N-Methyl 1-phenyl-2-amino-1,3-propane-diol derivs. - have anti:angina, local anaesthetic and anticonvulsant activity on smooth muscle

摘要

N-Alkyl-1-phenyl-2-amino-1, 3-propanediol derivs of formula (I) as the isomers or their mixts. and their salts are new (where R1 is H, 1-8C alkyl or phenoxymethyl and R2 is H, 1-8C alkyl, or 2,2-diphenylethyl with the conditions that when R1 is phenoxymethyl then R2 is methyl and when R2 is 2, 2-diphenylethyl then R1 is H). (I) are anti-angina active cpds. some of which have superior activity to prenilamine (3, 3-diphenyl-propyl -1-methyl-phenylethylamine). Some of the cpds. have local anaesthetic activity and anticonvulsant activity on smooth muscle, with some having superior activity to lidocaine. The cpds. have low toxicity e.g. oral LD50 in mice in range 700-2000 mg/kg, i.v. LD50.