2. Academic Validation
  3. Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent

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

Affiliation

  • 1 Lilly Research Laboratories, Eli Lilly and Company, 46285, Indianapolis, IN, USA. j.fritz@lilly.com
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.

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