Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists

Gregori J. Morriello,Robert J. DeVita,Sander G. Mills,Jonathan R. Young,Peter Lin,George Doss,Gary G. Chicchi,Julie DeMartino,Marc M. Kurtz,Kwei-Lan C. Tsao,Emma Carlson,Karen Townson,Alan Wheeldon,Susan Boyce,Neil Collinson,Nadia Rupniak,Stephen Moore

Bioorganic & Medicinal Chemistry（2008）

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摘要

A novel 5,5-fused pyrrolidine scaffold has been discovered which exhibits superior brain penetration and maintains excellent binding affinity, as well as, functional IP activity versus previously reported hNK1 antagonist.

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