Design, synthesis and anticonvulsive activity of analogs of gamma-vinyl GABA.
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.
Zhao
Long-Xuan
LX
Department of Chemistry, Liaoning Normal University, Dalian, Liaoning 116-029, P.R.China.
Park
Jae Gyu
JG
Moon
Yoon-Soo
YS
Basnet
Arjun
A
Choi
Jongwon
J
Kim
Eun-Kyung
EK
Jeong
Tae Cheon
TC
Jahng
Yurngdong
Y
Lee
Eung-Seok
ES
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
D000927:Anticonvulsants; D007540:Isonipecotic Acids; D009557:Nipecotic Acids; C030278:nipecotic acid; D014635:Valproic Acid; D020888:Vigabatrin