Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX.

Abstract

mPGES-1 is a promising target for development of new anti-inflammatory drugs. We aimed to create mPGES-1 inhibitors by modifying the structure of NSAIDs by replacing the carboxylic acid functionality by sulfonamide moieties. Compounds were also tested for 5-LOX inhibition. The most potent mPGES-1 inhibitor was lonazolac derivative 22 (IC₅₀ = 0.16 μM), while the best 5-LOX inhibition was attained by indomethacin derivative 17 (IC₅₀ = 0.9 μM). Inhibition of COX-1 activity was completely removed.

DOI: 10.1021/jm3010543

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@article{Elkady2012ModifiedAN, title={Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX.}, author={Mahmoud Elkady and Raimund Niess and Anja Schaible and Julia Bauer and Susann Luderer and Giulia Ambrosi and Oliver Werz and Stefan A Laufer}, journal={Journal of medicinal chemistry}, year={2012}, volume={55 20}, pages={8958-62} }