Title of article
Privileged structure based ligands for melanocortin receptors—4,4-Disubstituted piperidine derivatives
Author/Authors
Steven L. Kuklish، نويسنده , , Ryan T. Backer، نويسنده , , Karin Briner، نويسنده , , Christopher W. Doecke، نويسنده , , Saba Husain، نويسنده , , Jeffrey T. Mullaney، نويسنده , , Paul L. Ornstein، نويسنده , , John M. Zgombick، نويسنده , , Thomas P. O’Brien، نويسنده , , Matthew J. Fisher، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
3843
To page
3846
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.
Keywords
melanocortin , privileged structure , GPCR , G-protein coupled receptors , MC4
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797091
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