Design and synthesis of anticonvulsive agents as gamma-vinyl GABA-based potential dual acting prodrugs and their biological activities

Authors
Kim, YC Zhao, LX Kim, TH Je, SM Kim, EK Choi, H Chae, WG Park, M Choi, J Jahng, Y Lee, ES
Citation
Yc. Kim et al., Design and synthesis of anticonvulsive agents as gamma-vinyl GABA-based potential dual acting prodrugs and their biological activities, BIOORG MED, 10(7), 2000, pp. 609-613
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
7
Year of publication
2000
Pages
609 - 613
Database
ISI
SICI code
0960-894X(20000403)10:7<609:DASOAA>2.0.ZU;2-J
Abstract
For the development of new anticonvulsive agents, gamma-vinyl GABA (vigabat rin) and GABA mimetics derivatives were covalently coupled as potential dua l 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. (C) 200 0 Elsevier Science Ltd. All rights reserved.