Archibald J L, Beardsley D R, Bisset G M, Fairbrother P, Jackson J L, Opalko A, Ward T J
J Med Chem. 1980 Aug;23(8):857-61. doi: 10.1021/jm00182a009.
The synthesis of a series of 1-aralkyl-4-ureidopiperidines is reported. These compounds are related to the benzamidopiperidines exemplified by indoramin. Some of the ureidopiperidines are more potent antihypertensive agents than their benzamidopiperidine counterparts. Two examples, 1-(2-thenoyl)-3-[1-[2-(3-indolyl)ethyl]piperid-4-yl]urea and 1-(2-thenoyl)-3-[1-[4-(4-fluorophenyl)-4-oxobutyl]piperid-4-yl]urea (19 and 58), emerged as the most potent antihypertensive agents in this series.
报道了一系列1-芳烷基-4-脲基哌啶的合成。这些化合物与以吲哚拉明为代表的苯甲酰胺基哌啶有关。一些脲基哌啶作为抗高血压药比其对应的苯甲酰胺基哌啶更有效。两个例子,1-(2-噻吩甲酰基)-3-[1-[2-(3-吲哚基)乙基]哌啶-4-基]脲和1-(2-噻吩甲酰基)-3-[1-[4-(4-氟苯基)-4-氧代丁基]哌啶-4-基]脲(19和58),是该系列中最有效的抗高血压药。