Discovery of novel ( S)-α-phenyl-γ-amino butanamide containing CCR5 antagonists via functionality inversion approach

The ( S)-α-phenyl-γ-amino butanamide derivatives display high potency to antagonize CCR5 with nanomolar IC 50 values. By using functionality inversion approach, we identified a new scaffold containing ( S)-α-phenyl-γ-amino butanamide as CCR5 antagonists derived from the 1,3-propanediamine carboxamide pharmacophore protocol. The ( 2S)-2-phenyl-4-(8-aza-bicyclo[3.2.1]octan-8-yl)-butanamide derivatives display significantly high potency to antagonize CCR5 receptor with nanomolar IC 50 values.