Dhasmana A, Mehrotra S, Gupta T K, Bhargava K P, Parmar S S, Barthwal J P
Arzneimittelforschung. 1984;34(9):943-5.
A new series of 2,3-cyclopentano-3,4-dihydro-4-spirocyclopentano-1,5-benzodi azepine which are substituted in 5-position with beta-N-heterocycloethyl or gamma-N-heterocyclo-n-propyl groups have been synthesized and evaluated for their CNS depressant activity including anticonvulsant, analgesic and pentobarbital induced hypnosis. These compounds were also investigated for their ability to inhibit in vitro succinate dehydrogenase (SDH). In most of the compounds an appreciable CNS depressant activity has been found to be associated with the compounds possessing good SDH inhibitory activity. Low toxicity of these compounds was reflected by their high approximate LD50 values.
合成了一系列新的2,3-环戊烷并-3,4-二氢-4-螺环戊烷-1,5-苯并二氮杂卓，其5-位被β-N-杂环乙基或γ-N-杂环正丙基取代，并对其进行了中枢神经系统抑制活性评估，包括抗惊厥、镇痛和戊巴比妥诱导的催眠作用。还研究了这些化合物体外抑制琥珀酸脱氢酶（SDH）的能力。在大多数化合物中，已发现明显的中枢神经系统抑制活性与具有良好SDH抑制活性的化合物相关。这些化合物的高近似半数致死量值反映出它们的低毒性。
