Back to Search Start Over

Rapid access towards follow-up NOP receptor agonists using a knowledge based approach

Authors :
Duncan McArthur
Alasdair R.C. Smith
Niall M. Hamilton
Louise Evans
Ronald Palin
Helen Feilden
Dan Fletcher
Grant Wishart
Aaron Sutherland
Philip S. Jones
Mark A. Weston
Paul Ratcliffe
John K. Clark
Brian Montgomery
Andrea K. Houghton
Source :
Bioorganicmedicinal chemistry letters. 19(22)
Publication Year :
2009

Abstract

A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replacement of the benzimidazol-2-one moiety was explored. Compound 51 was found to be a high affinity, potent NOP receptor agonist with reduced affinity for the hERG channel.

Details

ISSN :
14643405
Volume :
19
Issue :
22
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry letters
Accession number :
edsair.doi.dedup.....62fe4ddf63cb135568f4a115431ad52a