合成クラーレ作用物質の効力と化学構造との関係

抄録

Many reports have indicated that numerous rules can be established as to the relationship detween the chemical structure and activity of curariform substanes. Pharmacological examination of the 20 kinds of compounds of this series synthesized revealed the following results.
1) It is a fact that the distance between the quaternary nitrogens is about 15°A but it was found that some variation appears by the manner of the binding bridge.
2) It was experimentally recognized that the activity is stronger when the nitrogencontaining ring is saturated than when unsaturated.
3) The rule that the activity is stronger when there is a methoxyl group in the nitrogencontaining ring, than when it is a hydroxyl or when there is no substituent was developed further to show that the activity is stronger in one with a methoxyl group than a methylenedioxy group, and in one with a larger number of the methoxyl groups.
4) No report has appeared to date regarding stereoisomers but the present experiments revealed that there were no marked differences in stereoisomers as to activity or lethal dose.