Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective opioid antagonists.

Bioorg Med Chem Lett 2006 Feb 18;16(4):864-8. Epub 2005 Nov 18.

Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA.

Structure-activity relationships at the 2alpha-position of the piperidine ring of the trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine mu-opioid antagonist series were investigated. This study showed that only small linear alkyl groups (methyl, propyl) are tolerated at the 2alpha-position of the piperidine ring of this series.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2005.11.010DOI Listing
February 2006
6 Reads

Publication Analysis

Top Keywords

structure-activity relationships
8
piperidine ring
8
2alpha-position piperidine
8
series investigated
4
investigated study
4
antagonist series
4
trans-45-dimethyl-4-3-hydroxyphenylpiperidine mu-opioid
4
study small
4
mu-opioid antagonist
4
linear alkyl
4
propyl tolerated
4
tolerated 2alpha-position
4
ring series
4
methyl propyl
4
groups methyl
4
relationships 2alpha-position
4
alkyl groups
4
small linear
4
ring trans-45-dimethyl-4-3-hydroxyphenylpiperidine
4
mu-selective opioid
4

Altmetric Statistics

Similar Publications