Synthesis and antinociceptive activity of seselin derivatives.
- Author:
Huan-fang GUO
1
;
Pei-lan ZHOU
;
Ze-hui GONG
;
Lan XIE
Author Information
1. Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
- Publication Type:Journal Article
- MeSH:
Analgesics;
chemical synthesis;
chemistry;
pharmacology;
Animals;
Chromones;
chemical synthesis;
chemistry;
pharmacology;
Coumarins;
chemical synthesis;
chemistry;
pharmacology;
Female;
Male;
Mice;
Molecular Structure;
Pain Measurement;
drug effects
- From:
Acta Pharmaceutica Sinica
2008;43(9):930-933
- CountryChina
- Language:Chinese
-
Abstract:
Natural product seselin and related derivatives with an angular pyranocoumarin skeleton were synthesized from 8-acetyl-7-hydroxycoumarins by condensation with acetone, reduction, and dehydration successively under mild conditions with total yield of > 50%. Twelve seselin derivatives were tested by the writhing response assay induced by acetic acid at a dose of 40 mg x kg(-1). Seselin (4a) and 4,8,8-trimethyl-9,9-dihydro-pyran[2,3-f] chromene-2,10-dione (2b) showed obviously antinociceptive activity with inhibitory effect of 85% and 50%, respectively, more or quite potent than aspirin in the same assay, suggesting that seselin derivatives could be a novel kind of potential antinociceptive agents.
