Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, UK.

Published: September 2002

AI Article Synopsis

  • A new group of spiroketal compounds that block NK(1) receptors is introduced.
  • The study analyzes how changes to the spiroether ring and aromatic groups affect the compounds' effectiveness.
  • As a result, several compounds were found to have strong binding capabilities and impressive ability to cross into the central nervous system.

Article Abstract

A series of novel spiroketal-based NK(1) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration.

Download full-text PDF

Source
http://dx.doi.org/10.1016/s0960-894x(02)00506-1DOI Listing

Publication Analysis

Top Keywords

nk1 antagonists
8
spirocyclic nk1
4
antagonists [45]
4
[45] [55]-spiroketals
4
[55]-spiroketals series
4
series novel
4
novel spiroketal-based
4
spiroketal-based nk1
4
antagonists described
4
described modifications
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!