851484-85-0Relevant academic research and scientific papers
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 (2005)
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.
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
LIGANDS OF MELANOCORTIN RECEPTORS AND COMPOSITIONS AND METHODS RELATED THERETO
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Page 40-41, (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
