Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor

Zhengming Chen; Ellen Davies; Wendy S Miller; Shen Shan; Kenneth J Valenzano; Donald J Kyle

doi:10.1016/j.bmcl.2004.08.032

Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5275-9. doi: 10.1016/j.bmcl.2004.08.032.

Authors

Zhengming Chen¹, Ellen Davies, Wendy S Miller, Shen Shan, Kenneth J Valenzano, Donald J Kyle

Affiliation

¹ Drug Discovery Research, Purdue Pharma L.P., 6 Cedar Brook Drive, Cranbury, NJ 08512, USA. zhengming_chen@hotmail.com

PMID: 15454210
DOI: 10.1016/j.bmcl.2004.08.032

Abstract

Small molecule mu agonists based on the 4-phenyl piperidine scaffold were designed and synthesized to further investigate the therapeutic potential of loperamide analogs. The resulting compounds show excellent agonistic activity towards the human mu receptor with interesting SAR trends within the series.

MeSH terms

Cell Line
Humans
Piperidines / chemical synthesis*
Piperidines / pharmacology*
Receptors, Opioid, mu / agonists*
Receptors, Opioid, mu / antagonists & inhibitors
Receptors, Opioid, mu / metabolism
Structure-Activity Relationship

Substances

Piperidines
Receptors, Opioid, mu