Design, synthesis and anticonvulsive activities of potential prodrugs linked by two-carbon chain.
For the development of new anticonvulsive agents, GABAmimetics such as nipecotic acid, isonipecotic acid, gamma-aminobutyric acid (GABA), gamma-vinyl GABA (vigabatrin) and valproic acid were covalently coupled through an ester bond by a two-carbon linker chain as potential pro-drugs and evaluated for their anticonvulsive activities.
Zhao
Long-Xuan
LX
College of Pharmacy, Yeungnam University, Kyongsan 712-749, Korea.
Moon
Yoon-Soo
YS
Basnet
Arjun
A
Park
Jae Gyu
JG
Kim
Eun-kyung
EK
Kim
Dae-Ok
DO
Jeong
Tae Cheon
TC
Jahng
Yurngdong
Y
Choi
Jongwon
J
Lee
Eung-Seok
ES
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D002244:Carbon / Q000737:chemistry*; D003292:Convulsants / Q000008:administration & dosage / Q000009:adverse effects / Q000037:antagonists & inhibitors; D019281:Dimerization; D015195:Drug Design; D004597:Electroshock / Q000009:adverse effects; D007274:Injections, Intraperitoneal; D007279:Injections, Subcutaneous; D007540:Isonipecotic Acids / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D008024:Ligands; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009557:Nipecotic Acids / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D011355:Prodrugs / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy / Q000503:physiopathology; D014635:Valproic Acid / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D020888:Vigabatrin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D005680:gamma-Aminobutyric Acid / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics
D000927:Anticonvulsants; D003292:Convulsants; D007540:Isonipecotic Acids; D008024:Ligands; D009557:Nipecotic Acids; D011355:Prodrugs; D005680:gamma-Aminobutyric Acid; D014635:Valproic Acid; D002244:Carbon; D020888:Vigabatrin