Prudchenko I A, Stashevskaia L V, Mikhaleva I I, Ivanov V T, Shandra A A, Godlevskiĭ L S, Mazarati A M
Bioorg Khim. 1993 Jan;19(1):43-55.
To study structure-functional relationship in the series of DSIP, eleven DSIP analogues varying in positions 1, 2 and 6 were synthesized by the solid-phase method using both Boc- and Fmoc-approaches. The antiepileptic action of these analogues was compared with that of DSIP. The seizure activity was induced by the corazol or picrotoxin i. p. injection. Some analogues proved more efficient as antiepileptic agents than DSIP after their central (50 micrograms/kg in rats) and peripheral (1.0 mg/kg in mice) administration.
为了研究一系列DSIP中的结构-功能关系,采用Boc法和Fmoc法通过固相法合成了11种在第1、2和6位有所不同的DSIP类似物。将这些类似物的抗癫痫作用与DSIP的进行了比较。惊厥活性通过腹腔注射戊四氮或印防己毒素诱导。一些类似物经中枢给药(大鼠50微克/千克)和外周给药(小鼠1.0毫克/千克)后,证明作为抗癫痫药比DSIP更有效。