New derivatives of amino alcohols with antiarrhythmic activity.
Nine new N-acyl derivatives of 2-amino-1-alcohols and 1-amino-2-alcohols with a potential arrhythmic activity have been obtained. In the preliminary screening 2-[N-(7-theophyllineacetyl)-amino]-2-methyl-1-propanol, 5, was more active in the chloroform-induced arrhythmia than quinidine. Unlike to propranolol and quinidine, compound 5 in doses of 5-30 mg/kg, iv, did not prevent distortions of the cardiac rhythm evoked by adrenaline and strophanthine. When administered at the peak of arrhythmia, it did not abolish disturbances of the cardiac rhythm. Compound 5 had a low toxicity (LD50 = 3000 mg/kg, ip), did not change the control ECG curve, showed no cardiodepressive activity, and had weaker local anesthetic properties than lignocaine.
Department of Chemical Technology of Drugs, Medical Academy, Kraków, Poland.
M
M
Eckstein
M
M
Cegła
J
J
Krupińska
B
B
Cebo
M
M
Michna
D000605:Amino Alcohols / Q000494:pharmacology*; D000818:Animals; D000889:Anti-Arrhythmia Agents; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains
D000605:Amino Alcohols; D000889:Anti-Arrhythmia Agents