title: [Design, synthesis and antiepileptic activity of 4-(2-acetoxybenzoylamino) butyrate derivatives].
abstract: A series of 4-(2-acetoxybenzoylamino) butyrate derivatives were designed and synthesized. All of the novel 12 compounds (7a-7k) were synthesized from gamma-aminobutyric acid (1) as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that most of these title compounds possessed antiepileptic activity. Compounds 7i-7k displayed strong antiepileptic activity and are worth for further development. Compounds 4, 7d-7h showed moderate antiepileptic activity. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyrate derivatives is also discussed preliminarily.
authors.affiliation: Department of Pharmacology, North Sichuan Medical College, NanChong 637000, China.
authors.forename: Wen-Hu
authors.initials: WH
authors.lastname: Liu
authors.forename: Dian
authors.initials: D
authors.lastname: He
authors.forename: Xin-Qiang
authors.initials: XQ
authors.lastname: Yin
authors.forename: Yi
authors.initials: Y
authors.lastname: Liu
mesh_terms: D015761:4-Aminopyridine; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D002087:Butyrates / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D015195:Drug Design; D004827:Epilepsy / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011897:Random Allocation; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000737:chemistry*
chemical_list: D000927:Anticonvulsants; D002087:Butyrates; D005680:gamma-Aminobutyric Acid; D015761:4-Aminopyridine