Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1643-6. doi: 10.1016/s0960-894x(01)00250-5.

Abstract

Solution-phase, parallel-synthesis techniques were used to optimize a series of nonbasic NK-1 antagonists, resulting in the identification of (R)-26, an orally bioavailable compound with subnanomolar potency.

MeSH terms

  • Neurokinin-1 Receptor Antagonists*
  • Structure-Activity Relationship

Substances

  • Neurokinin-1 Receptor Antagonists