76458-35-0Relevant academic research and scientific papers
Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ
Behnia, Kamelia,Bilder, Donna M.,Burford, Neil T.,Cavallaro, Cullen L.,Chao, Hannguang J.,Dabros, Marta,Gargalovic, Peter S.,Langish, Robert A.,Lawrence, R. Michael,Li, Yi-Xin,Myers, Michael C.,Nayeem, Akbar,Onorato, Joelle M.,Rose, Anne V.,Su, Shun,Wang, Tao,Wexler, Ruth R.,Yan, Mujing
, (2020)
This article describes the discovery of aryl hydroxy pyrimidinones and the medicinal chemistry efforts to optimize this chemotype for potent APJ agonism. APJ is a G-protein coupled receptor whose natural agonist peptide, apelin, displays hemodynamic improvement in the cardiac function of heart failure patients. A high throughput screen was undertaken to identify small molecule hits that could be optimized to mimic the apelin in vitro response. A potent and low molecular weight aryl hydroxy pyrimidinone analog 30 was identified through optimization of an HTS hit and medicinal chemistry efforts to improve its properties.
2-Imidazolines. IV (1). 1-Aryl-2-alkylthio-4,5-diamino-4,5-dihydroimidazoles. Synthesis and Properties
Meola, Stefania,Rivera, Elisabetta,Stradi, Riccardo,Gioia, Bruno
, p. 1041 - 1044 (2007/10/02)
1,2-Diimmonium salts (1) react with S-substituted isothioureas (3) yielding 2-alkylthio-4,5-diamino-4,5-dihydroimidazoles (4), which under mild pyrolytic conditions afforded 2-alkylthio-5-aminoimidazoles (7).Imidazolines (4) and imidazoles (7) were easily
