Abstract
Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and orally more efficacious γ-lactam series of selective NK1 antagonists. Optimization of the lactam series culminated in the identification of compounds with high binding affinity and excellent oral CNS activity.
Original language | English |
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Pages (from-to) | 4168-4171 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 18 |
Issue number | 14 |
DOIs | |
State | Published - 15 Jul 2008 |
Keywords
- CNS
- Emesis
- Lactam
- NK1
- Substance P