130982-68-2Relevant academic research and scientific papers
A New Class of Calcium Antagonists. Synthesis and Biological Activity of 11--6,6a,7,8,9,10,10a,11-octahydrodibenzothiepin Derivatives
Kurokawa, Mikio,Sato, Fuminori,Hatano, Naonobu,Honda, Yayoi,Uno, Hitoshi
, p. 593 - 599 (2007/10/02)
A series of 11--6,6a,7,8,9,10,10a,11-octahydrodibenzothiepin derivatives were prepared and found to be structurally new class of calcium antagonists.The structure-activivty relationship studies indicated that the optimum was (6aR*,10aR*,11R*)-11-butyryl>amino>-6,6a,7,8,9,10,10a,11-octahydrodibenzothiepin (31, pA2 8.16), which was superior to diltiazem (pA2 7.42) in calcium antagonistic activity.Compound 31 showed antihypertensive activity in anesthetized rats, without a significant effect on the heart rate.It had also antianginal effects in vasopressin-induced ST-elevation testings in rats.These potencies of 31 were essentially equal to those of diltiazem.
