Privileged structure based ligands for melanocortin receptors—Substituted benzylic piperazine derivatives
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- 作者：Matthew J. Fisher ; Ryan T. Backer ; Ivá ; n Collado ; Ó ; scar de Frutos ; Saba Husain ; Hansen M. Hsiung ; Steve L. Kuklish ; Ana I. Mateo ; Jeffrey T. Mullaney ; Paul L. Ornstein et al.
- 关键词：Melanocortin receptors ; Priveleged structures
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2005
- 出版时间：2005
- 年：2005
- 卷：15
- 期：22
- 页码：4973-4978
- 全文大小：136 K
文摘
Replacement of the aryl piperazine moiety in compound 1 with a variety of substituted benzylic piperazines (6) yields compounds that afford melanocortin receptor 4 (MCR4) activity. Analogs with ortho substitution on the aromatic ring afforded the highest affinity. Resolution of the stereocenter of the benzylic piperazine based privileged structure revealed that the R-enantiomer was more active.