Novel phenoxyalkylamine derivatives. II. Synthesis and Ca2+-antagonistic activities of .ALPHA.-alkyl-.ALPHA.-((phenoxypropylamino)propyl)-benzeneacetonitrile derivatives.
- 1 January 1988
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 36 (1) , 373-385
- https://doi.org/10.1248/cpb.36.373
Abstract
.alpha.-Alkyl-.alpha.-[(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.This publication has 0 references indexed in Scilit: