3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.

@article{Hipskind19963Aryl12diacetamidopropaneDA,
  title={3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.},
  author={Philip Arthur Hipskind and James Jeffry Howbert and Robert F. Bruns and San Soon Cho and Tom Crowell and Mark Mortensen Foreman and Donald R. Gehlert and Smriti Iyengar and Kirk Wallace Johnson and Joseph Herman Junior Krushinski and D. Leonard Corgan Li and Karen Lynn Lobb and Norman R. Mason and Brian Stephen Muehl and John Alexander Nixon and Lee Phebus and Domenico Regoli and Rosa Maria Ademe Simmons and Penny G. Threlkeld and Dic Waters and Bruce D. Gitter},
  journal={Journal of medicinal chemistry},
  year={1996},
  volume={39 3},
  pages={
          736-48
        }
}
Early structure-activity studies on racemic tryptophan ester and amide NK-1 antagonists 5-7 led to the discovery that the potency of the series could be markedly increased by moving the carbonyl function in these molecules to an off-chain position as in the 3-aryl-1,2-diacetamidopropane 9. Further medicinal chemistry incorporating this change resulted in the discovery of a novel series of highly potent aryl amino acid derived NK-1 antagonists of the R stereoisomeric series (IC50's = 100 pM to… CONTINUE READING
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