|Budget Amount *help
¥2,100,000 (Direct Cost : ¥2,100,000)
Fiscal Year 1991 : ¥1,100,000 (Direct Cost : ¥1,100,000)
Fiscal Year 1990 : ¥1,000,000 (Direct Cost : ¥1,000,000)
|Keywords||Camphor-1, 2, 3-triazine / CNS stimulant activity / Structure activity relationship / Pharmacophore / 構造活性相関 / カンファ-1,2,4ートリアジン / 主作用団 / ヘテロ環縮合カンファ-1,2,4ートリアジン類 / カンファー1,2,3ートリアジン / 中枢興奮作用 / 活性コンホメ-ション / ヒドラジノカンファー1,2,4ートリアジン / ヘテロ環の構築|
In order to clarify the relationship between structure and central nervous system(CNS)stimulant activity of camphor-1, 2, 3-triazine and related compounds, the isomeric 3-amino- or 3-hydrazino-camphor-1, 2, 4triazine was employed as building blocks for the synthesis of a series of camphor-1, 2, 4-triazines fused with imidazole, 1, 2, 4-triazole, thiodiazole, tetrazole-and pyrimidine.
The CNS stimulant activity of the obtained compounds was evaluated using mice. Among the tested compounds, 3-hydrazino-camphor-1, 2, 4-triazine showed the most potent activity and camphor-1, 2, 4-triazines fused with tetrazole and 1, 2, 4-triazole were potent. From these observations, it was concluded that the C-3 substituent of camphor-1, 2, 4-triazine consisted of a N-N bonding should be the essential pharmacophore for the CNS stimulant activity, because the replacement of a N-N group by a N-C group resulted in disappearance of the activity.