Drabczyńska A, Cebo B, Krupińska J, Michna M, Chłoń G, Zébala K
Department of Chemical Technology of Drugs, Medical Academy, Kraków, Poland.
Pol J Pharmacol Pharm. 1988 May-Jun;40(3):321-9.
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.
新型7,8-二取代茶碱1-6a，其8位带有手性或非手性的1,2-氨基醇部分，作为对循环系统具有预期活性的化合物被合成出来。对它们的抗心律失常活性和对心血管系统的作用进行了初步评估。仅外消旋的7-β-羟乙基-8-(1'-羟基丁-2'-基)氨基茶碱1及其对映体2、3表现出与奎尼丁相似的抗心律失常活性（毒性约低20倍），它们在疗效上没有明显差异。茶碱7位带有羟乙基部分的化合物（1-3、5）表现出降压作用。
