Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, UK.

Published: October 2002

A series of novel spiroether-based neurokinin-1 (NK(1)) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration.

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http://dx.doi.org/10.1016/s0960-894x(02)00509-7DOI Listing

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