High affinity phenylglycinol-based NK1 receptor antagonists

A P Owens; T Harrison; J D Moseley; C J Swain; S Sadowski; M A Cascieri

doi:10.1016/s0960-894x(97)10163-9

High affinity phenylglycinol-based NK1 receptor antagonists

Bioorg Med Chem Lett. 1998 Jan 6;8(1):51-6. doi: 10.1016/s0960-894x(97)10163-9.

Authors

A P Owens¹, T Harrison, J D Moseley, C J Swain, S Sadowski, M A Cascieri

Affiliation

¹ Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, Harlow, Essex, U.K. andrew_owens@merck.com

PMID: 9871627
DOI: 10.1016/s0960-894x(97)10163-9

Abstract

Heterocyclic replacements for the carboxamido group of the previously disclosed phenylglycinol-based human NK1 (hNK1) receptor antagonists have been investigated, ultimately leading to acyclic compounds with sub-nanomolar affinity for the hNK1 receptor.

MeSH terms

Ethanolamines
Glycine / analogs & derivatives*
Glycine / chemistry
Glycine / pharmacology
Humans
Molecular Structure
Neurokinin-1 Receptor Antagonists*
Structure-Activity Relationship

Substances

Ethanolamines
Neurokinin-1 Receptor Antagonists
N-phenylethanolamine
Glycine