Neuropharmacology Laboratory, Department of Pharmacology, Institute of Medical Sciences, Banares Hindu University, Varanasi, India.
Pharm Res. 1985 Jan;2(1):49-52. doi: 10.1023/A:1016374224529.
Thirty-three N (3)-2-, -3- or -4-substituted aryl-N (1)-(alkyl/aryl/substituted aryl)-triazene N (1)-oxides were synthesized and evaluated for their anticonvulsant and monoamine oxidase (MAO) inhibitory activities. Most of the compounds exhibited MAO inhibitory activity in vitro, and kinetic studies conducted with N (3)-4-chlorophenyl-N (1)-methyltriazene N (1)-oxide, the most potent inhibitor, showed that the inhibition is non-competitive in nature. The MAO inhibiting activity of the compounds correlated well with their anticonvulsant effect against maximal electroshock-induced seizures in rats. Acute toxicity studies indicate that the compounds have a wide margin of safety.
合成了 33 个 N(3)-2-、-3-或-4-取代芳基-N(1)-(烷基/芳基/取代芳基)-三氮烯 N(1)-氧化物,并评估了它们的抗惊厥和单胺氧化酶(MAO)抑制活性。大多数化合物表现出体外 MAO 抑制活性,对抑制作用最强的 N(3)-4-氯苯基-N(1)-甲基三氮烯 N(1)-氧化物进行的动力学研究表明,抑制作用具有非竞争性性质。化合物的 MAO 抑制活性与其对大鼠最大电休克诱导惊厥的抗惊厥作用密切相关。急性毒性研究表明,这些化合物具有很大的安全性。