Cignarella G, Pirisino G, Loriga M, Dorigotti L
Farmaco Sci. 1977 Apr;32(4):296-302. doi: 10.1002/chin.197736270.
A series of cis and trans N1-arylalkyl-N4-(2'-pyridyl)-2'6-dimethylpiperazines were synthetized and tested as adrenolytic and vasodilator agents. The N1-substitution with the 3,4-dimethoxyphenethyl group seems the most promising with regard to pharmacological activity, which was found to reside mainly in the trans isomer (3-II b). The adrenolytic activity of (3-II b) is comparable with that of the related 2-methyl derivative (1-III), while it is higher than that of (IV) in which the piperazine nucleus is C-unsubstituted.
合成了一系列顺式和反式N1-芳基烷基-N4-(2'-吡啶基)-2',6-二甲基哌嗪,并作为肾上腺能阻滞剂和血管扩张剂进行了测试。就药理活性而言,用3,4-二甲氧基苯乙基进行N1-取代似乎最有前景,发现药理活性主要存在于反式异构体(3-II b)中。(3-II b)的肾上腺能阻滞活性与相关的2-甲基衍生物(1-III)相当,而高于哌嗪核未被碳取代的(IV)。