Studies on the active conformation of the NK1 antagonist CGP 49823. Part 2. Fluoro-olefin analogs of tertiary amide rotamers

Article abstract of DOI:10.1016/S0960-894X(96)00624-5

Four fluoro-olefin analogs of CGP 49823 have been synthesized. Comparison of their binding affinities for the NK₁ receptor suggests an active conformation of CGP 49823, where the aromatic ring of the benzamide has a syn orientation towards the 2-benzyl substituent.