Cyclobutane derivatives as potent NK1 selective antagonists

Michelle Laci Wrobleski, Gregory A. Reichard, Sunil Paliwal, Sapna Shah, Hon Chung Tsui, Ruth A. Duffy, Jean E. Lachowicz, Cynthia A. Morgan, Geoffrey B. Varty, Neng Yang Shih

Research output: Contribution to journalArticlepeer-review

36 Scopus citations

Abstract

A series of novel cyclobutane derivatives as potent and selective NK1 receptor antagonists is described. Several compounds in this series exhibited high in vitro binding affinity (Ki {less-than or slanted equal to} 1 nM), and potent inhibition of central NK1 receptor following oral administration. Syntheses of these compounds are also described herein.

Original languageEnglish
Pages (from-to)3859-3863
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number14
DOIs
StatePublished - 15 Jul 2006

Keywords

  • CNS penetration
  • Cyclobutane
  • NK antagonist
  • Oral in vivo activity
  • Substance P

Fingerprint

Dive into the research topics of 'Cyclobutane derivatives as potent NK1 selective antagonists'. Together they form a unique fingerprint.

Cite this