Design and synthesis of anticonvulsive agents as gamma-vinyl GABA-based potential dual acting prodrugs and their biological activities.
For the development of new anticonvulsive agents, gamma-vinyl GABA (vigabatrin) and GABA mimetics derivatives were covalently coupled as potential dual acting prodrugs and evaluated for their anticonvulsive activities. Among the prepared compounds, 11 showed the most potent anticonvulsive activity, a shorter onset time and a broader spectrum compared to vigabatrin.
Kim
Y C
YC
College of Pharmacy, Yeungnam University, Kyongsan, South Korea.
Zhao
L X
LX
Kim
T H
TH
Je
S M
SM
Kim
E K
EK
Choi
H
H
Chae
W G
WG
Park
M
M
Choi
J
J
Jahng
Y
Y
Lee
E S
ES
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D001640:Bicuculline; D015195:Drug Design; D051379:Mice; D010433:Pentylenetetrazole; D010852:Picrotoxin; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy; D020888:Vigabatrin / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use
D000927:Anticonvulsants; D001640:Bicuculline; D010433:Pentylenetetrazole; D010852:Picrotoxin; D011355:Prodrugs; D020888:Vigabatrin