Privileged structure based ligands for melanocortin-4 receptors—Aliphatic piperazine derivatives

详细信息    查看全文

• 作者：Karin Briner ; Ivá ; n Collado ; Matthew J. Fisher ; Cristina Garcí ; a-Paredes ; Saba Husain ; Steven L. Kuklish ; Ana I. Mateo ; Thomas P. O’ ; Brien ; Paul L. Ornstein ; John Zgombick and Ó ; scar
• 关键词：Melanocortin receptors ; Privileged structures
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 July 2006
• 年：2006
• 卷：16
• 期：13
• 页码：3449-3453
• 全文大小：148 K

文摘

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.