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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Oral
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry*
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Benzodioxoles / chemical synthesis
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Benzodioxoles / chemistry*
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Benzodioxoles / pharmacology*
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Carrageenan / chemistry
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Computer Simulation
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Crystallography, X-Ray
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Cyclooxygenase Inhibitors / metabolism
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Disease Models, Animal
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Edema / chemically induced
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Edema / drug therapy
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Edema / prevention & control
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Female
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Hydrazones / chemical synthesis
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Hydrazones / chemistry*
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Hydrazones / pharmacology*
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Male
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Rats
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Rats, Wistar
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Thermodynamics
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Benzodioxoles
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Cyclooxygenase Inhibitors
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Hydrazones
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N-(6-((2-benzylidenehydrazinyl)carbonyl)-1,3-benzodioxol-5-yl)methanesulfonamide
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Carrageenan