Novel Phenoxyalkylamine Derivatives. VI. Synthesis and α-Blocking Activity of α-[(Phenoxyethylamino) propyl]-α-phenylacetonitrile Derivatives

Abstract

α-[(Phenoxyethylamino) propyl]-α-(4-methoxyphenyl) acetonitrile derivatives possessing methyl, bromo, nitro, amino or various sulfonamide groups at 3-position on ring A and an alkoxy group on ring B were synthesized. Their α-blocking activities were tested. The activity of 5-[1-cyano-4-[[2-(2-ethoxyphenoxy) ethyl] amino]-1-isopropylbutyl]-2-methoxy-benzenesulfonamide (15a) and 5-[1-cyano-4-[[2-(5-fluoro-2-methoxyphenoxy) ethyl] amino]-1-isopropylbutyl]-2-methoxybenzenesulfonamide (15c) was close to that of prazosin, a typical α-blocker. Structure-activity relationship of these derivatives is also stated.