Abstract
A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an α-methyl group at the benzylic position to improve potency and duration of in vivo activity are discussed. Several compounds with high affinity and sustained in vivo activity were identified.
Original language | English |
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Pages (from-to) | 1065-1069 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 16 |
Issue number | 4 |
DOIs | |
State | Published - 15 Feb 2006 |
Keywords
- Improved potency
- NK antagonist
- Sustained in vivo activity