3-Arylcoumarins: synthesis and potent anti-inflammatory activity

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5432-4. doi: 10.1016/j.bmcl.2014.10.033.

Wenchen Pu, Yuan Lin, Jianshuo Zhang, Fei Wang, Chun Wang, Guolin Zhang

PMID: 25453803 DOI: 10.1016/j.bmcl.2014.10.033

Abstract

Chronic inflammation is the persistent and excessive immune response and can lead to a variety of diseases. Aiming to discover new compounds with anti-inflammatory activity, we report herein the synthesis and biological evaluation of 3-arylcoumarins. Thirty five 3-arylcoumarins were prepared through Perkin condensation and further acid-promoted hydrolysis if necessary. In lipopolysaccharide-activated mouse macrophage RAW264.7 cells, 6,8-dichloro-3-(2-methoxyphenyl)coumarin (16) and 6-bromo-8-methoxy-3-(3-methoxyphenyl)coumarin (25) exhibited nitric oxide production inhibitory activity with the IC₅₀ values of 8.5 μM and 6.9 μM, respectively, providing a pharmacological potential as anti-inflammatory agents.

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