[Synthesis and biological activity of 1-(4-acylamino)benzyl-1,2,3,4-tetrahydroisoquinolines].
For searching more effective antiarrhythmic agents, on the basis of integration of the structural feature of certain potassium channel blockers available, various acylamino groups were introduced to the position 4 of the benzyl ring of this series of compounds. Thus, eight 1-(4-acylamino)benzyl-1,2,3,4-tetrahydroisoquinolines were designed and synthesized, which had not been reported in the literatures. Compounds V1, V2 and V6 at concentration 10(-6) mol.L-1 depressed rat aortia contraction induced by high KCl (80 mmol.L-1). The effect was similar to that of tetrandrine. Compound V6 showed potent antiarrhythmic activity at the dosage of 1 mg.kg-1.
He
L
L
Division of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009.
Huang
W
W
Shen
Y
Y
Peng
S
S
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001011:Aorta; D001145:Arrhythmias, Cardiac / Q000517:prevention & control; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley
D000634:Aminoquinolines; D000889:Anti-Arrhythmia Agents; D007546:Isoquinolines