Publication Details (including relevant citation information):
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. Bioorganic & Medicinal Chemistry Letters 2006 16 (9) 2341-2346
Abstract: 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. (C) 2005 Elsevier Ltd. All rights reserved.