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Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor |
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| Authors: | 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 |
| Institution: | Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. shi_qing@lilly.com |
| 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. |
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