Rubat C, Coudert P, Couquelet J M, Tronche P, Bastide J, Bastide P
Laboratoire de Chimie Therapeutique, Faculté de Pharmacie, Clermont-Ferrand, France.
Farmaco. 1990 Mar;45(3):331-40. doi: 10.1002/chin.199048183.
A series of 6,8-diaryl-1,2,4-triazolo[4,3-b] and 1,2,3,4-tetrazolo[1,5-b]pyridazines was synthesized from suitable chloropyridazines. The compounds were screened in mice for their ability to antagonize maximal electroshock-, pentylenetetrazole- and bicuculline-induced seizures; sedative effects were evaluated by a study of the spontaneous motor activity. Some of pyridazine derivatives exhibited appreciable anticonvulsant activity. Substituting the phenyl ring in the 6-position with an halogen atom led to a substantial increase of activity. Furthermore, none of the compounds was notably active in tests predictive of anxiolytic activity.
由合适的氯代哒嗪合成了一系列6,8 - 二芳基 - 1,2,4 - 三唑并[4,3 - b]和1,2,3,4 - 四唑并[1,5 - b]哒嗪。在小鼠中筛选这些化合物对抗最大电休克、戊四氮和荷包牡丹碱诱发癫痫发作的能力；通过对自发运动活动的研究评估其镇静作用。一些哒嗪衍生物表现出明显的抗惊厥活性。在6 - 位用卤原子取代苯环导致活性大幅增加。此外，在预测抗焦虑活性的试验中，没有一种化合物具有显著活性。
