6-Acyldecahydro [1,6]naphthyridines were synthesized as derivatives of matrine-type and allomatrine-type alkaloids, and the structure-activity relations were examined by the acetic acid-induced abdominal contraction test. All synthesized derivatives produced the antinociception in mice. The antinociceptive potencies of 15a-c and 16a-c were lower than those of 17a-c, 18a-c, 19a-c and 20a-c. Furthermore, those of the matrine-type derivatives 17b and 17c are greater than other derivatives. These findings suggest that less hindered tertiary amine and highly lipophilic acyl group are better functional groups for the greater antinociceptive potencies. Furthermore, these findings suggest that A or B ring of 1 and 2 are not essential for the antinociceptive effect.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1248/yakushi.123.337 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Colorimetric Detection of Naphthalene Enabled by Intra- to Intermolecular Charge Transfer Interplay Induced by π-hole···π Interactions of a TPA-Attached Pyrazinacene.
Chemistry
January 2025
Shibaura Institute of Technology: Shibaura Kogyo Daigaku, Applied Chemistry, Fukasaku 307, Minuma-ku, 337-8570, Saitama, JAPAN.
A new Donor-Acceptor type pyrazinacene derivative (1) featuring strong ICT was synthesized by linking electron-donating triphenylamine (TPA) and electron-accepting CN groups via a pyrazinacene core. The compound exhibits a dramatic color change from greenish blue to red-violet upon selective recognition of naphthalene (3) to form a 1:1 co-crystal (1•3). This color change is induced by intermolecular CT between pyrazinacene and naphthalene's aromatic moieties, driven by π-hole···π interactions.
View Article and Find Full Text PDFPolymer-Free Electrospinning of β-Cyclodextrin-Oligolactide for Magnolol and Honokiol Pharmaceutical Formulations.
Pharmaceutics
January 2025
Faculty of Pharmacy, "Grigore. T. Popa" University of Medicine and Pharmacy, 700115 Iasi, Romania.
Magnolol (MG) and honokiol (HK) are bioactive compounds extracted from and trees with significant pharmacological properties, including antioxidant and antibacterial activity. However, their poor water solubility and low bioavailability limit the therapeutic potential. To address these limitations, this study aims to develop MG and HK formulations by co-electrospinning using custom-synthesized β-cyclodextrin-oligolactide (β-CDLA) derivatives.
View Article and Find Full Text PDFCurcumin-Based Nanoparticles: Advancements and Challenges in Tumor Therapy.
Pharmaceutics
January 2025
Université de Lorraine, F-54000 Nancy, France.
Curcumin, a bioactive compound derived from the rhizome of L., has garnered significant attention for its potent anticancer properties. Despite its promising therapeutic potential, its poor bioavailability, rapid metabolism, and low water solubility hinder curcumin's clinical application.
View Article and Find Full Text PDFL-Threonine-Derived Biodegradable Polyurethane Nanoparticles for Sustained Carboplatin Release.
Pharmaceutics
December 2024
Department of Polymer Science and Engineering, Pusan National University, Busan 46241, Republic of Korea.
The use of polymeric nanoparticles (NPs) in drug delivery systems offers the advantages of enhancing drug efficacy and minimizing side effects; In this study, L-threonine polyurethane (LTPU) NPs have been fabricated by water-in-oil-in-water emulsion and solvent evaporation using biodegradable and biocompatible LTPU. This polymer was pre-synthesized through the use of an amino acid-based chain extender, desaminotyrosyl L-threonine hexyl ester (DLTHE), where urethane bonds are formed by poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) (PLA-PEG-PLA) triblock copolymer and 1,6-hexamethylene diisocyanate (HDI). LTPU is designed to be degraded by hydrolysis and enzymatic activity due to the presence of ester bonds and peptide bonds within the polymer backbone.
View Article and Find Full Text PDFNovel Co-Polyamides Containing Pendant Phenyl/Pyridinyl Groups with Potential Application in Water Desalination Processes.
Polymers (Basel)
January 2025
Centro de Nanotecnología Aplicada, Facultad de Ciencias, Ingeniería y Tecnología, Universidad Mayor, Camino La Pirámide 5750, Huechuraba 8580745, Chile.
This study explores the development and evaluation of a novel series of aromatic co-polyamides featuring diverse pendant groups, including phenyl and pyridinyl derivatives, designed for water desalination membrane applications. These co-polyamides, synthesized with a combination of hexafluoroisopropyl, oxyether, phenyl, and amide groups, exhibited excellent solubility in polar aprotic solvents, thermal stability exceeding 350 °C, and the ability to form robust, flexible films. Membranes prepared via phase inversion demonstrated variable water permeability and NaCl rejection rates, significantly influenced by the pendant group chemistry.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!