Peptidoaminobenzophenones, a novel class of ring-opened derivatives of 1,4-benzodiazepines
作者:Kentaro Hirai、Teruyuki Ishiba、Hirohiko Sugimoto、Kazuyuki Sasakura、Toshio Fujishita、Tatsuro Toyoda、Yuji Tsukinoki、Hirokuni Joyama、Hisao Hatakeyama、Katsumi Hirose
DOI:10.1021/jm00181a013
日期:1980.7
the corresponding NH derivatives. Some compounds had very high activities in antipentylenetetrazole and antifighting tests in mice when orally administered. Very weak toxicity was also found in these compounds. Water solubility of the peptidoaminobenzophenones and their salts were tested. Possible in these compounds. Water solubility of the peptidoaminobenzophenones and their salts were tested. Possible
已通过几种途径制备了一系列新的肽氨基二苯甲酮,并对其中枢神经系统活性进行了评估。讨论了系列中的结构-活动关系。通常,二肽基-N-甲基氨基二苯甲酮显示出比相应的NH衍生物更高的活性。口服时,某些化合物在抗戊烯四唑和小鼠抗战斗试验中具有很高的活性。在这些化合物中也发现非常弱的毒性。测试了肽氨基二苯甲酮及其盐的水溶性。这些化合物中可能存在。测试了肽氨基二苯甲酮及其盐的水溶性。还讨论了通过末端氨基酸的酶促裂解将肽氨基二苯甲酮进行体内转化,然后化学环化成1,4-苯并二氮杂ze的方法。