title: Design, synthesis and anticonvulsive activity of analogs of gamma-vinyl GABA.
abstract: For the development of new anticonvulsive agents, analogs of gamma-vinyl GABA (vigabatrin) containing GABA, gamma-vinyl GABA, valproic acid, nipecotic acid or isonipecotic acid moieties were prepared and evaluated for their anticonvulsive activities. Most of the prepared compounds showed moderate anticonvulsive activities. Among them compounds 10 and 16 displayed the most potent anticonvulsive activity and a broader spectrum compared to vigabatrin.
authors.affiliation: Department of Chemistry, Liaoning Normal University, Dalian, Liaoning 116-029, P.R.China.
authors.forename: Long-Xuan
authors.initials: LX
authors.lastname: Zhao
authors.forename: Jae Gyu
authors.initials: JG
authors.lastname: Park
authors.forename: Yoon-Soo
authors.initials: YS
authors.lastname: Moon
authors.forename: Arjun
authors.initials: A
authors.lastname: Basnet
authors.forename: Jongwon
authors.initials: J
authors.lastname: Choi
authors.forename: Eun-Kyung
authors.initials: EK
authors.lastname: Kim
authors.forename: Tae Cheon
authors.initials: TC
authors.lastname: Jeong
authors.forename: Yurngdong
authors.initials: Y
authors.lastname: Jahng
authors.forename: Eung-Seok
authors.initials: ES
authors.lastname: Lee
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000627:therapeutic use; D004195:Disease Models, Animal; D015195:Drug Design; D007540:Isonipecotic Acids / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D009557:Nipecotic Acids / Q000737:chemistry / Q000494:pharmacology; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D014635:Valproic Acid / Q000737:chemistry / Q000494:pharmacology; D020888:Vigabatrin / Q000138:chemical synthesis* / Q000627:therapeutic use
chemical_list: D000927:Anticonvulsants; D007540:Isonipecotic Acids; D009557:Nipecotic Acids; C030278:nipecotic acid; D014635:Valproic Acid; D020888:Vigabatrin