Antinociceptive Activity of a New Benzofuranone Derived from a Chalcone

:  Chalcones represent an important group of natural or synthetic compounds with a variety of biological activities including antinociceptive and anti‐inflammatory ones. The aim of this work was the synthesis of a new benzofuranone compound and evaluation of its antinociceptive potential in mice. Th...

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Bibliographic Details
Published in:Basic & clinical pharmacology & toxicology 2009-10, Vol.105 (4), p.257-261
Main Authors: Padaratz, Pâmela, Fracasso, Mauricio, De Campos‐Buzzi, Fátima, Corrêa, Rogério, Niero, Rivaldo, Monache, Franco Delle, Cechinel‐Filho, Valdir
Format: Article
Language:English
Subjects:
Acetaminophen - pharmacology
Analgesics - pharmacology
Animals
Anti-Inflammatory Agents - pharmacology
Aspirin - pharmacology
Benzofurans - chemical synthesis
Benzofurans - pharmacology
Biological and medical sciences
Capsaicin - metabolism
Chalcone - chemical synthesis
Chalcone - pharmacology
Dose-Response Relationship, Drug
Formaldehyde - metabolism
Glutamic Acid - metabolism
Linear Models
Male
Medical sciences
Mice
Nociception - drug effects
Pain - drug therapy
Pain Measurement
Pharmacology. Drug treatments
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Summary::  Chalcones represent an important group of natural or synthetic compounds with a variety of biological activities including antinociceptive and anti‐inflammatory ones. The aim of this work was the synthesis of a new benzofuranone compound and evaluation of its antinociceptive potential in mice. The new benzofuranone 4 was synthesized from chalcone 3. The antinociceptive activity of 4 was determined by writhing, formalin, capsaicin, and glutamate and hot‐plate tests. Compound 4 caused potent and dose‐related inhibition against the writhing test with ID50 6.1 (5.1−7.6) μmol/kg, i.p., being about 15 times more active than the reference drugs, acetyl salicylic acid and acetaminophen. It was also effective in a dose‐dependent manner in significantly reducing the painful stimulus in both phases of formalin, in the capsaicin and in the glutamate test with ID50 values of 27.3 (24.5−30.6) and 18.9 (18.5−19.4) μmol/kg (first and second phase), 12.6 (9.8−16.2) and 24.5 (20.4−29.6) μmol/kg respectively. The results showed that the studied compound exhibits both central and peripheral antinociceptive activities and might be further used as a model to obtain new and more potent analgesic drugs.
ISSN:1742-7835
1742-7843
DOI:10.1111/j.1742-7843.2009.00441.x