444583-49-7Relevant academic research and scientific papers
AMINOTROPANE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
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Page/Page column 17, (2008/06/13)
The present invention relates to compounds of formula (I) as defined herein that are melanocortin receptor agonists, to the preparation thereof and to the therapeutic use thereof in the treatment and in the prevention of obesity, diabetes and sexual dysfunctions that can affect both sexes, in the treatment of cardiovascular diseases, and also in anti-inflammatory uses or in the treatment of alcohol dependency.
Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor
Shi, Qing,Ornstein, Paul L.,Briner, Karin,Richardson, Timothy I.,Arnold, Macklin B.,Backer, Ryan T.,Buckmaster, Jennifer L.,Canada, Emily J.,Doecke, Christopher W.,Hertel, Larry W.,Honigschmidt, Nick,Hsiung, Hansen M.,Husain, Saba,Kuklish, Steve L.,Martinelli, Michael J.,Mullaney, Jeffrey T.,O'Brien, Thomas P.,Reinhard, Matt R.,Rothhaar, Roger,Shah, Jikesh,Wu, Zhipei,Xie, Chaoyu,Zgombick, John M.,Fisher, Matthew J.
, p. 2341 - 2346 (2007/10/03)
A series of benzylic piperazines (e.g., 4 and 5) attached to an 'address element', the dipeptide H-d-Tic-d-p-Cl-Phe-OH, 3 has been identified as ligands for the melanocortin subtype-4 receptor (MC4R). We describe herein the structure-activity relationship (SAR) studies on the N-terminal residue of the 'address element'. Several novel dipeptides and reduced dipeptides with high MC4R binding affinities and selectivity emerged from this SAR study.
