DESIGN OF DUAL ACTING ANTICONVULSANT-ANTIMUSCARINIC SUCCINIMIDE AND HYDANTOIN DERIVATIVES

Authors
HUDKINS RL DEHAVENHUDKINS DL DOUKAS P
Citation
Rl. Hudkins et al., DESIGN OF DUAL ACTING ANTICONVULSANT-ANTIMUSCARINIC SUCCINIMIDE AND HYDANTOIN DERIVATIVES, Bioorganic & medicinal chemistry letters, 7(8), 1997, pp. 979-984
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
8
Year of publication
1997
Pages
979 - 984
Database
ISI
SICI code
0960-894X(1997)7:8<979:DODAAS>2.0.ZU;2-O
Abstract
A series of 4-dialkylamino-2-butynyl-succinimide and -hydantoin deriva tives were designed containing pharmacophoric elements for dual acting anticonvulsant and antimuscarinic activity. Potent anticonvulsant age nts were identified with an extremely rapid onset of protective activi ty. Succinimides 13 and 18 exhibited ED50 values of 20 and 9.6 mg/kg 1 0 minutes after administration in the MES seizure model and also exhib ited good binding affinity for the M-1 muscarinic receptor. (C) 1997 E lsevier Science Ltd.