title: [Synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds].
abstract: It has been demonstrated by our previous research that 4-(2-acetoxybenzoylamino) butyramide derivatives exhibited good antiepileptic activities. In this paper, to explore the SAR and improve the antiepileptic activities of these derivatives, a series of novel 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds (5a-5n) were synthesized and biologically evaluated. Their structures were confirmed by 1H MNR, ESI-MS and elemental analysis. Pharmacological test in vivo showed that target compounds (5f, 5i-5n) displayed strong antiepileptic activities on 4-AP induced epilepsy in mice with ED50 values ranging from 0.3137 to 0.3604 mmol x kg(-1).
authors: Department of Pharmacology, North Sichuan Medical College, Nanchong 637007, China. lwh790214@163.com
authors: Wen-Hu
authors: WH
authors: Liu
authors: Shi-Bao
authors: SB
authors: Wang
authors: Yi
authors: Y
authors: Liu
mesh_terms: D015761:4-Aminopyridine; D000577:Amides / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004827:Epilepsy / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011897:Random Allocation; D018079:Receptors, GABA / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C582234:4-(2-acetoxybenzoylamino)butyramide; D000577:Amides; D000927:Anticonvulsants; D018079:Receptors, GABA; D015761:4-Aminopyridine