Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1367304 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
A new class of potent NK3R antagonists based on the Nâ²,2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ90 30 mg/kg po; plasma Occ90 0.95 μM) and has good selectivity and promising PK properties.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jason M. Elliott, Robert W. Carling, Mark Chambers, Gary G. Chicchi, Peter H. Hutson, A. Brian Jones, Angus MacLeod, Rose Marwood, Georgina Meneses-Lorente, Elena Mezzogori, Fraser Murray, Michael Rigby, Inmaculada Royo, Michael G.N. Russell,