SYNTHESIS AND CHARACTERIZATION OF ACENAPHTH-5-YL)-N'-(4-METHOXYNAPHTH-1-YL)GUANIDINE AS A GLUTAMATE RELEASE INHIBITOR AND POTENTIAL ANTIISCHEMIC AGENT

Authors
REDDY NL CONNAUGHTON S DALY D FISCHER JB
Citation
Nl. Reddy et al., SYNTHESIS AND CHARACTERIZATION OF ACENAPHTH-5-YL)-N'-(4-METHOXYNAPHTH-1-YL)GUANIDINE AS A GLUTAMATE RELEASE INHIBITOR AND POTENTIAL ANTIISCHEMIC AGENT, Bioorganic & medicinal chemistry letters, 5(19), 1995, pp. 2259-2262
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
19
Year of publication
1995
Pages
2259 - 2262
Database
ISI
SICI code
0960-894X(1995)5:19<2259:SACOA>2.0.ZU;2-H
Abstract
Structure-activity relationship (SAR) studies of N,N'-diarylguanidines as glutamate release inhibitors led to the synthesis of acenaphth-5-y l)-N'-(4-methoxynaphth-1-yl)guanidine (6). Compound 6, with IC50 value s of 1.3 and 2.2 mu M in C-14-guanidine flux and Ca-45(2+)-flux assays respectively, effectively inhibited both veratridine and K+-evoked gl utamate release in rat brain synaptosomal preparations.