A group of N-phenylacetamide, N-phenylpropanamide and N-benzylamide derivatives bearing 5-membered heterocyclic rings such as pyrazole, 1,2,4-triazole and imidazole rings at omega position were synthesized and their anticonvulsant activity was evaluated in the maximal electroshock test. The results indicated that the 1,2,4-triazole ring leads to superior activity than the pyrazole ring and inserting a CH2 group into the anilide structure leading to N-benzyl derivatives did not change the anticonvulsant activity, but caused a noticeable decrease in duration of action. The most active compound was 2-(1H-1,2,4-triazole-1-yl)-N-(2,6-dimethylphenyl)acetamide.
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http://dx.doi.org/10.1055/s-0031-1296331 | DOI Listing |
Med Chem
January 2025
São Paulo State University - UNESP, School of Pharmaceutical Sciences, Araraquara, São Paulo, Brazil.
Introduction: Epilepsy encompasses numerous syndromes characterized by spontaneous, intermittent, and abnormal electrical activity in the brain. Affecting about 1-2% of the population, it is estimated that approximately 30-40% of patients experience refractory epilepsy, which does not respond to traditional anticonvulsant drugs.
Aims: Therefore, developing novel, safe, and effective antiepileptic drugs remains a medical need.
Alzheimers Res Ther
January 2025
Radiology Department, Second Affiliated Hospital of Shantou University Medical College, Shantou, Guangdong, China.
Background: The imbalance of glutamate (Glu) and gamma-aminobutyric acid (GABA) neurotransmitter system plays a crucial role in the pathogenesis of Alzheimer's disease (AD). Riluzole is a Glu modulator originally approved for amyotrophic lateral sclerosis that has shown potential neuroprotective effects in various neurodegenerative disorders. However, whether riluzole can improve Glu and GABA homeostasis in AD brain and its related mechanism of action remain unknown.
View Article and Find Full Text PDFJAMA Neurol
November 2024
Centre de Recherche du Centre Hospitalier de l'Université de Montréal, Montréal, Québec, Canada.
Importance: How epilepsy may promote cardiovascular disease remains poorly understood.
Objective: To estimate the odds of new-onset cardiovascular events (CVEs) over 6 years in older people with vs without epilepsy, exploring how enzyme-inducing antiseizure medications (EIASMs) and traditional cardiovascular risk factors mediate these odds.
Design, Setting, And Participants: This was a prospective cohort study using the comprehensive cohort of the Canadian Longitudinal Study on Aging (CLSA), with 6 years of follow-up (2015-2021, analysis performed in December 2023).
Cureus
December 2024
Psychiatry, Drexel University College of Medicine, West Reading, USA.
Complex regional pain syndrome (CRPS) is a chronic pain disorder characterized by severe, disproportionate pain relative to an inciting event. The disorder's pathophysiology is complex, involving both central and peripheral nervous system alterations, alongside genetic, inflammatory, and psychological factors. Using data from TriNetX, this study investigated the impact of analgesic and adjuvant therapies on psychiatric outcomes in CRPS patients.
View Article and Find Full Text PDFJ Neurochem
January 2025
Department of Pathology, School of Veterinary Medicine, University of São Paulo, Sao Paulo, Brazil.
Autism spectrum disorder (ASD) is a complex developmental disorder characterized by several behavioral impairments, especially in socialization, communication, and the occurrence of stereotyped behaviors. In rats, prenatal exposure to valproic acid (VPA) induces autistic-like behaviors. Previous studies by our group have suggested that the autistic-like phenotype is possibly related to dopaminergic system modulation because tyrosine hydroxylase (TH) expression was affected.
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