[Synthesis and biological activity of 1-(4-alkyloxy)benzyl-1,2,3,4-tetrahydroisoquinolines and related compounds].
In an attempt to search for novel cardiovascular drugs which might act on calcium or potassium channels, on the basis of the previous study of our group, 15 1-(4-alkyloxy)benzyl-1,2,3,4-tetrahydroisoquinolines derivatives were designed and synthesized among which 10 were not reported previously in the literature. Preliminary pharmacological studies showed that most of these compounds exhibited relaxation of rat thoria aorta in vitro. Compound III9 exhibited potent inhibiting action on low KCl(20 mmol.L-1)-induced contraction of rat aorta, and significant protective effect on experimental arrhythmia in rats.
He
L
L
Division of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009.
Huang
W
W
Gao
H
H
Peng
S
S
D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001013:Aorta, Thoracic; D001145:Arrhythmias, Cardiac / Q000517:prevention & control; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D051381:Rats
D000889:Anti-Arrhythmia Agents; D007546:Isoquinolines