Two new series of 1-(1,2,5-thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2, 6)]heptanes were synthesized and evaluated for their in vitro activity in cell lines transfected with either the human M1 or M2 receptor. 3-Phenyl-2-propyn-1-yloxy and -1-ylthio analogues substituted with halogen in the meta position showed high functional potency, efficacy, and selectivity toward the M1 receptor subtype. A quite unique functional M1 receptor selectivity was observed for compounds 8b, 8d, 8f, 9b, 9d, and 9f. Bioavailability studies in rats indicated an oral bioavailability of about 20-30%, with the N-oxide as the only detected metabolite.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm9910019 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Insights into the Mode of Action of Novel Morpholinated Curcumin Derivatives Exhibiting Potent Antitumor Activity in Bladder Cancer Cells In Vitro.
Molecules
January 2025
Department of Toxicology, Poznan University of Medical Sciences, Rokietnicka 3 Street, 60-806 Poznan, Poland.
Although curcumin is a well-known natural polyphenol with many biological activities, its clinical application has been limited by low aqueous solubility and stability. Therefore, curcumin derivatives have been proposed to overcome these limitations and increase anticancer activity. This study tested curcumin derivatives with modified feruloyl moieties ( and ) and the β-diketo moiety () to better understand their anticancer mechanism against human bladder cancer cells.
View Article and Find Full Text PDFTargeting the Hippo and Rap1 signaling pathways: the anti-proliferative effects of curcumin in colorectal cancer cell lines.
Med Oncol
January 2025
Department of Medical Surgical Nursing, College of Nursing, Princess Nourah bint Abdulrahman University, P.O. Box 84428, 11671, Riyadh, Saudi Arabia.
CRC has the third-highest cancer incidence and death. Many human cancers, including colorectal cancer, are connected to abnormal signaling pathway gene expression. Many human malignancies include Hippo and Rap1 signaling.
View Article and Find Full Text PDFCurcumin Improves Hippocampal Cell Bioenergetics, Redox and Inflammatory Markers, and Synaptic Proteins, Regulating Mitochondrial Calcium Homeostasis.
Neurotox Res
January 2025
Laboratory of Neurobiology of Aging, Centro Científico y Tecnológico de Excelencia Ciencia & Vida, Fundación Ciencia & Vida, Avenida del Valle Norte 725, Huechuraba, Santiago, 8580702, Chile.
Mitochondria produces energy through oxidative phosphorylation (OXPHOS), maintaining calcium homeostasis, survival/death cell signaling mechanisms, and redox balance. These mitochondrial functions are especially critical for neurons. The hippocampus is crucial for memory formation in the brain, which is a process with high mitochondrial function demand.
View Article and Find Full Text PDFCurcumin Modulates Platelet Activation and ROS Production Induced by Amyloid Peptides: New Perspectives in Attenuating Prothrombotic Risk in Alzheimer's Disease Patients.
Nutrients
December 2024
Department of Biology and Biotechnology, University of Pavia, 27100 Pavia, Italy.
Background/objectives: Amyloid peptides, whose accumulation in the brain as senile plaques is associated with the onset of Alzheimer's disease, are also found in cerebral vessels and in circulation. In the bloodstream, amyloid peptides promote platelet adhesion, activation, oxidative stress, and thrombosis, contributing to the cardiovascular complications observed in Alzheimer's disease patients. Natural compounds, such as curcumin, are known to modulate platelet activation induced by the hemostatic stimuli thrombin and convulxin.
View Article and Find Full Text PDFThe anticancer activity of fucoidan coated selenium nanoparticles and curcumin nanoparticles against colorectal cancer lines.
Sci Rep
January 2025
Department of Fish Processing and Biotechnology, Faculty of Aquatic and Fisheries Sciences, Kafrelsheikh University, Kafrelsheikh, 33516, Egypt.
Cancers still globally endanger millions of people yearly; the incidences/mortalities of colorectal cancers are particularly increasing. The natural nanoparticles (NPs) and marine biopolymers were anticipated to provide effectual safe significances for managing cancers. The transformation of curcumin to nano-curcumin (NCur) was conducted with gum Arabic.
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!