S. Sakurai, F. Okada, K. Mitani
Oct 1, 1990
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Journal
Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
Abstract
alpha-[(Phenoxyethylamino)propyl]-alpha-(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 alpha-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 alpha-blocker. Structure-activity relationship of these derivatives is also stated.