Privileged structure based ligands for melanocortin receptors--4,4-disubstituted piperidine derivatives |
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| Authors: | Kuklish Steven L Backer Ryan T Briner Karin Doecke Christopher W Husain Saba Mullaney Jeffrey T Ornstein Paul L Zgombick John M O'Brien Thomas P Fisher Matthew J |
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| Institution: | Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46258, USA. Kuklish_steven@lilly.com |
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| Abstract: | Homologation and cyclization back to the chiral methine of compound 3 yields achiral 4,4-disubstituted piperidine privileged structures (e.g., 8a) useful in the construction of melanocortin 4 receptor (MC4R) ligands. The piperidine nitrogen was replaced with carbon, oxygen, sulfur, and sulfone with minor erosion of binding. The methyl cyclohexane substituent was the most potent while significant affinity was still seen for smaller lipophilic groups such as ethyl. |
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