Studies on the Relationship Between the Structure and Anticonvulsant Activity of Cinnamamides and Their Analogs

高等学校化学研究 ›› 1989, Vol. 5 ›› Issue (2): 125-137.

Studies on the Relationship Between the Structure and Anticonvulsant Activity of Cinnamamides and Their Analogs

Wang Shuyu, Li Renli, Liu Weichin

School of Pharmaceutical Sciences, Beijing Medical University, Beijing

收稿日期:1988-05-05 出版日期:1989-04-24 发布日期:2011-09-09
基金资助:
Projects Supported by the National Fund of Natural Sciences

Studies on the Relationship Between the Structure and Anticonvulsant Activity of Cinnamamides and Their Analogs

Wang Shuyu, Li Renli, Liu Weichin

School of Pharmaceutical Sciences, Beijing Medical University, Beijing

Received:1988-05-05 Online:1989-04-24 Published:2011-09-09
Supported by:
Projects Supported by the National Fund of Natural Sciences

摘要/Abstract

摘要： On the basis of systematic modification of the structure of componds of antiepilepsirine type, more than 200 cinnamamides were synthesized and tested by animal assay (maximal electroshock seizure, MES).Pharmacological evaluation showed that the configuration and the substituents on the phenyl ring and the nitrogen of amides, and substituents on the double bond displayed an important effect on the anticonvulsant activity.For studying the effect of the modification of structure to anticonvulsant activity, Hansch approach was employed to study the QSAR among 38 cinnamamides, and Hopfinger's MSA was employed to study the MSA-QSAR among 26 cinnamamides.

关键词: Cinnamamides, Anticonvulsant activity, Cinf iguration, QSAR, MAS

Abstract: On the basis of systematic modification of the structure of componds of antiepilepsirine type, more than 200 cinnamamides were synthesized and tested by animal assay (maximal electroshock seizure, MES).Pharmacological evaluation showed that the configuration and the substituents on the phenyl ring and the nitrogen of amides, and substituents on the double bond displayed an important effect on the anticonvulsant activity.For studying the effect of the modification of structure to anticonvulsant activity, Hansch approach was employed to study the QSAR among 38 cinnamamides, and Hopfinger's MSA was employed to study the MSA-QSAR among 26 cinnamamides.

Key words: Cinnamamides, Anticonvulsant activity, Cinf iguration, QSAR, MAS

Wang Shuyu, Li Renli, Liu Weichin . Studies on the Relationship Between the Structure and Anticonvulsant Activity of Cinnamamides and Their Analogs[J]. 高等学校化学研究, 1989, 5(2): 125-137.

Wang Shuyu, Li Renli, Liu Weichin . Studies on the Relationship Between the Structure and Anticonvulsant Activity of Cinnamamides and Their Analogs[J]. Chemical Research in Chinese Universities, 1989, 5(2): 125-137.

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Studies on the Relationship Between the Structure and Anticonvulsant Activity of Cinnamamides and Their Analogs

Studies on the Relationship Between the Structure and Anticonvulsant Activity of Cinnamamides and Their Analogs

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