874623-59-3Relevant academic research and scientific papers
Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1-yl) cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1
Cioffi, Christopher L.,Wolf, Mark A.,Guzzo, Peter R.,Sadalapure, Kashinath,Parthasarathy, Visweswaran,Dethe, Dattatraya,Maeng, Jun-Ho,Carulli, Edmund,Loong, David T.J.,Fang, Xiao,Hu, Min,Gupta, Priya,Chung, Mark,Bai, Mei,Moore, Nick,Luche, Michele,Khmelnitsky, Yuri,Love, Patrick L.,Watson, Megan A.,Mhyre, Andrew J.,Liu, Shuang
, p. 1257 - 1261 (2013)
The design, synthesis, and structure-activity relationships (SAR) of a series of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1 (GlyT-1) are described. Optimization of the benzamide and central ring
SUBSTITUTED AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 173; 175, (2017/02/24)
The present invention relates to substituted amide derivatives of formula (I) having dual pharmacological activity towards both the sigma (σ) receptor, and the p-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
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.
