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.
J E Fritz  1 ,  P A Hipskind ,  K L Lobb ,  J A Nixon ,  P G Threlkeld ,  B D Gitter ,  C L McMillian ,  S W Kaldor
Affiliations
  • 1. Lilly Research Laboratories, Eli Lilly and Company, 46285, Indianapolis, IN, USA. [email protected]
PMID: 11425527 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.