Synthesis and pharmacological properties of some dipyrido[1,3]diazepinones.

L Kaczmarek, P Nantka-Namirski, A Kłodzińska, B Bujak, E Tatarczyńska
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Abstract

The synthesis of two isomeric dipyrido[1,3]diazepinones (3a,4) and N-monosubstituted derivatives of 3a by cyclocondensation of corresponding bipyridinediamines (1, 2) with urea was described. The alkylation of 3a and 4 with alkyl halides 6 in K2CO3/DMF/TBAB system gave N,N'-disubstituted compounds 7 and 8. Dipyrido[1,3]diazepinones 8a and 3b-d showed a weak general depressive action on the central nervous system and they were also devoid of antidepressant, anxiolytic, anticonvulsant and serotoninolytic or serotoninomimetic properties.

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一些双嘧多[1,3]二氮卓酮类化合物的合成及药理性质。
本文报道了用相应的联吡啶二胺(1,2)与尿素环缩合法制备两种异构体双吡啶[1,3]二氮卓酮(3a,4)及其n -单取代衍生物。在K2CO3/DMF/TBAB体系中,3a和4与烷基卤化物6烷基化,得到N,N'-二取代化合物7和8。双嘧多[1,3]、二氮卓酮8a和3b-d对中枢神经系统有较弱的全身抑制作用,且不具有抗抑郁、抗焦虑、抗惊厥和5 -羟色胺或拟5 -羟色胺的特性。
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