Schenker E, Salzmann R
Arzneimittelforschung. 1979;29(12):1835-43.
The synthesis of a series of 3-hydrazinopyridazines is described. Several of these compounds exhibited high antihypertensive activity in the rat. The most potent member of the series is l-benzoyl-3-hydrazino-5,6,7,8-tetrahydropyrido-[4,3-c]pyridazine, compound 28 [1], which is now under clinical trial [2] under the clinical code number BQ 22-708 (endrazaline, Miretilan). It was possible to discover certain structure-activity relationships.
本文描述了一系列3-肼基哒嗪的合成。其中几种化合物在大鼠中表现出高抗高血压活性。该系列中最有效的成员是1-苯甲酰基-3-肼基-5,6,7,8-四氢吡啶并[4,3-c]哒嗪,即化合物28 [1],目前正在进行临床试验[2],临床代码为BQ 22-708(恩扎拉林,米雷替兰)。有可能发现某些构效关系。