Abstract：
: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.
journal_name
Basic Clin Pharmacol Toxicoljournal_title
Basic & clinical pharmacology & toxicologyauthors
Padaratz P,Fracasso M,de Campos-Buzzi F,Corrêa R,Niero R,Delle Monache F,Cechinel-Filho Vdoi
10.1111/j.1742-7843.2009.00441.xsubject
Has Abstractpub_date
2009-10-01 00:00:00pages
257-61issue
4eissn
1742-7835issn
1742-7843pii
PTO441journal_volume
105pub_type
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