In this study, eight new omega-(1H-imidazol-1-yl)-N-phenylacetamide and propionamide derivatives having 2,6-dimethyl, 2,6-dichloro, 2-chloro-6-methyl and 2-isopropyl substitutions on N-phenyl ring were synthesized to evaluate anticonvulsant activity against maximal electroshock test. The most active compounds in the series were the derivatives bearing 2-isopropyl and 2,6-dimethyl substituents on N-phenyl ring.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.farmac.2003.07.011 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Acute anticonvulsant effects of dapsone on PTZ- and MES-induced seizures in mice: NLRP3 inflammasome inhibition and Nrf2/HO-1 pathway preservation.
Pharmacol Rep
January 2025
Experimental Medicine Research Center, Tehran University of Medical Sciences, P.O. Box: 13145-784, Tehran, Iran.
Background: Epilepsy, a neurological disorder characterized by recurrent seizures, presents considerable difficulties in treatment, particularly when dealing with drug-resistant cases. Dapsone, recognized for its anti-inflammatory properties, holds promise as a potential therapeutic option. However, its effectiveness in epilepsy requires further investigation.
View Article and Find Full Text PDFFlunarizine as a Candidate for Drug Repurposing Against Human Pathogenic Mammarenaviruses.
Viruses
January 2025
Department of Immunology and Microbiology, Scripps Research Institute, La Jolla, CA 92037, USA.
Lassa fever (LF), a viral hemorrhagic fever disease with a case fatality rate that can be over 20% among hospitalized LF patients, is endemic to many West African countries. Currently, no vaccines or therapies are specifically licensed to prevent or treat LF, hence the significance of developing therapeutics against the mammarenavirus Lassa virus (LASV), the causative agent of LF. We used in silico docking approaches to investigate the binding affinities of 2015 existing drugs to LASV proteins known to play critical roles in the formation and activity of the virus ribonucleoprotein complex (vRNP) responsible for directing replication and transcription of the viral genome.
View Article and Find Full Text PDFSpinorphin Molecules as Opportunities for Incorporation into Spinorphin@AuNPs Conjugate Systems for Potential Sustained Targeted Delivery to the Brain.
Pharmaceuticals (Basel)
January 2025
Institute of Neurobiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.
This study explores the potential for the synthesis of peptide nanosystems comprising spinorphin molecules (with rhodamine moiety: Rh-S, Rh-S5, and Rh-S6) conjugated with nanoparticles (AuNPs), specifically peptide Rh-S@AuNPs, peptide Rh-S5@AuNPs, and peptide Rh-S6@AuNPs, alongside a comparative analysis of the biological activities of free and conjugated peptides. The examination of the microstructural characteristics of the obtained peptide systems and their physicochemical properties constitutes a key focus of this study. Zeta (ζ) potential, Fourier transformation infrared (FTIR) spectroscopy, circular dichroism (CD), scanning electron microscopy (SEM-EDS), transmission electron microscopy (TEM), and UV-Vis spectrophotometry were employed to elucidate the structure-activity correlations of the peptide@nano AuNP systems.
View Article and Find Full Text PDFAnticonvulsant Effects of Synthetic -(3-Methoxybenzyl)oleamide and -(3-Methoxybenzyl)linoleamide Macamides: An In Silico and In Vivo Study.
Molecules
January 2025
Escuela Profesional de Farmacía y Bioquímica, Universidad Católica de Santa María, Urb. San José s/n, Umacollo, Arequipa 04000, Peru.
Epilepsy is a chronic neurological disorder that affects nearly 50 million people worldwide. Experimental evidence suggests that epileptic neurons are linked to the endocannabinoid system and that inhibition of the FAAH enzyme could have neuroprotective effects by increasing the levels of endogenous endocannabinoid anandamide. In this context, the use of macamides as therapeutic agents in neurological diseases has increased in recent years.
View Article and Find Full Text PDFPinelliae Rhizoma: a systematic review on botany, ethnopharmacology, phytochemistry, preclinical and clinical evidence.
Chin J Nat Med
January 2025
Macao Centre for Research and Development in Chinese Medicine, State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao SAR 999078, China. Electronic address:
Pinelliae Rhizoma (PR), known as Banxia in Chinese, Hange in Japanese, and Banha in Korean, is a renowned herbal medicine in East Asia derived from the dry tuber of Pinellia ternata (Thunb.) Breit. (PT).
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!