Sj. Veenstra et al., STUDIES ON THE ACTIVE CONFORMATION OF THE NK1 ANTAGONIST GCP-49823 .2. FLUORO-OLEFIN ANALOGS OF TERTIARY AMIDE ROTAMERS, Bioorganic & medicinal chemistry letters, 7(3), 1997, pp. 351-354
Four fluoro-olefin analogs of CGP 49823 have been synthesized. Compari
son of their binding affinities for the NK1 receptor suggests an activ
e conformation of CGP 49823, where the aromatic ring of the benzamide
has a syn orientation towards the 2-benzyl substituent. (C) 1997, Else
vier Science Ltd.