Influence of Alkylamides of Glutamic Acid and Related Compounds on the Central Nervous System. II. Syntheses of Amides of Glutamic Acid and Related Compounds, and Their Effects on the Central Nervous System
作者:RYOHEI KIMURA、TOSHIRO MURATA
DOI:10.1248/cpb.19.1301
日期:——
Eleven kinds of 5-alkylamides of L-and DL-glutamic acid were synthesized and assessed for anticonvulsant effects. Against lethal convulsion induced by caffeine, maximum efficacy was observed with alkylamides possessing C7 to C8 alkyl radicals in the position 5 of glutamic acid, and the compounds having C5 to C7 alkyl groups were shown to have the highest toxity. Differences in the response between L-compound and DL-compound are not significant. Synthesized ω-alkylamides of L-glutamic acid, L-aspartic acid and DL-2-aminoadipic acid did neither increase nor decrease the oxygen consumption by the rat brain cortex slices.
合成了十一种L-和DL-谷氨酸的5-烷基酰胺,并评估了其抗癫痫效果。在咖啡因诱导的致命性抽搐中,观察到具有C7至C8烷基基团的烷基酰胺在谷氨酸的5位具有最大的效能,而具有C5至C7烷基的化合物显示出最高的毒性。L-化合物和DL-化合物之间的反应差异并不显著。合成的L-谷氨酸、L-天冬氨酸和DL-2-氨基己二酸的ω-烷基酰胺既没有增加也没有减少大鼠脑皮层切片的氧气消耗。