Parravicini F, Scarpitta G, Dorigotti L, Pifferi G
Farmaco Sci. 1979 Apr;34(4):299-310.
The synthesis of 2-(6-dialkylamino-3-pyridazinyl)hydrazinecarboxylates (II) and hydrazides (V) from the corresponding 3-chloro-6-dialkylaminopyridazines (I) is described. The 6-substituted derivatives of 2,3-dihydro-1,2,4-triazolo[4,3-b]pyridazine-3-ones (III) and 1,2,4-triazolo[4,3-b)pyridazines (VI) were obtained by thermal cyclization of (II) and (V), respectively. The new acyl derivatives were evaluated together with todralazine and budralazine as antihypertensive agents in comparison with propildazine and hydralazine. The ethoxycarbonyl compound [(II g), ISF 2469] exhibits good antihypertensive activity particularly via oral administration. Its interesting pharmacodynamic properties, including slow onset and long-lasting action, qualify it for further pharmacological and clinical studies.
描述了由相应的3-氯-6-二烷基氨基哒嗪(I)合成2-(6-二烷基氨基-3-哒嗪基)肼羧酸酯(II)和酰肼(V)的方法。分别通过(II)和(V)的热环化反应得到了2,3-二氢-1,2,4-三唑并[4,3-b]哒嗪-3-酮(III)和1,2,4-三唑并[4,3-b]哒嗪(VI)的6-取代衍生物。将这些新的酰基衍生物与托屈嗪和布屈嗪一起作为抗高血压药物进行评估,并与丙酰肼和肼屈嗪作比较。乙氧羰基化合物[(II g),ISF 2469]表现出良好的抗高血压活性,尤其是通过口服给药时。其有趣的药效学特性,包括起效缓慢和作用持久,使其有资格进行进一步的药理学和临床研究。