The effect of some 8-aminoalkanol derivatives of theophylline on cardiovascular system.
Novel 7,8-disubstituted theophyllines 1-6a, with chiral or achiral moiety of 1,2-aminoalcohol in position 8, were obtained as the compounds with expected activity on circulation. Preliminary evaluation of their antiarrhythmic activity and the effect on the cardiovascular system was carried out. The antiarrhythmic activity similar to that of quinidine (with ca. 20 times lower toxicity) was found only for racemic 7-beta-hydroxyethyl-8-(1'-hydroxybut-2'-yl) aminotheophylline 1 and its enantiomers 2, 3 which did not differ markedly in their efficacy. The compounds with the hydroxyethyl moiety in position 7 of theophylline (1-3, 5) showed the hypotensive effect.
Drabczyńska
A
A
Department of Chemical Technology of Drugs, Medical Academy, Kraków, Poland.
Cebo
B
B
Krupińska
J
J
Michna
M
M
Chłoń
G
G
Zébala
K
K
D000605:Amino Alcohols / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D002319:Cardiovascular System / Q000187:drug effects*; D005260:Female; D006168:Guinea Pigs; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D013806:Theophylline / Q000031:analogs & derivatives*
D000605:Amino Alcohols; D013806:Theophylline