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Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions |
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| Authors: | Shue Ho-Jane Chen Xiao Schwerdt John H Paliwal Sunil Blythin David J Lin Ling Gu Danlin Wang Cheng Reichard Gregory A Wang Hongwu Piwinski John J Duffy Ruth A Lachowicz Jean E Coffin Vicki L Nomeir Amin A Morgan Cynthia A Varty Geoffrey B Shih Neng-Yang |
| Affiliation: | Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. |
| 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 alpha-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. |
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