511538-96-8Relevant 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
SUBSTITUTED AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 178; 180, (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.
Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1
Cioffi, Christopher L.,Liu, Shuang,Wolf, Mark A.,Guzzo, Peter R.,Sadalapure, Kashinath,Parthasarathy, Visweswaran,Loong, David T. J.,Maeng, Jun-Ho,Carulli, Edmund,Fang, Xiao,Karunakaran, Kalesh,Matta, Lakshman,Choo, Sok Hui,Panduga, Shailijia,Buckle, Ronald N.,Davis, Randall N.,Sakwa, Samuel A.,Gupta, Priya,Sargent, Bruce J.,Moore, Nicholas A.,Luche, Michele M.,Carr, Grant J.,Khmelnitsky, Yuri L.,Ismail, Jiffry,Chung, Mark,Bai, Mei,Leong, Wei Yee,Sachdev, Nidhi,Swaminathan, Srividya,Mhyre, Andrew J.
, p. 8473 - 8494 (2016/10/03)
We previously disclosed the discovery of rationally designed N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1 (GlyT-1), represented by analogues 10 and 11. We describe herein further structure-activit
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor
Chen, Caroline W.,Tran, Joe A.,Fleck, Beth A.,Tucci, Fabio C.,Jiang, Wanlong,Chen, Chen
, p. 6825 - 6831 (2008/09/16)
A series of trans-N-alkyl-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanemethylamines was synthesized and characterized for binding and function at the melanocortin-4 receptor (MC4R), and several potent benzylamine derivatives were i
Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor
Tran, Joseph A.,Pontillo, Joseph,Arellano, Melissa,Fleck, Beth A.,Tucci, Fabio C.,Marinkovic, Dragan,Chen, Caroline W.,Saunders, John,Foster, Alan C.,Chen, Chen
, p. 3434 - 3438 (2007/10/03)
A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound 14t displayed binding affinity (Ki) of 4.2 and 1100 nM at MC4R and MC3R, respectively.
Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor
Pontillo, Joseph,Tran, Joe A.,White, Nicole S.,Arellano, Melissa,Fleck, Beth A.,Marinkovic, Dragan,Tucci, Fabio C.,Saunders, John,Foster, Alan C.,Chen, Chen
, p. 5237 - 5240 (2007/10/03)
Synthesis and structure-activity relationship studies of a series of cyclohexylpiperazines bearing an amide side chain as ligands of the MC4 receptor are discussed. Compounds such as 11i from this series are potent agonists (EC50 = 33 nM, IA = 96%).
LIGANDS OF MELANOCORTIN RECEPTORS AND COMPOSITIONS AND METHODS RELATED THERETO
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Page 40, (2010/02/07)
Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I) including stereoisomers, prodrugs, and pharmaceutically acceptable salts
