Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives |
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| Authors: | Briner Karin Collado Iván Fisher Matthew J García-Paredes Cristina Husain Saba Kuklish Steven L Mateo Ana I O'Brien Thomas P Ornstein Paul L Zgombick John de Frutos Oscar |
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| Affiliation: | Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46258, USA. |
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| Abstract: | Aliphatic carbocyclic replacement of the benzyl group of compound 1 yielded compounds with high affinity for the melanocortin-4 receptor (MC4R). Compounds with a cyclohexyl group showed a consistent high affinity, while different polar groups with less basicity were good replacements for the original diethyl amines. Substitution of the polar group found in these privileged structures with an aliphatic moiety produced compounds with high affinity for MC4R. |
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