Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH₃ or 2-CH₃

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• 作者：Agnieszka Gunia-Krzyżak^a ; ^{agnieszka.gunia@uj.edu.pl} ; Dorota Żelaszczyk^a ; Anna Rapacz^b ; Ewa Żesławska^c ; Anna M. Waszkielewicz^a ; Katarzyna Pańczyk^a ; Karolina Słoczyńska^d ; Elżbieta Pękala^d ; Wojciech Nitek^e ; Barbara Filipek^b ; Henryk Marona^a
• 关键词：Anticonvulsant ; Cinnamamide ; Crystal structure ; MES ; Pharmacophore ; scPTZ ; 6-Hz
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：25
• 期：2
• 页码：471-482
• 全文大小：1248 K
• 卷排序：25

文摘

(E)-N-cinnamoyl derivatives of aminoalkanols were tested in rodents. Maximal electroshock, subcutaneous pentylenetetrazole and 6-Hz tests were performed. Anticonvulsant activity was enhanced by p-Cl and o-CH3 substitution in phenyl ring. Benzodiazepine receptors and serotonergic receptors were possible molecular targets. Tested compounds were stable in rat liver microsomes model of biotransformation.