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 language | English |
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Pages (from-to) | 3859-3863 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 16 |
Issue number | 14 |
DOIs | |
State | Published - 15 Jul 2006 |
Keywords
- CNS penetration
- Cyclobutane
- NK antagonist
- Oral in vivo activity
- Substance P