| Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites. | |
| | |
MedLine Citation:
|
PMID: 3031294 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Baclofen (beta-p-chlorophenyl-GABA) is the only selective agonist for the bicuculline-insensitive GABAB receptor. We report the synthesis of new GABA analogues and baclofen analogues. In vitro, two compounds, 4-amino-3-benzo[b]furan-2-ylbutanoic acid (9g) and 4-amino-3-(5-methoxybenzo[b]furan-2-yl)butanoic acid (9h), showed an affinity for the GABAB receptor. The results obtained with racemic compounds of benzofuran structure, new for this series, and the surprising inactivity of compound 3a (4-amino-3-(4-hydroxyphenyl)butanoic acid) permit the proposal of an hypothesis for the structure-activity relationships with regard to GABAB receptor. |
| | |
Authors:
|
P Berthelot; C Vaccher; A Musadad; N Flouquet; M Debaert; M Luyckx |
Related Documents
:
|
20490464 - Evaluation of the biological effects of (s)-dimethyl 2-(3-(phenyltellanyl) propanamido)... 20045404 - Discovery and characterization of a novel potent, selective and orally active inhibitor... 16613724 - Amino acid derivatives. part i. synthesis, antiviral and antitumor evaluation of new al... 3486134 - Research on heterocyclic compounds. xix--2-methylimidazo[1,2-a]pyridine-3-acetic acids. 8500204 - Absolute configuration of l-methionine sulfoximine as a toxic principle in cnestis pala... 17306914 - Comparison of dietary triacylglycerol oil and diacylglycerol oil in protein kinase c ac... |
Publication Detail:
|
Type: Comparative Study; Journal Article |
Journal Detail:
|
Title: Journal of medicinal chemistry Volume: 30 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 1987 Apr |
Date Detail:
|
Created Date: 1987-05-11 Completed Date: 1987-05-11 Revised Date: 2006-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: UNITED STATES |
Other Details:
|
Languages: eng Pagination: 743-6 Citation Subset: IM |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Baclofen / analogs & derivatives*, chemical synthesis, metabolism, pharmacology Cerebral Cortex / metabolism Male Rats Rats, Inbred Strains Receptors, GABA-A / drug effects*, metabolism Receptors, GABA-B Stereoisomerism Structure-Activity Relationship gamma-Aminobutyric Acid / analogs & derivatives*, chemical synthesis, metabolism, pharmacology |
| Chemical | |
Reg. No./Substance:
|
0/Receptors, GABA-A; 0/Receptors, GABA-B; 1134-47-0/Baclofen; 56-12-2/gamma-Aminobutyric Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Beta-adrenoceptor antagonist activity of bivalent ligands. 1. Diamide analogues of practolol.
Next Document: Resolution of racemic carbocyclic analogues of purine nucleosides through the action of adenosine de...