Synthesis of 3-amino-3,4-dihydro-2(1<i>H</i>)-quinazolinones as potential anticonvulsants
作者:M. J. Kornet、T. Varia、W. Beaven
DOI:10.1002/jhet.5570210627
日期:1984.11
4-dihydro-2(1H)-quinazolinones have been synthesized from ethyl chloroformate and o-aminobenzylhydrazines. The latter compounds were obtained from the metal hydride reduction of either o-aminobenzhydrazides or o-acylaniline hydrazones. All compounds were evaluated in mice in the maximal electroshock (MES) seizure and pentylenetetrazole (sc Met) seizure threshold tests for anticonvulsant activity and in
由氯甲酸乙酯和邻氨基苄基肼合成了十三种3-氨基-3,4-二氢-2(1 H)-喹唑啉酮。后者的化合物是从邻氨基苯甲酰肼或邻苯二甲酰的金属氢化物还原获得的。在小鼠的最大电击(MES)癫痫发作和戊四氮(sc Met)癫痫发作阈值试验中评估了所有化合物的抗惊厥活性,并在Rotodod试验中确定了神经毒性。其中的五种化合物在一项或两项测试中以300 mg / kg或更低的剂量显示出活性。活性最高的化合物是3-二甲基氨基-3,4-二氢-2(1 H)-喹唑啉酮。