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). Pharmacologica...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.展开更多
Melting point (T_m), melting enthalpy (△H_m), melting entropy (△S_m) are important thermodynamic parameters of compounds. The thermodynamic parameters of a series of β-substituted para-chlorocinnamamides were first...Melting point (T_m), melting enthalpy (△H_m), melting entropy (△S_m) are important thermodynamic parameters of compounds. The thermodynamic parameters of a series of β-substituted para-chlorocinnamamides were first reported in this note. Cinnamamides display a variety of pharmacological actions. The relationship between their structure and anticonvulsant activity in particular has been studied extensively. Literature reported that the partition coefficient (log p, octanol/water), dipole moment and inductive effect index (Ⅰ) of the compounds,展开更多
Arylation of acrylamide and acrylonitrile were carried out with various arenediazonium tetrafluoroborates in the presence of a catalytic amount of Pd(OAc)(2) in ethanol and a variety of substituted (E)-cinnamamides an...Arylation of acrylamide and acrylonitrile were carried out with various arenediazonium tetrafluoroborates in the presence of a catalytic amount of Pd(OAc)(2) in ethanol and a variety of substituted (E)-cinnamamides and (E)-cinnamonitriles were obtained in high yields under mild reaction conditions.展开更多
Two new cinnamamide derivatives designated as cimicifugamide((?))and isocimicifu- gamide((?)),have been isolated from the rhizomes of Cimicifuga dahurica(Turcz.)Maxim..Their structures were established based on spectr...Two new cinnamamide derivatives designated as cimicifugamide((?))and isocimicifu- gamide((?)),have been isolated from the rhizomes of Cimicifuga dahurica(Turcz.)Maxim..Their structures were established based on spectral evidence as N-(3'-methoxy-4'-hydroxyphenethyl)- 4-0-β-D-galactopyrano syl-ferulamide(E)and N-(3'-methoxy-4'-hydroxyphenetnyl)-4-0-β-D-ga- lactopyranosyl-isoferulamide(Z)respectively.展开更多
基金Projects Supported by the National Fund of Natural Sciences
文摘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.
文摘Melting point (T_m), melting enthalpy (△H_m), melting entropy (△S_m) are important thermodynamic parameters of compounds. The thermodynamic parameters of a series of β-substituted para-chlorocinnamamides were first reported in this note. Cinnamamides display a variety of pharmacological actions. The relationship between their structure and anticonvulsant activity in particular has been studied extensively. Literature reported that the partition coefficient (log p, octanol/water), dipole moment and inductive effect index (Ⅰ) of the compounds,
基金This work was supported by the Natural Science Foundation of Jiangxi Province.
文摘Arylation of acrylamide and acrylonitrile were carried out with various arenediazonium tetrafluoroborates in the presence of a catalytic amount of Pd(OAc)(2) in ethanol and a variety of substituted (E)-cinnamamides and (E)-cinnamonitriles were obtained in high yields under mild reaction conditions.
文摘Two new cinnamamide derivatives designated as cimicifugamide((?))and isocimicifu- gamide((?)),have been isolated from the rhizomes of Cimicifuga dahurica(Turcz.)Maxim..Their structures were established based on spectral evidence as N-(3'-methoxy-4'-hydroxyphenethyl)- 4-0-β-D-galactopyrano syl-ferulamide(E)and N-(3'-methoxy-4'-hydroxyphenetnyl)-4-0-β-D-ga- lactopyranosyl-isoferulamide(Z)respectively.
