Discovery of a series of potent, orally active α,α- disubstituted piperidine NK1 antagonists

Dong Xiao, Cheng Wang, Anandan Palani, Hon Chung Tsui, Gregory Reichard, Sunil Paliwal, Neng Yang Shih, Robert Aslanian, Ruth Duffy, Jean Lachowicz, Geoffrey Varty, Cynthia Morgan, Fei Liu, Amin Nomeir

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

Modification of prototype NK1 antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK1 antagonists.

Original languageEnglish
Pages (from-to)6313-6315
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number21
DOIs
StatePublished - 1 Nov 2010

Keywords

  • Dibasic amine metabolite
  • NK antagonist

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