Novel Phenoxyalkylamine Derivatives. II. : Synthesis and Ca²⁺-Antagonistic Activities of α-Alkyl-α-[(phenoxypropylamino)propyl]-benzeneacetonitrile Derivatives

Abstract

α-Alkyl-α-[(phenoxypropylamino)propyl]benzeneacetonitrile derivatives containing various substituents on the ring of the benzeneacetonitrile moiety (A), the quaternary carbon atom and the ring of the phenoxy moiety (B) were prepared, and their Ca²⁺-antagonistic activities were evaluated. Among these compounds, the N-Me derivatives with a 3, 4, 5-(OMe)₃ group on the A ring, an iso-Pr group on the quaternary carbon atom, and a m-OMe, 3, 5-(OMe)₂, 3, 5-Me₂ or 3, 4, 5-(OMe)₃ group on the B ring were found to possess Ca²⁺-antagonistic activity higher than pA₂=9. The effects of substitutions at the A ring, the quaternary carbon atom and the B ring are discussed.