Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: orally effective anti-inflammatory drug candidates.

Article Details

Citation
Copy to clipboard

Tributino JL, Duarte CD, Correa RS, Doriguetto AC, Ellena J, Romeiro NC, Castro NG, Miranda AL, Barreiro EJ, Fraga CA

Novel 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazones: orally effective anti-inflammatory drug candidates.

Bioorg Med Chem. 2009 Feb 1;17(3):1125-31. doi: 10.1016/j.bmc.2008.12.045. Epub 2008 Dec 25.

PubMed ID
19135376 [ View in PubMed
]
Abstract

We described herein the molecular design of novel in vivo anti-inflammatory 6-methanesulfonamide-3,4-methylenedioxyphenyl-N-acylhydrazone derivatives (1) planned by applying the molecular hybridization approach. This work also points out to the discovery of LASSBio-930 (1c) as a novel anti-inflammatory and anti-hyperalgesic prototype, which was able to reduce carrageenan-induced rat paw edema with an ED(50) of 97.8 micromol/kg, acting mainly as a non-selective COX inhibitor.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
NimesulideProstaglandin G/H synthase 2IC 50 (nM)3500N/AN/ADetails