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Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor
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
Affiliation: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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