3-Piperazino:ethyl-di:hydro-quinoline-di:one derivs. - useful for controlling blood pressure

摘要

Quinoline derivs. of formula (I) and their salts with acids are new: In (I) R1 is H or 1-3C alkyl opt. substd. by phenyl; R2-4 are H or 1-3C alkyl; R5 is phenyl (opt. substd. by CH3.CH3O or halo) or pyridyl. Pref. cpds. have R1 is H; R2 is H or CH3; R3-4 are CH3; R5 is phenyl opt. substd. at 2- or 4- position by CH3, CH3O, F or Cl. They are made e.g. by reacting the corresp. 3-(2-haloethyl)cpd. with an R5-piperazine. (I) are useful for reducing blood pressure. They are formulated conventionally, e.g. as tablets contg. 100 mg. and all cpds. tested had acute (14-day) oral LD50 in mice >=340 mg/kg.