFB) and mycelia Skardu (SKM), Malam Jaba fruiting body (MJFB) and Malam Jaba mycelia (MJM), Krair Mansehra fruiting body (KMFB) and Krair Mansehra mycelia (KMM), and Thandiani fruiting body (TFB) and Thandiani mycelia (TM).
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