A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)acetamide derivatives were optimized to achieve potent agonistic activity, both in vitro and in vivo, for the arginine vasopressin V(2) receptor, resulting in the eventual discovery of compound 1g. Molecular modeling of compound 1g with V(2) receptor was also examined to evaluate the binding mode of this series of compounds.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmc.2009.10.038 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Associations between skeletal muscle mass and elevated blood pressure are independent of body fat: a cross-sectional study in young adult women of African ancestry.
Br J Nutr
January 2025
SAMRC/Wits Developmental Pathways for Health Research Unit, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, South Africa.
Although research on the relationship between lean body mass and blood pressure (BP) has been inconsistent, most studies reported that measures of lean body mass are associated with a higher risk of hypertension. We explored relationships between body composition (fat and skeletal muscle mass) and BP in 1162 young adult African women. DXA-derived measures of whole body, central and arm fat mass were associated with higher systolic and diastolic BP, while leg fat percentage was associated with lower systolic and diastolic BP.
View Article and Find Full Text PDFHierarchical Selenium-Doped Nickel-Cobalt Hybrids on Carbon Paper for the Overall Water-Splitting Electrocatalytic System.
ACS Appl Mater Interfaces
January 2025
Department of Battery and Chemical Engineering, Hanyang University, Ansan, Gyeonggi-do 15588, Republic of Korea.
Designing and constructing hierarchically structured materials with heterogeneous compositions is the key to developing an effective catalyst for overall water-splitting applications. Herein, we report the fabrication of hollow-structured selenium-doped nickel-cobalt hybrids on carbon paper as a self-supported electrode (denoted as Se-Ni|Co/CP, where Ni|Co hybrids consist of nickel-cobalt alloy-incorporated nickel-cobalt oxide). The procedure involves direct growth of zeolitic imidazolate framework-67 (ZIF-67) on bimetal-based nickel-cobalt hydroxide (NiCoOH) electrodeposited on CP, followed by selenous etching and pyrolysis to obtain the final Se-Ni|Co/CP electrocatalytic system.
View Article and Find Full Text PDFSynergistic Cu(II)/Amine-Catalyzed Cyclization of Enynone: Assembly of Tetralone and Tetrahydronaphthylimine.
Org Lett
January 2025
School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan 411201, China.
An unprecedented synergistic copper- and amine-catalyzed cyclization of enynone is reported. This reaction features an efficient and straightforward construction of multisubstituted tetralone through an amine-assisted regioselective oxygen atom transfer process and stereoselective intramolecular Michael addition cyclization. Under dehydrative reaction conditions, the synthesis of tetrahydronaphthylimine derivatives with ketone group tolerance is achieved, which could be challenging via traditional methods.
View Article and Find Full Text PDFImmunohistochemistry-based molecular subtypes of urothelial carcinoma derive different survival benefit from platinum chemotherapy.
J Pathol Clin Res
January 2025
Department of Urology, University of Duisburg-Essen, Essen, Germany.
Distinct molecular subtypes of muscle-invasive bladder cancer (MIBC) may show different platinum sensitivities. Currently available data were mostly generated at transcriptome level and have limited comparability to each other. We aimed to determine the platinum sensitivity of molecular subtypes by using the protein expression-based Lund Taxonomy.
View Article and Find Full Text PDFCordycepin and Its Structural Derivatives Effectively Suppress the High Expression of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase in Breast Carcinomas: A Computational Drug Development Approach.
Curr Med Chem
January 2025
Laboratory of Pharmaceutical Biotechnology and Bioinformatics, Department of Genetic Engineering and Biotechnology, Jashore University of Science and Technology, Jashore, 7408, Bangladesh.
Background: Breast cancer is a frequently diagnosed malignant disease and the primary cause of mortality among women with cancer worldwide. The therapy options are influenced by the molecular subtype due to the intricate nature of the condition, which consists of various subtypes. By focusing on the activation of receptors, Epidermal Growth Factor Receptor (EGFR) tyrosine kinase can be utilized as an effective drug target for therapeutic purposes of breast cancer.
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!