2. Academic Validation
  3. N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

  • Bioorg Med Chem Lett. 2006 Nov 15;16(22):5748-51. doi: 10.1016/j.bmcl.2006.08.086.
Jason M Elliott 1,  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,  Bindi Sohal,  Kwei Lan Tsao,  Brian Williams
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. jason@elliottj25.fsnet.co.uk
PMID: 16950620 DOI: 10.1016/j.bmcl.2006.08.086
Abstract

A new class of potent NK3R antagonists based on the N',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 (Occ(90) 30 mg/kg po; plasma Occ(90) 0.95 microM) and has good selectivity and promising PK properties.

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