22912-29-4Relevant academic research and scientific papers
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ1Receptor Antagonists for the Treatment of Pain
García, Mónica,Llorente, Virginia,Garriga, Lourdes,Christmann, Ute,Rodríguez-Escrich, Sergi,Virgili, Marina,Fernández, Bego?a,Bordas, Magda,Ayet, Eva,Burgue?o, Javier,Pujol, Marta,Dordal, Albert,Portillo-Salido, Enrique,Gris, Georgia,Vela, José Miguel,Almansa, Carmen
, p. 10139 - 10154 (2021/07/28)
A new series of propionamide derivatives was developed as dual μ-opioid receptor agonists and σ1receptor antagonists. Modification of a high-throughput screening hit originated a series of piperazinylcycloalkylmethyl propionamides, which were e
Discovery of a novel series of selective HCN1 blockers
McClure, Kelly J.,Maher, Michael,Wu, Nancy,Chaplan, Sandra R.,Eckert III, William A.,Lee, Dong H.,Wickenden, Alan D.,Hermann, Michelle,Allison, Brett,Hawryluk, Natalie,Breitenbucher, J. Guy,Grice, Cheryl A.
scheme or table, p. 5197 - 5201 (2011/10/02)
The discovery of a series of novel, potent, and selective blockers of the cyclic nucleotide-modulated channel HCN1 is disclosed. Here we report an SAR study around a series of selective blockers of the HCN1 channel. Utilization of a high-throughput VIPR assay led to the identification of a novel series of 2,2-disubstituted indane derivatives, which had moderate selectivity and potency at HCN1. Optimization of this hit led to the identification of the potent, 1,1-disubstituted cyclohexane HCN1 blocker, 2-ethoxy-N-((1-(4- isopropylpiperazin-1-yl)cyclohexyl)methyl)benzamide. The work leading to the discovery of this compound is described herein.
