3-Arylcoumarins: Synthesis and potent anti-inflammatory activity |
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| Institution: | 1. Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, PR China;2. University of Chinese Academy of Sciences, Beijing 100049, PR China;3. College of Life Sciences, Sichuan University, Chengdu 610064, PR China;1. Department of Anesthesiology of Affiliated Tumor Hospital of Xiang-Ya Medical College of Central South University, Changsha, China;2. Department of Anesthesiology of University of Miami Miller School of Medicine, Miami, FL, USA;3. Second Xiangya Hospital of Xiangya Medical School, Central South University, Changsha, China;1. Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Joan XXIII 27-31, 08028 Barcelona, Spain;2. Department of Pathogen Molecular Biology, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, United Kingdom;3. Bradford School of Pharmacy, University of Bradford, West Yorkshire BD7 1 DP, United Kingdom;4. Department of Pharmaceutics, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana;5. Departament de Farmacologia, de Terapèutica i de Toxicologia, Universitat Autònoma de Barcelona, 08193-Bellaterra, Barcelona, Spain;1. Department of Chemistry, Faculty of Arts & Science, Yildiz Technical University, Istanbul, Turkey;2. Bioengineering Department, Chemistry and Metallurgy Faculty, Yildiz Technical University, Istanbul, Turkey;1. School of Pharmacy, Anhui Medical University, Hefei 230032, PR China;2. Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China;3. State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China |
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| 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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| Keywords: | Anti-inflammatory activity Nitric oxide production Coumarin Perkin reaction |
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