N-Aryl-γ-lactams as integrin αvβ3 antagonists

Abstract Novel α v β 3 antagonists based on the N -aryl-γ-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for α v β 3 receptor with excellent selectivity against the structurally related α IIb β 3 receptor. Additional interactions of N -aryl-γ-lactam derivatives with α v β 3 were found when compared to c(-RGDf[NMe]V-) peptide antagonist. The effects of the conformation and configuration of the γ-lactam core on the binding were also assessed.