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J Med Chem. 2012 Oct 25;55(20):8958-62. doi: 10.1021/jm3010543. Epub 2012 Oct 9.

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

Author information

1
Department of Pharmaceutical/Medicinal Chemistry, Eberhard Karls University, Tübingen, Auf der Morgenstelle 8, D-72076 Tübingen, Germany.

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.

PMID:
22992107
DOI:
10.1021/jm3010543
[Indexed for MEDLINE]

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