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本文报道22个奎宁环类和托品类双季铵和多季铵化合物的合成及其对膈肌膈神经标本的抑制作用。初步试验表明,带有草酰胺链的化合物较其他链[—(CH_2)_6—或—CH_2OCH_2—]的好。通过这两类化合物的构效分析,看出化合物中即便具有神经节阻断剂作用的短链(3,6或8个原子),但如在分子的氨基部分以较庞大的环状基团奎宁环或托品(分别带有适当取代基)替代成为大季铵头时,则转化为神经肌肉阻断作用。
This article reports the synthesis of 22 quinuclidine and tropine double quaternary ammonium and polyquaternium compounds and their inhibitory effect on the phrenic nerve diaphragm specimens. Preliminary experiments show that compounds with oxalate chains are better than other chains [- (CH_2) _6- or -CH_2OCH_2-]. Through the structure-activity analysis of these two compounds, it can be seen that even short-chain (3, 6 or 8 atoms) which have the function of ganglion blocker in the compound can be obtained by using the bulky cyclic group Quinuclidine or Tropsch (with appropriate substituents, respectively) instead of a large quaternary ammonium head translates into neuromuscular blockade.