Synthesis and structure–activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor
…, K Briner, TI Richardson, MB Arnold, RT Backer…
Index: 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 and Medicinal Chemistry Letters, 2006 , vol. 16, # 9 p. 2341 - 2346
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Citation Number: 8
Abstract
A series of benzylic piperazines (eg, 4 and 5) attached to an 'address element', the dipeptide Hd-Tic-dp-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.
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