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 fo...

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Bibliographic Details
Published in:Archives of pharmacal research 2003-10, Vol.26 (10), p.785-795
Main Authors: Zhao, Long-Xuan, Moon, Yoon-Soo, Basnet, Arjun, Park, Jae Gyu, Kim, Eun-kyung, Kim, Dae-Ok, Jeong, Tae Cheon, Jahng, Yurngdong, Choi, Jongwon, Lee, Eung-Seok
Format: Article
Language:English
Subjects:
Animals
Anticonvulsants - chemical synthesis
Anticonvulsants - pharmacology
Carbon - chemistry
Convulsants - administration & dosage
Convulsants - adverse effects
Convulsants - antagonists & inhibitors
Dimerization
Drug Design
Electroshock - adverse effects
gamma-Aminobutyric Acid - administration & dosage
gamma-Aminobutyric Acid - chemistry
gamma-Aminobutyric Acid - pharmacokinetics
Injections, Intraperitoneal
Injections, Subcutaneous
Isonipecotic Acids - administration & dosage
Isonipecotic Acids - chemistry
Isonipecotic Acids - pharmacokinetics
Ligands
Male
Mice
Mice, Inbred ICR
Nipecotic Acids - administration & dosage
Nipecotic Acids - chemistry
Nipecotic Acids - pharmacokinetics
Prodrugs - chemical synthesis
Prodrugs - metabolism
Prodrugs - pharmacology
Seizures - chemically induced
Seizures - drug therapy
Seizures - physiopathology
Valproic Acid - administration & dosage
Valproic Acid - chemistry
Valproic Acid - pharmacokinetics
Vigabatrin - administration & dosage
Vigabatrin - chemistry
Vigabatrin - pharmacokinetics
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Description
Summary: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.
ISSN:0253-6269
1976-3786
DOI:10.1007/BF02980021