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Cyclic urea derivatives as potent NK1 selective antagonists
Ho-Jane Shue1, Xiao Chen, Neng-Yang Shih
1Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorganic & Medicinal Chemistry Letters
|July 16, 2005
Summary
Novel urea derivatives act as potent and selective neurokinin-1 (NK1) receptor antagonists. These compounds show promise for oral administration and brain penetration, with their syntheses detailed.
Area of Science:
- Medicinal Chemistry
- Neuroscience
- Pharmacology
Background:
- Neurokinin-1 (NK1) receptors are implicated in various physiological processes.
- Development of selective NK1 receptor antagonists is an active area of research.
Purpose of the Study:
- To synthesize and characterize novel five- and six-membered ring urea derivatives.
- To evaluate these derivatives as potential NK1 receptor antagonists.
Main Methods:
- Synthesis of a series of novel urea derivatives.
- In vitro and/or in vivo assays to determine NK1 receptor antagonism.
- Assessment of oral bioavailability and brain penetration.
Main Results:
- Several novel urea derivatives were successfully synthesized.
- Compounds demonstrated potent and selective NK1 receptor antagonism.
- Selected compounds exhibited favorable oral activity and brain penetration.
Conclusions:
- The described urea derivatives represent a promising class of NK1 receptor antagonists.
- These findings support further investigation for therapeutic applications.